PROTAC therapy as a new targeted therapy for lung cancer

Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries

Sung, H., Ferlay, J., Siegel, R. L., Laversanne, M., Soerjomataram, I., Jemal, A., & Bray, F. (2021) · CA: A Cancer Journal for Clinicians · doi:10.3322/caac.21660 · Cited by 108,699 · see citing works

Cancer statistics, 2022

Siegel, R. L., Miller, K. D., Fuchs, H. E., & Jemal, A. (2022) · CA: A Cancer Journal for Clinicians · doi:10.3322/caac.21708 · Cited by 17,196 · see citing works

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib

Lynch, T. J., Bell, D. W., Sordella, R., Gurubhagavatula, S., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Haserlat, S. M., Supko, J. G., Haluska, F. G., et al. (2004) · New England Journal of Medicine · doi:10.1056/nejmoa040938 · Cited by 11,486 · see citing works

<i>EGFR</i> Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy

Paez, J. G., Jänne, P. A., Lee, J. C., Tracy, S., Greulich, H., Gabriel, S., Herman, P., Kaye, F. J., Lindeman, N., Boggon, T. J., et al. (2004) · Science · doi:10.1126/science.1099314 · Cited by 9,368 · see citing works

Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma

Mok, T. S., Wu, Y.-L., Thongprasert, S., Yang, C.-H., Chu, D.-T., Saijo, N., Sunpaweravong, P., Han, B., Margono, B., Ichinose, Y., et al. (2009) · New England Journal of Medicine · doi:10.1056/nejmoa0810699 · Cited by 8,261 · see citing works

Comprehensive molecular profiling of lung adenocarcinoma

The Cancer Genome Atlas Research Network (2014) · Nature · doi:10.1038/nature13385 · Cited by 5,732 · see citing works

Osimertinib in Untreated <i>EGFR</i> -Mutated Advanced Non–Small-Cell Lung Cancer

Soria, J.-C., Ohe, Y., Vansteenkiste, J., Reungwetwattana, T., Chewaskulyong, B., Lee, K. H., Dechaphunkul, A., Imamura, F., Nogami, N., Kurata, T., et al. (2018) · New England Journal of Medicine · doi:10.1056/nejmoa1713137 · Cited by 5,508 · see citing works

Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial

Rosell, R., Carcereny, E., Gervais, R., Vergnenegre, A., Massuti, B., Felip, E., Palmero, R., Garcia-Gomez, R., Pallares, C., Sanchez, J. M., et al. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(11)70393-x · Cited by 5,489 · see citing works

Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer

Soda, M., Choi, Y. L., Enomoto, M., Takada, S., Yamashita, Y., Ishikawa, S., Fujiwara, S.-I., Watanabe, H., Kurashina, K., Hatanaka, H., et al. (2007) · Nature · doi:10.1038/nature05945 · Cited by 5,439 · see citing works

The biology and management of non-small cell lung cancer

Herbst, R. S., Morgensztern, D., & Boshoff, C. (2018) · Nature · doi:10.1038/nature25183 · Cited by 4,891 · see citing works

Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial

Mitsudomi, T., Morita, S., Yatabe, Y., Negoro, S., Okamoto, I., Tsurutani, J., Seto, T., Satouchi, M., Tada, H., Hirashima, T., et al. (2010) · The Lancet Oncology · doi:10.1016/s1470-2045(09)70364-x · Cited by 4,090 · see citing works

Comprehensive genomic characterization of squamous cell lung cancers

The Cancer Genome Atlas Research Network (2012) · Nature · doi:10.1038/nature11404 · Cited by 3,994 · see citing works

PROTAC targeted protein degraders: the past is prologue

Békés, M., Langley, D. R., & Crews, C. M. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00371-6 · Cited by 3,395 · see citing works

Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma With <i>EGFR</i> Mutations

Sequist, L. V., Yang, J. C.-H., Yamamoto, N., O'Byrne, K., Hirsh, V., Mok, T., Geater, S. L., Orlov, S., Tsai, C.-M., Boyer, M., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2012.44.2806 · Cited by 3,228 · see citing works

Overall Survival with Osimertinib in Untreated, <i>EGFR</i> -Mutated Advanced NSCLC

Ramalingam, S. S., Vansteenkiste, J., Planchard, D., Cho, B. C., Gray, J. E., Ohe, Y., Zhou, C., Reungwetwattana, T., Cheng, Y., Chewaskulyong, B., et al. (2020) · New England Journal of Medicine · doi:10.1056/nejmoa1913662 · Cited by 2,914 · see citing works

Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation

Sakamoto, K. M., Kim, K. B., Kumagai, A., Mercurio, F., Crews, C. M., & Deshaies, R. J. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.141230798 · Cited by 2,609 · see citing works

Comprehensive genomic profiles of small cell lung cancer

George, J., Lim, J. S., Jang, S. J., Cun, Y., Ozretić, L., Kong, G., Leenders, F., Lu, X. L., Fernandez‐Cuesta, L., Bosco, G., et al. (2015) · Nature · doi:10.1038/nature14664 · Cited by 2,325 · see citing works

Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial

Wu, Y.-L., Zhou, C., Hu, C.-P., Feng, J., Lu, S., Huang, Y., Li, W., Hou, M., Shi, J. H., Lee, K. Y., et al. (2014) · The Lancet Oncology · doi:10.1016/s1470-2045(13)70604-1 · Cited by 1,978 · see citing works

RAS Proteins and Their Regulators in Human Disease

Simanshu, D. K., Nissley, D. V., & McCormick, F. (2017) · Cell · doi:10.1016/j.cell.2017.06.009 · Cited by 1,943 · see citing works

Phthalimide conjugation as a strategy for in vivo target protein degradation

Winter, G. E., Buckley, D. L., Paulk, J., Roberts, J. M., Souza, A., Dhe-Paganon, S., & Bradner, J. E. (2015) · Science · doi:10.1126/science.aab1433 · Cited by 1,760 · see citing works

KRAS ^G12C Inhibition with Sotorasib in Advanced Solid Tumors

Hong, D. S., Fakih, M. G., Strickler, J. H., Desai, J., Durm, G. A., Shapiro, G. I., Falchook, G. S., Price, T. J., Sacher, A., Denlinger, C. S., et al. (2020) · New England Journal of Medicine · doi:10.1056/nejmoa1917239 · Cited by 1,733 · see citing works

The 2021 WHO Classification of Lung Tumors: Impact of Advances Since 2015

Nicholson, A. G., Tsao, M., Beasley, M. B., Borczuk, A., Brambilla, E. M., Cooper, W. A., Đačić, S., Jain, D., Kerr, K. M., Lantuéjoul, S., et al. (2021) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2021.11.003 · Cited by 1,606 · see citing works

Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials

Yang, J. C.-H., Wu, Y.-L., Schuler, M., Sebastian, M., Popat, S., Yamamoto, N., Zhou, C., Hu, C.-P., O'Byrne, K., Feng, J., et al. (2015) · The Lancet Oncology · doi:10.1016/s1470-2045(14)71173-8 · Cited by 1,574 · see citing works

Acquired Resistance to KRAS ^G12C Inhibition in Cancer

Awad, M. M., Liu, S., Rybkin, I. I., Arbour, K. C., Dilly, J., Zhu, V. W., Johnson, M. L., Heist, R. S., Patil, T., Riely, G. J., et al. (2021) · New England Journal of Medicine · doi:10.1056/nejmoa2105281 · Cited by 1,247 · see citing works

Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial

Wu, Y.-L., Cheng, Y., Zhou, X., Lee, K. H., Nakagawa, K., Niho, S., Tsuji, F., Linke, R., Rosell, R., Corral, J., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30608-3 · Cited by 1,216 · see citing works

Distinct patterns of somatic genome alterations in lung adenocarcinomas and squamous cell carcinomas

Cancer Genome Atlas Research Network, Campbell, J. D., Alexandrov, A., Kim, J., Wala, J., Berger, A. H., Pedamallu, C. S., Shukla, S. A., Guo, G., Brooks, A. N., et al. (2016) · Nature Genetics · doi:10.1038/ng.3564 · Cited by 1,200 · see citing works

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Lu, J., Qian, Y., Altieri, M., Dong, H., Wang, J., Raina, K., Hines, J., Winkler, J. D., Crew, A. P., Coleman, K., et al. (2015) · Chemistry &amp; Biology · doi:10.1016/j.chembiol.2015.05.009 · Cited by 1,140 · see citing works

Adagrasib in Non–Small-Cell Lung Cancer Harboring a <i> KRAS ^G12C </i> Mutation

Jänne, P. A., Riely, G. J., Gadgeel, S. M., Heist, R. S., Ou, S.-H. I., Pacheco, J. M., Johnson, M. L., Sabari, J. K., Leventakos, K., Yau, E., et al. (2022) · New England Journal of Medicine · doi:10.1056/nejmoa2204619 · Cited by 1,061 · see citing works

Targeted protein degradation: expanding the toolbox

Schapira, M., Calabrese, M. F., Bullock, A. N., & Crews, C. M. (2019) · Nature Reviews Drug Discovery · doi:10.1038/s41573-019-0047-y · Cited by 960 · see citing works

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

Khan, S., Zhang, X., Lv, D., Zhang, Q., He, Y., Zhang, P., Liu, X., Thummuri, D., Yuan, Y., Wiegand, J. S., et al. (2019) · Nature Medicine · doi:10.1038/s41591-019-0668-z · Cited by 688 · see citing works

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

Burslem, G. M., Smith, B. E., Lai, A. C., Jaime-Figueroa, S., McQuaid, D. C., Bondeson, D. P., Toure, M., Dong, H., Qian, Y., Wang, J., et al. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.09.009 · Cited by 686 · see citing works

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

Bai, L., Zhou, H., Xu, R., Zhao, Y., Chinnaswamy, K., McEachern, D., Chen, J., Yang, C.-Y., Liu, Z., Wang, M., et al. (2019) · Cancer Cell · doi:10.1016/j.ccell.2019.10.002 · Cited by 652 · see citing works

EGFR in Cancer: Signaling Mechanisms, Drugs, and Acquired Resistance

Uribe, M. L., Marrocco, I., & Yarden, Y. (2021) · Cancers · doi:10.3390/cancers13112748 · Cited by 604 · see citing works

The biology and treatment of EML4-ALK non-small cell lung cancer

Sasaki, T., Rodig, S. J., Chirieac, L. R., & Janne, P. A. (2010) · European Journal of Cancer · doi:10.1016/j.ejca.2010.04.002 · Cited by 556 · see citing works

Third-generation EGFR and ALK inhibitors: mechanisms of resistance and management

Cooper, A. J., Sequist, L. V. D., & Lin, J. J. (2022) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-022-00639-9 · Cited by 525 · see citing works

Targeted Degradation of Oncogenic KRAS ^G12C by VHL-Recruiting PROTACs

Bond, M. J., Chu, L., Nalawansha, D. A., Li, K., & Crews, C. M. (2020) · ACS Central Science · doi:10.1021/acscentsci.0c00411 · Cited by 450 · see citing works

Targeted protein degraders crowd into the clinic

Mullard, A. (2021) · Nature Reviews Drug Discovery · doi:10.1038/d41573-021-00052-4 · Cited by 409 · see citing works

Drugging RAS: know the enemy

Papke, B., & Der, C. J. (2017) · Science · doi:10.1126/science.aam7622 · Cited by 399 · see citing works

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Zhou, B. N., Hu, J., Xu, F., Chen, Z., Bai, L., Fernández‐Salas, E., Lin, M., Liu, L., Yang, C., Zhao, Y., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01816 · Cited by 372 · see citing works

Light-induced control of protein destruction by opto-PROTAC

Liu, J., Chen, H., Ma, L., He, Z., Wang, D., Liu, Y., Lin, Q., Zhang, T., Gray, N. S., Kanıskan, H. Ü., et al. (2020) · Science Advances · doi:10.1126/sciadv.aay5154 · Cited by 305 · see citing works

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation

Cromm, P. M., Samarasinghe, K. T. G., Hines, J., & Crews, C. M. (2018) · Journal of the American Chemical Society · doi:10.1021/jacs.8b08008 · Cited by 293 · cited 1× · see citing works

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Qin, C., Hu, Y., Zhou, B., Fernandez-Salas, E., Yang, C.-Y., Liu, L., McEachern, D., Przybranowski, S., Wang, M., Stuckey, J., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00506 · Cited by 281 · see citing works

Exploring Targeted Degradation Strategy for Oncogenic KRASG12C

Zeng, M., Xiong, Y., Safaee, N., Nowak, R. P., Donovan, K. A., Yuan, C. J., Nabet, B., Gero, T. W., Feru, F., Li, L., et al. (2020) · Cell Chemical Biology · doi:10.1016/j.chembiol.2019.12.006 · Cited by 275 · see citing works

The PROTACtable genome

Schneider, M., Radoux, C. J., Hercules, A., Ochoa, D., Dunham, I., Zalmas, L.-P., Hessler, G., Ruf, S., Shanmugasundaram, V., Hann, M. M., et al. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00245-x · Cited by 273 · see citing works

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

Khan, S., He, Y., Zhang, X., Yuan, Y., Pu, S., Kong, Q., Zheng, G., & Zhou, D. (2020) · Oncogene · doi:10.1038/s41388-020-1336-y · Cited by 252 · see citing works

Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic

Hu, Z., & Crews, C. M. (2022) · ChemBioChem · doi:10.1002/cbic.202100270 · Cited by 231 · see citing works

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK)

Zhang, C., Han, X.-R., Yang, X., Jiang, B., Liu, J., Xiong, Y., & Jin, J. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.03.071 · Cited by 226 · see citing works

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

Powell, C. E., Gao, Y., Tan, L., Donovan, K. A., Nowak, R. P., Loehr, A., Bahcall, M., Fischer, E. S., Jänne, P. A., George, R. E., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01655 · Cited by 198 · see citing works

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders

Cheng, M., Yu, X., Lu, K. J., Xie, L., Wang, L., Meng, F., Han, X., Chen, X., Liu, J., Xiong, Y., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01566 · Cited by 197 · see citing works

The Role of STAT3 in Non-Small Cell Lung Cancer

Harada, D., Takigawa, N., & Kiura, K. (2014) · Cancers · doi:10.3390/cancers6020708 · Cited by 192 · see citing works

Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

Wang, M., Lu, J., Wang, M., Yang, C.-Y., & Wang, S. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00471 · Cited by 172 · see citing works

Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity,

Lv, D., Pal, P., Liu, X., Jia, Y., Thummuri, D., Zhang, P., Hu, W., Pei, J., Zhang, Q., Zhou, S., et al. (2021) · Nature Communications · doi:10.1038/s41467-021-27210-x · Cited by 158 · see citing works

Mutant-selective degradation by BRAF-targeting PROTACs

Alabi, S., Jaime-Figueroa, S., Yao, Z., Gao, Y., Hines, J., Samarasinghe, K. T. G., Vogt, L., Rosen, N., & Crews, C. M. (2021) · Nature Communications · doi:10.1038/s41467-021-21159-7 · Cited by 152 · see citing works

Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations

Jang, J., To, C., Clercq, D. J. H. D., Park, E., Ponthier, C. M., Shin, B. H., Mushajiang, M., Nowak, R. P., Fischer, E. S., Eck, M. J., et al. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.202003500 · Cited by 151 · see citing works

Development of hypoxia-activated PROTAC exerting a more potent effect in tumor hypoxia than in normoxia

Cheng, W., Li, S., Wen, X., Han, S., Wang, S., Han, W., Song, Z., Wang, Y., Tian, X., & Zhang, X. (2021) · Chemical Communications · doi:10.1039/d1cc05715d · Cited by 129 · see citing works

Functional characterization of a PROTAC directed against BRAF mutant V600E

Posternak, G., Tang, X., Maisonneuve, P., Jin, T., Lavoie, H., Daou, S., Orlicky, S. M., de Rugy, T. G., Caldwell, L., Chan, K., et al. (2020) · Nature Chemical Biology · doi:10.1038/s41589-020-0609-7 · Cited by 128 · see citing works

Overcoming Cancer Drug Resistance Utilizing PROTAC Technology

Burke, M. R., Smith, A. R., & Zheng, G. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.872729 · Cited by 126 · see citing works

Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)

Kang, C. H., Lee, D.-H., Lee, C. O., Ha, J. D., Park, C. H., & Hwang, J. Y. (2018) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2018.09.169 · Cited by 126 · see citing works

Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems

Qu, X., Liu, H., Song, X., Sun, N., Zhong, H., Qiu, X., Yang, X., & Jiang, B. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113328 · Cited by 120 · see citing works

6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases

Wood, E. R., Shewchuk, L. M., Ellis, B., Brignola, P. S., Brashear, R. L., Caferro, T. R., Dickerson, S. H., Dickson, H. D., Donaldson, K. H., Gaul, M. D., et al. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0708281105 · Cited by 113 · see citing works

Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC

Yang, F., Wen, Y., Wang, C., Zhou, Y., Zhou, Y., Zhang, Z.-M., Liu, T., & Lu, X. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.114088 · Cited by 109 · see citing works

Design and synthesis of selective degraders of EGFRL858R/T790M mutant

Zhang, X., Xu, F., Tong, L., Zhang, T., Xie, H., Lu, X., Ren, X., & Ding, K. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112199 · Cited by 109 · see citing works

Discovery of potent small molecule PROTACs targeting mutant EGFR

Zhao, H., Yang, X., Lei, H., Xi, X.-X., Lu, S., Zhang, J., Xin, M., & Zhang, S. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112781 · Cited by 105 · see citing works

Clinical considerations for the design of PROTACs in cancer

Nieto‐Jiménez, C., Morafraile, E. C., Alonso‐Moreno, C., & Ocaña, A. (2022) · Molecular Cancer · doi:10.1186/s12943-022-01535-7 · Cited by 99 · see citing works

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands

Zhao, H., Wang, H., Mao, Y.-Z., Zhang, H., Xin, M., Xi, X.-X., Lei, H., Mao, S., Li, D., & Zhang, S. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01827 · Cited by 94 · see citing works

Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations

Zhou, C., Fan, Z., Zhou, Z., Li, Y., Cui, R., Liu, C., Zhou, G., Diao, X., Jiang, H., Zheng, M., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01774 · Cited by 94 · see citing works

Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance

Sun, N., Ren, C., Kong, Y., Zhong, H., Chen, J., Li, Y., Zhang, J., Zhou, Y., Qiu, X., Lin, H., et al. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112190 · Cited by 85 · see citing works

Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK)

Xie, S., Sun, Y., Liu, Y., Li, X., Li, X., Zhong, W., Zhan, F., Zhu, J., Yao, H., Yang, D., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00270 · Cited by 81 · see citing works

HJM-561, a Potent, Selective, and Orally Bioavailable EGFR PROTAC that Overcomes Osimertinib-Resistant EGFR Triple Mutations

Du, Y., Chen, Y., Wang, Y., Chen, J., Lu, X., Zhang, L., Li, Y., Wang, Z., Ye, G., & Zhang, G. (2022) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-0835 · Cited by 78 · see citing works

Discovery of novel potent covalent inhibitor-based EGFR degrader with excellent in vivo efficacy

Shi, S., Du, Y., Huang, L. H., Cui, J., Niu, J., Xu, Y., & Zhu, Q. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.105605 · Cited by 75 · see citing works

Discovery of Selective Small Molecule Degraders of BRAF-V600E

Han, X., Chen, L., Wei, Y., Yu, W., Chen, Y., Zhang, C., Jiao, B., Shi, T., Sun, L., Zhang, C., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b02083 · Cited by 64 · see citing works

BCL-XL PROTAC degrader DT2216 synergizes with sotorasib in preclinical models of KRASG12C-mutated cancers

Khan, S., Wiegand, J., Zhang, P., Hu, W., Thummuri, D., Budamagunta, V., Hua, N., Jin, L., Allegra, C. J., Kopetz, S. E., et al. (2022) · Journal of Hematology &amp; Oncology · doi:10.1186/s13045-022-01241-3 · Cited by 62 · see citing works

Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation

Zhang, H., Xie, R., AI-furas, H., Li, Y., Wu, Q., Li, J., Xu, F., & Xu, T. (2022) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.1c00645 · Cited by 60 · see citing works

Discovery of a PROTAC targeting ALK with in vivo activity

Yan, G., Zhong, X.-X., Lin, Y., Pu, C., Shan, H., Lan, S., Zhou, M., Hou, X., Yang, J., & Li, R. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.113150 · Cited by 59 · see citing works

BRD4 Levels Determine the Response of Human Lung Cancer Cells to BET Degraders That Potently Induce Apoptosis through Suppression of Mcl-1

Zong, D., Gu, J., Cavalcante, G. C., Yao, W., Zhang, G., Wang, S., Owonikoko, T. K., He, X., & Sun, S. (2020) · Cancer Research · doi:10.1158/0008-5472.can-19-3674 · Cited by 59 · see citing works

Clinical evaluation of dacomitinib for the treatment of metastatic non-small cell lung cancer (NSCLC): current perspectives

Lavacchi, D., Mazzoni, F., & Giaccone, G. (2019) · Drug Design Development and Therapy · doi:10.2147/dddt.s194231 · Cited by 58 · see citing works

Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib

Ren, C., Sun, N., Kong, Y., Qu, X., Liu, H., Zhong, H., Song, X., Yang, X., & Jiang, B. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113335 · Cited by 49 · see citing works

Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo

Zhang, W., Li, P., Sun, S., Jia, C., Yang, N., Zhuang, X., Zheng, Z., & Li, S. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114509 · Cited by 42 · see citing works

Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile

Ren, C., Sun, N., Liu, H., Kong, Y., Sun, R., Qiu, X., Chen, J., Li, Y., Zhang, J., Zhou, Y., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00373 · Cited by 41 · see citing works

Susceptibility of Lung Carcinoma Cells to Nanostructured Lipid Carrier of ARV-825, a BRD4 Degrading Proteolysis Targeting Chimera

Vartak, R., Saraswat, A. L., Yang, Y., Chen, Z., & Patel, K. R. (2022) · Pharmaceutical Research · doi:10.1007/s11095-022-03184-3 · Cited by 39 · see citing works

FAK-targeting PROTAC demonstrates enhanced antitumor activity against KRAS mutant non-small cell lung cancer

Liu, J., Xue, L., Xu, X., Luo, J., & Zhang, S. (2021) · Experimental Cell Research · doi:10.1016/j.yexcr.2021.112868 · Cited by 33 · see citing works

Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study

Sun, Y., Wang, R., Sun, Y., Wang, L., Xue, Y., Wang, J., Wu, T., Yin, W., Qin, Q., Sun, Y., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114373 · Cited by 33 · see citing works

Whole-genome characterization of lung adenocarcinomas lacking alterations in the RTK/RAS/RAF pathway

Carrot‐Zhang, J., Yao, X., Devarakonda, S. H. K., Deshpande, A. S., Damrauer, J. S., Silva, T. C., Wong, C. K., Choi, H. Y., Felau, I., Robertson, A. G., et al. (2021) · Cell Reports · doi:10.1016/j.celrep.2021.108707 · Cited by 30 · see citing works

Design and Synthesis of Proteolysis Targeting Chimeras (Protacs) as an Egfr Degrader Based on Co-1686

Li, Q., Guo, Q., Wang, S., Wan, S., Li, Z., Zhang, J., & Wu, X. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114455 · Cited by 30 · see citing works

Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models

Sun, D., Nikonova, A. S., Zhang, P., Deneka, A. Y., Fitzgerald, M. E., Michael, R. E., Lee, L., Lilly, A. C., Fisher, S. L., Phillips, A. J., et al. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0831 · Cited by 13 · see citing works

Therapeutic efficacy of the novel SHP2 degrader SHP2-D26, alone or in combination, against lung cancer is associated with modulation of p70S6K/S6, Bim and Mcl-1

Deng, Y., Ma, G., Vallega, K. A., Wang, D., Wang, M., Wang, C., Wang, S., Ramalingam, S. S., & Sun, S. (2022) · Cancer Gene Therapy · doi:10.1038/s41417-022-00472-3 · Cited by 12 · see citing works

Pilot Study of Dacomitinib for Patients With Metastatic EGFR-Mutant Lung Cancers With Disease Progression After Initial Treatment With Osimertinib

Choudhury, N. J., Makhnin, A., Tobi, Y. Y., Daly, R. M., Preeshagul, I. R., Iqbal, A. N., Ahn, L. S. H., Hayes, S. A., Heller, G., Kris, M. G., et al. (2021) · JCO Precision Oncology · doi:10.1200/po.21.00005 · Cited by 11 · see citing works

The novel BET degrader, QCA570, is highly active against the growth of human NSCLC cells and synergizes with osimertinib in suppressing osimertinib-resistant EGFR-mutant NSCLC cells.

Liu, C., Qian, L., Vallega, K. A., Ma, G., Zong, D., Chen, L., Wang, S., Ramalingam, S. R., Qin, Z. S., & Sun, S. (2022) · PubMed Central · Cited by 9 · see citing works

Rare molecular subtypes of lung cancer

Harada, G., Yang, S., Cocco, E., & Drilon, A. E. D. C. (2023) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-023-00733-6 · Cited by 122 · see citing works

PROTACs: Emerging Targeted Protein Degradation Approaches for Advanced Druggable Strategies

Sincere, N. I., Anand, K., Ashique, S., Yang, J., & You, C. (2023) · Molecules · doi:10.3390/molecules28104014 · Cited by 109 · see citing works

20 years since the approval of first EGFR-TKI, gefitinib: Insight and foresight

Singh, S. K., Sadhukhan, S., & Sonawane, A. (2023) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2023.188967 · Cited by 104 · see citing works

PROTACs: A novel strategy for cancer drug discovery and development

Han, X., & Sun, Y. (2023) · MedComm · doi:10.1002/mco2.290 · Cited by 67 · see citing works

Leveraging aptamers for targeted protein degradation

Yang, Z., Pang, Q., Zhou, J., Xuan, C., & Xie, S. (2023) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2023.05.008 · Cited by 50 · see citing works

Efficacy and Safety Evaluation of 177Lu-FAP-2286 in the Treatment of Advanced Lung Cancer

Xie, Y., Ma, J., Tang, W., Zhang, Y., Zhang, C., & Chen, Y. (2024) · Clinical Nuclear Medicine · doi:10.1097/rlu.0000000000005297 · Cited by 47 · see citing works

