PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies

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

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

Lymphoma incidence patterns by WHO subtype in the United States, 1992-2001

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Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

Davis, R. E., Ngo, V. N., Lenz, G., Tolar, P., Young, R. M., Romesser, P. B., Kohlhammer, H., Lamy, L., Zhao, H., Yang, Y., et al. (2010) · Nature · doi:10.1038/nature08638 · Cited by 1,651

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

Honigberg, L. A., Smith, A. M., Sirisawad, M., Verner, E., Loury, D., Chang, B., Li, S., Pan, Z., Thamm, D. H., Miller, R. A., et al. (2010) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1004594107 · Cited by 1,561

Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

Woyach, J. A., Furman, R. R., Liu, T.-M., Ozer, H. G., Zapatka, M., Ruppert, A. S., Xue, L., Li, D. H.-H., Steggerda, S. M., Versele, M., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1400029 · Cited by 1,275

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 & Biology · doi:10.1016/j.chembiol.2015.05.009 · Cited by 1,140

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

Byrd, J. C., Harrington, B. K., O'Brien, S. M., Jones, J. A., Schuh, A., Devereux, S., Chaves, J. M., Wierda, W. G., Awan, F. T., Brown, J. R., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1509981 · Cited by 916

Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase

Pan, Z., Scheerens, H., Li, S., Schultz, B. E., Sprengeler, P. A., Burrill, L. C., Mendonca, R. V., Sweeney, M. D., Scott, K. C. K., Grothaus, P. G., et al. (2006) · ChemMedChem · doi:10.1002/cmdc.200600221 · Cited by 690

Bruton’s tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

Mohamed, A. J., Yu, L., Bäckesjö, C., Vargas, L., Faryal, R., Aints, A., Christensson, B., Berglöf, A., Vihinen, M., Nore, B. F., et al. (2009) · Immunological Reviews · doi:10.1111/j.1600-065x.2008.00741.x · Cited by 516

E3 ligase ligand optimization of Clinical PROTACs

Jiang, H., Xiong, H., Gu, S.-X., & Wang, M. (2023) · Frontiers in Chemistry · doi:10.3389/fchem.2023.1098331 · Cited by 64

Journey of PROTAC: From Bench to Clinical Trial and Beyond

Berkley, K., Zalejski, J., Sharma, N., & Sharma, A. K. (2025) · Biochemistry · doi:10.1021/acs.biochem.4c00577 · Cited by 62

Development of a PROTAC-Based Targeting Strategy Provides a Mechanistically Unique Mode of Anti-Cytomegalovirus Activity

Hahn, F., Hamilton, S. T., Wangen, C., Wild, M. R., Kicuntod, J., Brückner, N., Follett, J. E. L., Herrmann, L., Kheimar, A., Kaufer, B. B., et al. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms222312858 · Cited by 64

Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders

Chen, L., Chen, Y., Zhang, C., Jiao, B., Liang, S., Qiong, T., Chai, H., Yu, W., Qian, Y., Yang, H., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01342 · Cited by 55

Targeting Protein Kinases Degradation by PROTACs

Yu, F., Cai, M., Shao, L., & Zhang, J. (2021) · Frontiers in Chemistry · doi:10.3389/fchem.2021.679120 · Cited by 55

Recent Advances in PROTAC-Based Antiviral Strategies

Ahmad, H., Zia, B., Husain, H., & Husain, A. (2023) · Vaccines · doi:10.3390/vaccines11020270 · Cited by 57

Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

Krajčovičová, S., Jorda, R., Hendrychová, D., Kryštof, V., & Soural, M. (2018) · Chemical Communications · doi:10.1039/c8cc08716d · Cited by 53

Targeting Tubulin-colchicine Site for Cancer Therapy: Inhibitors, Antibody- Drug Conjugates and Degradation Agents

Duan, Y., Liu, W., Tian, L., Mao, Y., & Song, C. (2019) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026619666190618130008 · Cited by 54

Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases

Luo, X., Archibeque, I., Dellamaggiore, K., Smither, K., Homann, O. R., Lipford, J. R., & Mohl, D. A. (2022) · iScience · doi:10.1016/j.isci.2022.103985 · Cited by 55

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Zhong, Y., Chi, F., Wu, H., Liu, Y., Xie, Z., Huang, W., Shi, W., & Qian, H. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114142 · Cited by 52

Medicinal Chemistry Strategies for the Development of Bruton’s Tyrosine Kinase Inhibitors against Resistance

Sun, S., Wu, S.-H., Kang, J.-B., Ma, Y.-Y., Chen, L., Cao, P., Chang, L., Ding, N., Xue, X., Li, N., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00030 · Cited by 54

MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment

Vicente, A. T. S., & Salvador, J. A. R. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms231911068 · Cited by 56

Proteomic characterization of post-translational modifications in drug discovery

Zhai, L., Chen, K., Hao, B., & Tan, M. (2022) · Acta Pharmacologica Sinica · doi:10.1038/s41401-022-01017-y · Cited by 53

Next Generation BTK Inhibitors in CLL: Evolving Challenges and New Opportunities

Frustaci, A. M., Deodato, M., Zamprogna, G., Cairoli, R., Montillo, M., & Tedeschi, A. (2023) · Cancers · doi:10.3390/cancers15051504 · Cited by 50

Triazol: A Privileged Scaffold for Proteolysis Targeting Chimeras

Xia, L., Ba, M.-Y., Liu, W., Cheng, W., Hu, C.-P., Zhao, Q., Yao, Y., Sun, M., & Duan, Y. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0159 · Cited by 51

Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs

Chen, Y., Ning, Y., Bai, G., Tong, L., Zhang, T., Zhou, J., Zhang, H., Xie, H., Ding, J., & Duan, W. (2021) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00474 · Cited by 49

Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents

Wang, C., Zhang, Y., Shi, L., Yang, S., Chang, J., Zhong, Y., Li, Q., & Xing, D. (2022) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2022.2074414 · Cited by 50

The Role of the Ubiquitin Proteasome System in Glioma: Analysis Emphasizing the Main Molecular Players and Therapeutic Strategies Identified in Glioblastoma Multiforme

Maksoud, S. (2021) · Molecular Neurobiology · doi:10.1007/s12035-021-02339-4 · Cited by 48

Progress in the development of small molecular inhibitors of the Bruton’s tyrosine kinase (BTK) as a promising cancer therapy

Liu, X., Xu-Liu, Pang, X., Yuan, X. Y., Yu, G.-X., Li, Y.-R., Guan, Y.-F., Zhang, Y., Song, J., Zhang, Q., et al. (2021) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116358 · Cited by 46

Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective

Pei, H., Guo, W., Peng, Y., Xiong, H., & Chen, Y. (2022) · Medicinal Research Reviews · doi:10.1002/med.21886 · Cited by 45

Aberrant Activation of NF-κB Signalling in Aggressive Lymphoid Malignancies

Kennedy, R., & Klein, U. (2018) · Cells · doi:10.3390/cells7110189 · Cited by 46

Pharmacological Modulation of the Crosstalk between Aberrant Janus Kinase Signaling and Epigenetic Modifiers of the Histone Deacetylase Family to Treat Cancer

Mustafa, A. M., & Krämer, O. H. (2022) · Pharmacological Reviews · doi:10.1124/pharmrev.122.000612 · Cited by 42

Journey of Von Hippel-Lindau (VHL) E3 ligase in PROTACs design: From VHL ligands to VHL-based degraders

Setia, N., Almuqdadi, H. T. A., & Abid, M. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.116041 · Cited by 42

The resistance mechanisms and treatment strategies of BTK inhibitors in B-cell lymphoma

Wang, H., Zhang, W., Yang, J., & Zhou, K. (2021) · Hematological Oncology · doi:10.1002/hon.2933 · Cited by 41

Recent advances in targeted protein degraders as potential therapeutic agents

Yang, N., Kong, B., Zhu, Z., Huang, F., Zhang, L., Lu, T., Chen, Y., Zhang, Y., & Jiang, Y. (2023) · Molecular Diversity · doi:10.1007/s11030-023-10606-w · Cited by 44

If small molecules immunotherapy comes, can the prime be far behind?

Zhang, J., Zhang, Y., Qu, B., Yang, H., Hu, S., & Dong, X. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113356 · Cited by 40

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

Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy

Chen, S., Chen, Z., Lu, L., Zhao, Y., Zhou, R., Xie, Q., Shu, Y., Lin, J., Yu, X., & Wang, Y. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115403 · Cited by 39

Advancements in delivery Systems for Proteolysis-Targeting Chimeras (PROTACs): Overcoming challenges and expanding biomedical applications

Yu, Y., Hu, W., Xu, Y., Xu, H.-B., & Gao, J.-Q. (2025) · Journal of Controlled Release · doi:10.1016/j.jconrel.2025.113719 · Cited by 44

Targeting SHP2 as a therapeutic strategy for inflammatory diseases

Liu, Y., Yang, X., Wang, Y., Yang, Y., Sun, D., Li, H., & Chen, L. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113264 · Cited by 40

PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs

Maneiro, M., Vita, E. D., Conole, D., Kounde, C. S., Zhang, Q., & Tate, E. W. (2021) · Progress in medicinal chemistry · doi:10.1016/bs.pmch.2021.01.002 · Cited by 38

Design and linkage optimization of ursane-thalidomide-based PROTACs and identification of their targeted-degradation properties to MDM2 protein

Qi, Z., Yang, G., Deng, T., Wang, J., Zhou, H., Popov, S. A., Shults, E. E., & Wang, C. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.104901 · Cited by 39

Discovery of potent and selective HER2 PROTAC degrader based Tucatinib with improved efficacy against HER2 positive cancers

Hu, M., Li, Y., Li, J., Zhou, H., Liu, C., Liu, Z., Gong, Y., Ying, B., & Xie, Y. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114775 · Cited by 40

ByeTAC: Bypassing E-Ligase-Targeting Chimeras for Direct Proteasome Degradation

Loy, C. A., Ali, E. M. H., Seabrook, L. J., Harris, T. J., Kragness, K. A., Albrecht, L. V., & Trader, D. J. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c00485 · Cited by 42

Light-Controllable PROTACs for Temporospatial Control of Protein Degradation

Liu, J., Peng, Y., & Wei, W. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.678077 · Cited by 38

Novel Design Strategies to Enhance the Efficiency of Proteolysis Targeting Chimeras

Zhao, C., & Dekker, F. J. (2022) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.2c00089 · Cited by 38

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

A Buchwald–Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3‐Ligase PROTACs**

Hayhow, T. G., Borrows, R. E. A., Diène, C. R., Fairley, G., Fallan, C., Fillery, S. M., Scott, J. S., & Watson, D. W. (2020) · Chemistry - A European Journal · doi:10.1002/chem.202003137 · Cited by 36

PROTAC: targeted drug strategy. Principles and limitations

Koroleva, O. A., Dutikova, Y. V., Trubnikov, A. V., Zenov, F. A., Manasova, E. V., Shtil, A. A., & Kurkin, A. V. (2022) · Russian Chemical Bulletin · doi:10.1007/s11172-022-3659-z · Cited by 38

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 34

Targeted Protein Degradation: Clinical Advances in the Field of Oncology

Salama, A. K. A. A., Trkulja, M. V., Casanova, E., & Uras, I. Z. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms232315440 · Cited by 36

BTK Is the Target That Keeps on Giving: A Review of BTK-Degrader Drug Development, Clinical Data, and Future Directions in CLL

Salvaris, R., Brennan, J., & Lewis, K. L. (2025) · Cancers · doi:10.3390/cancers17030557 · Cited by 39

Small-molecule PROTACs: Novel Agents for Cancer Therapy

Wan, Y., Yan, C., Gao, H. J., & Liu, T. (2020) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0340 · Cited by 32

Construction of an IMiD-based azide library as a kit for PROTAC research

Liu, H., Sun, R., Ren, C., Qiu, X., Yang, X., & Jiang, B. (2020) · Organic & Biomolecular Chemistry · doi:10.1039/d0ob02120b · Cited by 30

Progress of small molecules for targeted protein degradation: PROTACs and other technologies

Zhao, H., Xin, M., & Zhang, S. (2023) · Drug Development Research · doi:10.1002/ddr.22026 · Cited by 31

A comprehensive review of emerging approaches in machine learning for de novo PROTAC design

Gharbi, Y., & Mercado, R. (2024) · Digital Discovery · doi:10.1039/d4dd00177j · Cited by 32

Unleashing the Power of Covalent Drugs for Protein Degradation

Fu, M., Jin, H., Wang, S., Shen, L., Liu, H., Liu, Y., Zheng, Y., & Dai, X. (2025) · Medicinal Research Reviews · doi:10.1002/med.22101 · Cited by 31

Discovery of CN0 as a novel proteolysis-targeting chimera (PROTAC) degrader of PARP1 that can activate the cGAS/STING immunity pathway combined with daunorubicin

Lin, S., Tu, G., Yu, Z., Jiang, Q., Zhang, L., Liu, J., Liu, Q., Huang, X., Xu, J., Lin, Y., et al. (2022) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2022.116912 · Cited by 29

Enzyme‐Activated Orthogonal Proteolysis Chimeras for Tumor Microenvironment‐Responsive Immunomodulation

Sun, C., Liu, S., Lau, J. W., Yang, H., Chen, Y., & Xing, B. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202423057 · Cited by 31

Targeted Protein Degradation: The New Frontier of Antimicrobial Discovery?