Unconventional PROTACs for Targeted Protein Degradation in Cancer Therapy

Zhang, X., Song, Z., Zhang, X., Zou, J., Yu, G., Chen, X. S., & Wang, S. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202507702 · Cited by 41 · see citing works

Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions

Fan, G., Chen, S., Zhang, Q., Yu, N., Shen, Z., Liu, Z., Guo, W., Tang, Z., Yang, J., & Liu, M. (2025) · MedComm · doi:10.1002/mco2.70401 · Cited by 44 · see citing works

Targeted Protein Degradation (TPD) for Immunotherapy: Understanding Proteolysis Targeting Chimera-Driven Ubiquitin-Proteasome Interactions

Kamaraj, R., Ghosh, S., Das, S., Sen, S., Kumar, P. R., Majumdar, M., Dasgupta, R., Mukherjee, S., Das, S., Ghose, I., et al. (2024) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.4c00253 · Cited by 37 · see citing works

ALK inhibitors in cancer: mechanisms of resistance and therapeutic management strategies

Poei, D., Ali, S., Ye, S., & Hsu, R. C. (2024) · Cancer Drug Resistance · doi:10.20517/cdr.2024.25 · Cited by 37 · see citing works

The role of E2F2 in cancer progression and its value as a therapeutic target

Gao, Y., Qiao, X., Liu, Z., & Zhang, W. (2024) · Frontiers in Immunology · doi:10.3389/fimmu.2024.1397303 · Cited by 35 · see citing works

Design and optimization strategies of PROTACs and its Application, Comparisons to other targeted protein degradation for multiple oncology therapies

Malarvannan, M., Unnikrishnan, S., Monohar, S., Ravichandiran, V., & Paul, D. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107984 · Cited by 33 · see citing works

Discovery of the GSH responsive “Y-PROTACs” targeting ALK and CDK4/6 as a potential treatment for cancer

Wang, S., Luo, D., Pu, C., Ma, X., Zhang, H., Feng, Z., Deng, R., Yu, S., Liu, Y., Huang, Q., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.115082 · Cited by 31 · see citing works

Regulation of HNRNP family by post-translational modifications in cancer

Li, B., Wen, M., Gao, F., Wang, Y., Wei, G., & Duan, Y. (2024) · Cell Death Discovery · doi:10.1038/s41420-024-02198-7 · Cited by 28 · see citing works

CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications

Thapa, R., Bhat, A. A., Gupta, G., Jyothi, S. R., Kaur, I., Kumar, S., Sharma, N., Prasad, G. V. S., Pramanik, A., & Ali, H. (2024) · Chemical Biology & Drug Design · doi:10.1111/cbdd.70009 · Cited by 24 · see citing works

Advances in metal-based nano drugs and diagnostic probes for tumor

Ding, J., He, Z., Zhai, Y., Ye, L., Ji, J., Yang, X., & Zhai, G. (2023) · Coordination Chemistry Reviews · doi:10.1016/j.ccr.2023.215594 · Cited by 24 · see citing works

Exploiting E3 ligases for lung cancer therapy: The promise of DCAF-PROTACs

Hussain, M. S., Eltaib, L., Rana, A. J., Maqbool, M., Ashique, S., Alanazi, M. N., Khan, Y., & Agrawal, M. (2025) · Pathology - Research and Practice · doi:10.1016/j.prp.2025.156001 · Cited by 22 · see citing works

Targeting KRASG12C in Non-Small-Cell Lung Cancer: Current Standards and Developments

Torres-Jiménez, J., Espinar, J. B., Bote, H., Berjaga, M. Z., Esteban-Villarrubia, J., Fraile, J. Z., & Paz-Ares, L. G. (2024) · Drugs · doi:10.1007/s40265-024-02030-7 · Cited by 22 · see citing works

Computational strategies for PROTAC drug discovery

Wu, J., Wang, W., & Leung, C. (2023) · Acta Materia Medica · doi:10.15212/amm-2022-0041 · Cited by 20 · see citing works

Drp1: Focus on Diseases Triggered by the Mitochondrial Pathway

Sun, F., Fang, M., Zhang, H., Song, Q., Li, S., Li, Y., Jiang, S., & Yang, L. (2024) · Cell Biochemistry and Biophysics · doi:10.1007/s12013-024-01245-5 · Cited by 20 · see citing works

SLC7A11 inhibits ferroptosis and downregulates PD-L1 levels in lung adenocarcinoma

Huang, Z., Chen, X., Wang, Y., Yuan, J., Li, J., Hang, W., & Meng, H. (2024) · Frontiers in Immunology · doi:10.3389/fimmu.2024.1372215 · Cited by 20 · see citing works

EGFR: New Insights on Its Activation and Mutation in Tumor and Tumor Immunotherapy

Gu, Y., He, H., Qiao, S., Shao, Y., Wang, L., Zhang, Z., Zhang, L., & Zhou, F. (2025) · Advanced Science · doi:10.1002/advs.202505785 · Cited by 17 · see citing works

Development of PROTACS degrading KRAS and SOS1

Hamilton, G., Eggerstorfer, M.-T., & Stickler, S. (2024) · Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics · doi:10.32604/or.2024.051653 · Cited by 16 · see citing works

Proteolysis Targeting Chimera Agents (PROTACs): New Hope for Overcoming the Resistance Mechanisms in Oncogene-Addicted Non-Small Cell Lung Cancer

Cordani, N., Nova, D., Sala, L., Abbate, M. I., Colonese, F., Cortinovis, D. L., & Canova, S. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms252011214 · Cited by 17 · see citing works

Recent Advances in the Development of Pro-PROTAC for Selective Protein Degradation

Hakem, F. T., Abdelwaly, A., Alshaman, R., Alattar, A., Alanazi, F. E., Zaitone, S. A., & Helal, M. A. (2025) · Pharmaceutics · doi:10.3390/pharmaceutics17091160 · Cited by 14 · see citing works

YAP at the Crossroads of Biomechanics and Drug Resistance in Human Cancer

Huang, M. L., Wang, H., Mackey, C., Chung, M. C., Guan, J., Zheng, G., Roy, A., Xie, M., Vulpe, C. D., & Tang, X. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms241512491 · Cited by 14 · see citing works

Next-generation cancer therapeutics: PROTACs and the role of heterocyclic warheads in targeting resistance

Omar, E. A., Rajesh, R., Das, P. K., Pal, R., Matada, G. S. P., & Maji, L. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.117034 · Cited by 14 · see citing works

EGFR Targeted Liposomal PROTAC Assisted With Epigenetic Regulation as an Efficient Strategy for Osimertinib‐Resistant Lung Cancer Therapy

Wang, D., Liu, Y., Chen, Y., Dai, C., Hu, W., Han, J., Li, Z., Yin, F., Zhang, Y., & Chen, S. (2025) · Advanced Science · doi:10.1002/advs.202510197 · Cited by 13 · see citing works

Recent advances in medicinal chemistry strategies for the development of METTL3 inhibitors

Li, G., Chen, W., Liu, D., & Tang, S. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117560 · Cited by 13 · see citing works

Resistance in Lung Cancer Immunotherapy and How to Overcome It: Insights from the Genetics Perspective and Combination Therapies Approach

Zieliński, P., Stępień, M., Chowaniec, H., Kalyta, K., Czerniak, J., Borowczyk, M., Dwojak, E., Mroczek, M., Dworacki, G., Ślubowska, A., et al. (2025) · Cells · doi:10.3390/cells14080587 · Cited by 13 · see citing works

Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase

Qiao, J. X., Williams, D., Gill, P., Li, L., Norris, D. J., Tokarski, J. S., Wong, J., Qi, H., Hafeji, Y. A., Downes, D. P., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c02083 · Cited by 11 · see citing works

Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras

Hamilton, G., Stickler, S., & Rath, B. (2023) · Current Pharmaceutical Design · doi:10.2174/1381612829666230418114520 · Cited by 11 · see citing works

Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors

Wang, Q., Zhu, Y., & Pei, J. (2024) · Future Medicinal Chemistry · doi:10.1080/17568919.2024.2389764 · Cited by 10 · see citing works

Targeting Hyaluronan Synthesis in Cancer: A Road Less Travelled

Karalis, T. T. (2023) · Biologics · doi:10.3390/biologics3040022 · Cited by 9 · see citing works

Loss of DDX24 inhibits lung cancer progression by stimulating IKBKG splicing-mediated autophagy

Sun, S., Jing, X., Tong, G., Chen, C., Xie, S., Wang, C., Chen, D., Zhao, J., Qi, Y., Zhang, W., et al. (2025) · Theranostics · doi:10.7150/thno.102425 · Cited by 9 · see citing works

Mechanistic Insights and Therapeutic Potentials of Ubiquitin‐Proteasome System in Non‐Small Cell Lung Cancer

Zhou, G., Tan, J., Zhang, Z., Zhou, Z., Zhang, L., & Zhang, Z. (2025) · Cell Proliferation · doi:10.1111/cpr.70050 · Cited by 9 · see citing works

Fundamental concepts of protein therapeutics and spacing in oncology: an updated comprehensive review

Far, B. F., Safaei, M., Mokhtari, F., Fallahi, M. S., & Naimi‐Jamal, M. R. (2023) · Medical Oncology · doi:10.1007/s12032-023-02026-5 · Cited by 9 · see citing works

The Impact of Genetic Mutations on the Efficacy of Immunotherapies in Lung Cancer

Lui, K., Cheung, K., Ng, W. W. M., Wang, Y., Au, D. W. H., & Cho, W. C. S. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms252211954 · Cited by 8 · see citing works

Discovery of a Novel EGFR PROTAC Degrader against C797S Resistance Mutation with Potent Antitumor Efficacy in NSCLC Treatment

Wang, X., Wang, C., Ma, Y., Piao, Y., Shi, Y., Yang, S., Li, J., & Fan, Y. L. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00693 · Cited by 8 · see citing works

PROTACs in Ovarian Cancer: Current Advancements and Future Perspectives

Vorderbruggen, M., Velázquez‐Martínez, C. A., Natarajan, A., & Karpf, A. R. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25105067 · Cited by 7 · see citing works

Study on the inhibition of non-small cell lung cancer mediated by chitosan-based gene carrier delivering STAT3-shRNA

Zhang, W., Song, L., Zhou, Y., Sun, J., Li, C., Han, B., Chang, J., Han, B., & Wang, T. (2024) · International Journal of Biological Macromolecules · doi:10.1016/j.ijbiomac.2024.138211 · Cited by 7 · see citing works

AXL enhances the self-renewal of cancer stem-like cells and Osimertinib chemoresistance by regulating SCD1 in non-small cell lung cancer

Pan, Q., Yang, X., Chen, Z., Deng, Q., Liu, J., Ke, Y., Lin, F., Huang, W., Lin, Z., Yu, X., et al. (2025) · Biochemical Pharmacology · doi:10.1016/j.bcp.2025.117067 · Cited by 7 · see citing works

Targeted Degradation of Class 1 HDACs With PROTACs is Highly Effective at Inducing DLBCL Cell Death

Alraddadi, A. M., Smalley, J. P., Alzahrani, W., Saleh, A., Al-Mansour, F. S. H., He, B., Cao, T. H., Jayne, S., Dyer, M. J. S., Hodgkinson, J. T., et al. (2025) · eJHaem · doi:10.1002/jha2.70127 · Cited by 7 · see citing works

The Role of Reactive Oxygen Species in Lung Cancer Development: Nanomedicine as a Therapeutic Strategy

Olazábal-Morán, M., Pérez, E., Esteban-Arranz, A., & Garrido, A. (2025) · Biomolecules · doi:10.3390/biom15091316 · Cited by 7 · see citing works

Aurora A degradation by HSP90 interactome-mediating PROTACs in A549 and paclitaxel-resistant A549 cells

Deng, X.-Y., Xu, H., Peng, Y.-X., Guo, Y.-Y., He, R.-F., & Lu, G. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118141 · Cited by 5 · see citing works

Exploratory Analysis of [68Ga]Ga-FAP-2286 PET/CT Quantitative Parameters for Predicting Response to [177Lu]Lu-FAP-2286 Therapy in Non-small Cell Lung Cancer

Fan, M., Guo, X., Liu, G., Tian, C., Zhao, J., & Chen, Y. (2025) · Clinical Nuclear Medicine · doi:10.1097/rlu.0000000000006210 · Cited by 5 · see citing works

Self-assembled Nano-PROTACs: bridging chemical design and biological barriers in targeted protein degradation

Zhang, N., Liang, J.-X., Hu, B.-N., Wang, Y., An, H., & Wang, H. (2026) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2026.115861 · Cited by 5 · see citing works

Targeting KRAS-G12C in lung cancer: The emerging role of PROTACs in overcoming resistance

Chidambaram, K., Rekha, A., Goyal, A., & Rana, M. (2025) · Pathology - Research and Practice · doi:10.1016/j.prp.2025.155954 · Cited by 5 · see citing works

E3 ubiquitin ligases in lung cancer: Emerging insights and therapeutic opportunities

Basu, B., Kal, S., Karmakar, S., Basu, M., & Ghosh, M. K. (2023) · Life Sciences · doi:10.1016/j.lfs.2023.122333 · Cited by 5 · see citing works

Unconventional PROTACs for Targeted Protein Degradation in Cancer Therapy

Zhang, X., Song, Z., Zhang, X., Zou, J., Yu, G., Chen, X. S., & Wang, S. (2025) · Angewandte Chemie · doi:10.1002/ange.202507702 · Cited by 4 · see citing works