Powell, M., Blaskovich, M. A. T., & Hansford, K. A. (2021) · ACS Infectious Diseases · doi:10.1021/acsinfecdis.1c00203 · Cited by 29

PROTAC delivery in tumor immunotherapy: Where are we and where are we going?

Li, Y., Wu, Y., Gao, S., Sun, T., & Jiang, C. (2024) · Journal of Controlled Release · doi:10.1016/j.jconrel.2024.11.076 · Cited by 29

PROTACs in gastrointestinal cancers

Chen, Y., Yang, Q., Xu, J., Tang, L., Zhang, Y., Du, F., Zhao, Y., Wu, X., Li, M., Shen, J., et al. (2022) · Molecular Therapy — Oncolytics · doi:10.1016/j.omto.2022.10.012 · Cited by 28

Bromodomain and BET family proteins as epigenetic targets in cancer therapy: their degradation, present drugs, and possible PROTACs

Muddassir, M., Soni, K. V., Sangani, C. B., AlArifi, A. S., Afzal, M. F., Abduh, N. A. Y., Duan, Y., & Bhadja, P. (2020) · RSC Advances · doi:10.1039/d0ra07971e · Cited by 27

PROTAC for Bruton’s tyrosine kinase degradation alleviates inflammation in autoimmune diseases

Zhu, C., Yang, Z., Zhang, Y., Li, Z., Li, G., Yang, B., Kang, N., Wang, J., Sun, Y., Ding, N., et al. (2024) · Cell Discovery · doi:10.1038/s41421-024-00711-x · Cited by 27

NF-κB Mutations in Germinal Center B-Cell Lymphomas: Relation to NF-κB Function in Normal B Cells

Pasqualucci, L., & Klein, U. (2022) · Biomedicines · doi:10.3390/biomedicines10102450 · Cited by 26

Recent advances in dual PROTACs degrader strategies for disease treatment

Liu, J., Liu, Y., Tang, J., Gong, Q., Yan, G., Fan, H., Zhang, X., & Pu, C. (2024) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2024.116901 · Cited by 25

BTK kinase activity is dispensable for the survival of diffuse large B-cell lymphoma

Yuan, H., Zhu, Y., Cheng, Y., Hou, J., Jin, F., Li, M., Jia, W. Q., Cheng, Z., Xing, H., Liu, M., et al. (2022) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2022.102555 · Cited by 24

Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors

Arthur, R., Valle‐Argos, B., Steele, A. J., & Packham, G. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00009 · Cited by 24

Navigating PROTACs in Cancer Therapy: Advancements, Challenges, and Future Horizons

Ibrahim, S., Khan, M. U., Khurram, I., Rehman, R., Rauf, A., Ahmad, Z., Aljohani, A. S. M., Abdulmonem, W. A., & Quradha, M. M. (2025) · Food Science & Nutrition · doi:10.1002/fsn3.70011 · Cited by 27

Proteolysis targeting chimera technology: a novel strategy for treating diseases of the central nervous system

Ma, K., Han, X.-X., Han, X., & Zhou, S. (2021) · Neural Regeneration Research · doi:10.4103/1673-5374.308075 · Cited by 24

The Role of BTK Inhibition in the Treatment of Chronic Lymphocytic Leukemia: A Clinical View

Tambaro, F. P., Novellis, D. D., & Wierda, W. G. (2021) · Journal of Experimental Pharmacology · doi:10.2147/jep.s265284 · Cited by 23

Next-generation Bruton’s Tyrosine Kinase (BTK) Inhibitors Potentially Targeting BTK C481S Mutation- Recent Developments and Perspectives

Das, D., Wang, J., & Hong, J. (2022) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026622666220801101706 · Cited by 23

Discovery of Ibrutinib-based BTK PROTACs with in vivo anti-inflammatory efficacy by inhibiting NF-κB activation

Huang, J., Ma, Z., Yang, Z., He, Z., Bao, J., Peng, X., Liu, Y., Chen, T., Cai, S., Chen, J., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115664 · Cited by 24

Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs

Fu, D., Yuan, Y., Qin, F., Xu, Y., Cui, X., Li, G., Yao, S., Deng, Y., & Tang, Z. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113850 · Cited by 22

A non‐covalent inhibitor XMU‐MP‐3 overrides ibrutinib‐resistant BtkC481S mutation in B‐cell malignancies

Gui, F., Jiang, J., He, Z., Li, L., Li, Y., Deng, Z., Lu, Y., Wu, X., Chen, G., Su, J., et al. (2019) · British Journal of Pharmacology · doi:10.1111/bph.14809 · Cited by 20

Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges

Wang, C., Zhang, Y., Zhang, T., Shi, L., Geng, Z., & Xing, D. (2022) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2022.2076675 · Cited by 22

Targeting Protein Degradation Pathways in Tumors: Focusing on their Role in Hematological Malignancies

Wolska, A., & Smolewski, P. (2022) · Cancers · doi:10.3390/cancers14153778 · Cited by 21

Targeted Protein Degradation: An Emerging Therapeutic Strategy in Cancer

Barghout, S. H. (2020) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520620666200410082652 · Cited by 21

Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)

Tomaselli, D., Mautone, N., Mai, A., & Rotili, D. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112750 · Cited by 21

BRD4-specific PROTAC inhibits basal-like breast cancer partially through downregulating KLF5 expression

Kong, Y., Lan, T., Wang, L., Chen, G., Lv, W., Zhang, H., Zhou, C., Sun, X., Liu, W., Haihui, H., et al. (2024) · Oncogene · doi:10.1038/s41388-024-03121-1 · Cited by 25

Design, synthesis, and biological evaluation of small molecule PROTACs for potential anticancer effects

Da, Y., Liu, S., Lin, P., Wang, F., Yan, R., Shu, Y., & Lin, J. (2019) · Medicinal Chemistry Research · doi:10.1007/s00044-019-02485-4 · Cited by 20

Exploiting the ubiquitin system in myeloid malignancies. From basic research to drug discovery in MDS and AML

Drulă, R., Iluta, S., Gulei, D., Iuga, C. A., Dima, D. M., Ghiaur, G., Buzoianu, A. D., Ciechanover, A. J., & Tomuleasa, C. (2022) · Blood Reviews · doi:10.1016/j.blre.2022.100971 · Cited by 20

FAK Inhibitors As Promising Anticancer Targets: Present and Future Directions

Mustafa, M., El‐Hafeez, A. A. A., Abdelhafeez, D. A., Abdelhamid, D. S., Mostafa, Y. A., Ghosh, P., Hayallah, A. M., & Abuo‐Rahma, G. E. A. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0015 · Cited by 17

Targeting micro-environmental pathways by PROTACs as a therapeutic strategy

Liu, J., Peng, Y., Inuzuka, H., & Wei, W. (2022) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2022.07.001 · Cited by 20

Recent advances in the molecular design and applications of proteolysis targeting chimera-based multi-specific antiviral modality

Zhou, Y., Xu, S., López‐Carrobles, N., Ding, D., Liu, X., Menéndez‐Arias, L., & Zhan, P. (2023) · Acta Materia Medica · doi:10.15212/amm-2023-0019 · Cited by 20

BTK inhibitors resistance in B cell malignancies: Mechanisms and potential therapeutic strategies

Liu, X., Lin, Y., Zhuang, Q., Deng, H., Liu, A., & Sun, J. (2025) · Blood Reviews · doi:10.1016/j.blre.2025.101273 · Cited by 19

Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases

Huang, J., Ma, Z., Peng, X., Yang, Z., Wu, Y., Zhong, G., Ouyang, T., Chen, Z., Liu, Y., Wang, Q., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01414 · Cited by 18

Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity

Koide, E., Mohardt, M. L., Doctor, Z. M., Yang, A., Hao, M., Donovan, K. A., Kuismi, C. C., Nelson, A. J., Abell, K., Aguiar, M., et al. (2023) · ChemBioChem · doi:10.1002/cbic.202300141 · Cited by 18

Progress in RAS‐targeted therapeutic strategies: From small molecule inhibitors to proteolysis targeting chimeras

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Chimera induced protein degradation: PROTACs and beyond

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Heat stress targets and degrades BCR::ABL1 oncoproteins to overcome drug-resistance in Philadelphia chromosome-positive acute lymphoblastic leukemia

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A Comprehensive Review of Small-Molecule Inhibitors Targeting Bruton Tyrosine Kinase: Synthetic Approaches and Clinical Applications

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A comprehensive primer and review of PROTACs and their In Silico design

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Discovery of a highly potent and selective Bruton’s tyrosine kinase inhibitor avoiding impairment of ADCC effects for B-cell non-Hodgkin lymphoma

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PROTAC Targeting BTK for the Treatment of Ibrutinib-resistant B-cell Malignancies

Sun, Y., & Rao, Y. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160691-00147

Bruton's tyrosine kinase inhibitors in B‐cell non‐Hodgkin's lymphomas

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Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas

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