Design of conditional and tumor-activated PROTACs for selective degradation in lung cancer

Lin, L., Zheng, F., Wei, H., Wu, X., Yan, H., & Ding, Y. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118432 · Cited by 4 · see citing works

PROTACs in targeted protein degradation: Advances in development and AI-enhanced drug discovery

Du, M., Liu, T., Wang, W., Fan, S., Tian, M., Du, Q., Wang, Z., Li, X., Liu, X., Xia, Q., et al. (2026) · European Journal of Medicinal Chemistry Reports · doi:10.1016/j.ejmcr.2026.100332 · Cited by 4 · see citing works

Revolutionizing lung cancer treatment: Introducing PROTAC therapy as a novel paradigm in targeted therapeutics

Mahajan, A. A., Panzade, G., Bhuniya, T., Das, P., Bhattacharjee, B., Das, S., Chowdhury, A., Chakraborty, K., Guha, S., Samant, A., et al. (2024) · Current Problems in Cancer · doi:10.1016/j.currproblcancer.2024.101172 · Cited by 4 · see citing works

Exosome-mediated intercellular communication and PROTACs delivery: A dual approach for precision therapy in colon cancer

Mohite, P. B., Puri, A. V., Munde, S. V., Yadav, V., Mukerjee, N., Patil, R., Mahindrakar, N., Prasad, G. V. S., Verma, R., & Sinha, A. (2024) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2024.106596 · Cited by 4 · see citing works

Advances of E3 ligases in lung cancer

Yu, J., Zhao, Y., & Xie, Y. (2024) · Biochemistry and Biophysics Reports · doi:10.1016/j.bbrep.2024.101740 · Cited by 4 · see citing works

WDR62 mediates MAPK/ERK pathway to stimulate DNA damage repair and attenuate cisplatin sensitivity in lung adenocarcinoma

Xu, L., Guo, Y., Qi, Z., & Zheng, Y. (2025) · Anti-Cancer Drugs · doi:10.1097/cad.0000000000001682 · Cited by 3 · see citing works

Myc family proteins: Molecular drivers of tumorigenesis and resistance in neuroendocrine tumors

Hylton-McComas, H. M., Cordes, A. F., Floros, K. V., Faber, A. C., Drapkin, B. J., & Miles, W. O. (2025) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2025.189332 · Cited by 3 · see citing works

Hypoxia promotes pancreatic adenocarcinoma progression by stabilizing ID1 via TRIM21 suppression

Cheng, R., Tang, Y., Cao, X., Huang, Z., Guo, Y., Jin, R., Wang, Y., Liu, Y., Xue, L., & Wang, Y. (2025) · Frontiers in Oncology · doi:10.3389/fonc.2025.1616968 · Cited by 3 · see citing works

Selective and spatiotemporal‑resolved nano-PROTAC for lung cancer therapy

Xu, X., Wang, L., Lin, S., Wu, X., Lin, X., Guan, X., Tang, S., Zhang, N., Zhang, Y., Zhang, L., et al. (2025) · Colloids and Surfaces B Biointerfaces · doi:10.1016/j.colsurfb.2025.115135 · Cited by 3 · see citing works

Revolutionizing protein degradation: Harnessing nanoparticles for PROTAC delivery

Fan, Y., Su, J., Yang, J., Guan, X., Gong, Y., Yang, D., Qin, A., & Zhang, L. (2026) · Materials Today Bio · doi:10.1016/j.mtbio.2026.102949 · Cited by 3 · see citing works

Actinidia eriantha Benth. Root as a New Phytomedicine Inhibits Non-Small Cell Lung Cancer by Regulating·TGF-β/FOXO/mTOR

Zhang, X., Xiao, Q., Chen, H., Yang, S., Li, Q., & Peng, L. (2025) · International Journal of Molecular Sciences · doi:10.3390/ijms26188957 · Cited by 2 · see citing works

Multinuclear Ce III –P III –W VI Cluster-Incorporated Phospho(III)tungstate Utilized in a Chip-Based Sensor for the Selective Detection of MicroRNA-21

Liu, G., Jiang, J., Li, Y., Zeng, B., Chen, L., & Zhao, J. (2025) · Inorganic Chemistry · doi:10.1021/acs.inorgchem.5c04297 · Cited by 2 · see citing works

Discovery of a first-in-class protein degrader for the c-ros oncogene 1 (ROS1)

Yang, J., Wu, Y., Zhu, Q., Qu, X., Ou, H., Liu, H., Wei, Y., Ge, D., Lu, C., Jiang, B., et al. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107590 · Cited by 2 · see citing works

Proteolysis Targeting Chimera (PROTACs) in Cancer: From Molecular Mechanisms to Therapeutic Opportunities

Yang, J., Qiao, Q., Lin, N., Niu, M., Su, L., & Yin, B. (2025) · Journal of Biochemical and Molecular Toxicology · doi:10.1002/jbt.70427 · Cited by 2 · see citing works

Self-Sustained Nanozyme Triggers Dual-Pronged Ferroptosis via ROS Storm and Barrier Collapse in a Remodeled Tumor Microenvironment

Hong, S. D., Qin, C., You, Z.-F., Zhang, Y., Wang, K., Jia, X., & Liu, W. (2025) · ACS Applied Nano Materials · doi:10.1021/acsanm.5c03799 · Cited by 1 · see citing works

Role of the SOX family in non‑small cell lung cancer: Molecular mechanisms and therapeutic implications (Review)

Wang, K., Li, Y., Guo, Z., Song, L., Ding, X., Liu, L., Hu, T., Bian, Y., Huang, C., & Miao, L. (2025) · Oncology Reports · doi:10.3892/or.2025.9024 · Cited by 1 · see citing works

Novel PROTACs with polyhedral alkanes as linkers for enhanced ALK degradation in drug-resistant NSCLC

Chu, D., Han, H., Wei, C., Zhang, X., Yan, H., & Wang, J. (2025) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2025.118521 · Cited by 1 · see citing works

Arylidene-Thiazoldione Scaffold Acts as the E3 Ligand of DCAF11 for PROTAC Design

Liang, J., Liu, Y., Zhao, M., Chen, L., Qin, J., Ma, W., Wang, Y., Wu, H., Tian, R., Wei, T., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02188 · Cited by 1 · see citing works

Aptamers targeting immune checkpoints for tumor immunotherapy: a comprehensive review

Gedla, M. K., Kotla, R. S. P., Kumar, R., Kamesh, V., Joshua, S., Kamalakannan, D., & Ramasamy, J. (2026) · Frontiers in Oncology · doi:10.3389/fonc.2026.1762902 · Cited by 1 · see citing works

Bifunctional proximity-inducing strategies for targeted and programmable post-translational modifications

Tanga, S., Das, P., Samoi, T. B., Hota, A., Karmakar, A., & Maji, B. (2026) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2026.115874 · Cited by 1 · see citing works

Anticancer Therapy with Proteolysis-targeting Chimeras [PROTACs] Targeting the Tumor-microenvironment: Development, Current State and Prospects

Vanangamudi, M., Kaushik, M., Guptha, P. M., Surendran, V., & Gupta, P. K. (2024) · Current Cancer Therapy Reviews · doi:10.2174/0115733947304955240430124514 · Cited by 1 · see citing works

Emerging Paradigms in Lung Cancer Treatment: Recent Breakthroughs and Innovation

Zahid, A., Khaliq, A., Nisa, M. U., Maqsood, Q., Hussain, N., Ali, S. W., & Abbas, S. M. (2024) · Interdisciplinary cancer research · doi:10.1007/16833_2024_255 · Cited by 1 · see citing works

8-Aza Quinazolines as Brain Penetrant SOS1 Inhibitors for Treating Cancer

Sabnis, R. W. (2023) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.3c00416 · Cited by 1 · see citing works

An HDAC4-specific PROTAC degrader achieves radiation sensitization by enhancing ferroptosis in lung cancer

Cheng, C., Sun, L., Yang, J., Liu, Z., Zhang, F., Qiu, L., Yu, M., Wang, T., Huang, J., Wang, L., et al. (2026) · Nature Communications · doi:10.1038/s41467-026-73682-0

Role of Ubiquitin Ligases and Conjugases in Targeted Cancer Therapy

Vriend, J. P. (2023) · Cancers · doi:10.3390/cancers15133460

Advances in research of ursolic acid and its derivatives as potential drug candidates against various types of lung cancers

Li, S., Dai, L., Tan, Y., Jiang, K., Wei, X., Hu, Y., Hu, Y., Lin, J., Yao, X., Mi, P., et al. (2023) · Medicinal Chemistry Research · doi:10.1007/s00044-023-03147-2

Delivery Systems: Miniaturised PROTAC, Nano PROTAC, and Aptamer-Based RNA PROTAC

Patel, M. P., Kalyani, H. K., Patel, K. M., Patel, B., Patel, D. H., & Patel, J. K. (2024) · Springer eBooks · doi:10.1007/978-981-97-5077-1_17

Network biology and bioinformatics-based framework to identify the impacts of SARS-CoV-2 infections on lung cancer and tuberculosisPreprint

Waaje, A., Sarkar, M. S., & Islam, M. Z. (2024) · medRxiv · doi:10.1101/2024.09.10.24313452

Effects of microRNA on the growth and targeted therapy response on lung cancer

Zhu, M., Jiang, Y., & Liu, L. (2024) · Clinical and Translational Discovery · doi:10.1002/ctd2.70011

Advancing cancer immunotherapy: Small-Molecule, biomacromolecular, and nanoscale PROTACs targeting PD-L1 for degradation

Meng, Y., Zhang, Y., Yu, W., Xing, D., & Wang, C. (2025) · Materials Today Advances · doi:10.1016/j.mtadv.2025.100606

Autophagosome degraders: a novel therapeutic strategy with broad application potential in human diseases

Zuo, W., Huang, X., Peng, C., Han, B., & Zhao, Q. (2025) · Future Medicinal Chemistry · doi:10.1080/17568919.2025.2605014

Targeting ubiquitin signaling vulnerabilities in KEAP1-inactivated lung cancer

Shah, V. J., Hartmann, O., Wegner, M., Prieto‐Garcia, C., Kazi, R. S., zu Herrnsheim, V. V. H., Wanli, A., Mačinković, I., Bohnacker, B., Husnjak, K., et al. (2026) · The EMBO Journal · doi:10.1038/s44318-026-00737-9

CAR immune cell therapy strategies and advances for lung cancer

Zheng, S., Chen, Y., Li, R., & Peng, S. (2026) · Discover Oncology · doi:10.1007/s12672-026-04981-7

Progressive insights into nanomaterials for cancer starvation therapy

Shi, J., Cui, J., Sun, X., Sun, J., He, Z., Luo, C., & Zhang, S. (2026) · Science China Materials · doi:10.1007/s40843-025-3988-6

BindingDB Entry 50019272: Discovery of the GSH responsive "Y-PROTACs" targeting ALK and CDK4/6 as a potential treatment for cancer.

BindingDB (2024) · UC San Diego · doi:10.7270/q279491k

BindingDB Entry 50020518: 8-Aza Quinazolines as Brain Penetrant SOS1 Inhibitors for Treating Cancer.

BindingDB (2024) · UC San Diego · doi:10.7270/q24m991n

BindingDB Entry 50022702: Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase.

BindingDB (2026) · UC San Diego · doi:10.7270/q21g0s3m

BindingDB Entry 50023634: Next-generation cancer therapeutics: PROTACs and the role of heterocyclic warheads in targeting resistance.

BindingDB (2026) · UC San Diego · doi:10.7270/q2bc44fh

Targeted Protein Degradation in Lung Cancer: The Emerging Role of PROTAC Technology and E3 Ligases

Hussain, M. S., Babu, M. A., Afzal, M., Roopashree, R., Lal, M., Rekha, A., Oliver, B. G. G., MacLoughlin, R. J., Chakraborty, A., Dua, K., et al. (2025) · Current Medicinal Chemistry · doi:10.2174/0109298673382742250619055201 · Cited by 4 · see citing works

Proteolysis Targeting Chimera Agents (PROTACs): New Hope for Overcoming the Resistance Mechanisms in Oncogene-Addicted Non-Small Cell Lung Cancer

Cordani, N., Nova, D., Sala, L., Abbate, M. I., Colonese, F., Cortinovis, D. L., & Canova, S. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms252011214 · Cited by 17 · see citing works

Design of conditional and tumor-activated PROTACs for selective degradation in lung cancer

Lin, L., Zheng, F., Wei, H., Wu, X., Yan, H., & Ding, Y. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118432 · Cited by 4 · see citing works

Revolutionizing lung cancer treatment: Introducing PROTAC therapy as a novel paradigm in targeted therapeutics

Mahajan, A. A., Panzade, G., Bhuniya, T., Das, P., Bhattacharjee, B., Das, S., Chowdhury, A., Chakraborty, K., Guha, S., Samant, A., et al. (2024) · Current Problems in Cancer · doi:10.1016/j.currproblcancer.2024.101172 · Cited by 4 · see citing works

Targeted therapy based on ubiquitin-specific proteases, signalling pathways and E3 ligases in non-small-cell lung cancer

Yang, Y., Zhao, C.-J., Jin, Z.-F., Zheng, J., & Ma, L. (2023) · Frontiers in Oncology · doi:10.3389/fonc.2023.1120828 · Cited by 11 · see citing works