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

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Phthalimide conjugation as a strategy for in vivo target protein degradation

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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

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

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Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

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Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia

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Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase

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

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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

Targeted protein degradation: mechanisms, strategies and application

Zhao, L., Zhao, J., Zhong, K., Tong, A., & Jia, D. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00966-4 · Cited by 1,035

PROTACs: past, present and future

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PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future

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PROTACs: great opportunities for academia and industry

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Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

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Challenges and Opportunities in Cancer Drug Resistance

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Current strategies for the design of PROTAC linkers: a critical review

Troup, R. I., Fallan, C., & Baud, M. G. J. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00018 · Cited by 424

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

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Light-Induced Protein Degradation with Photocaged PROTACs

Xue, G., Wang, K., Zhou, D., Zhong, H., & Pan, Z. (2019) · Journal of the American Chemical Society · doi:10.1021/jacs.9b06422 · Cited by 377

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Li, X., Pu, W., Zheng, Q., Ai, M., Chen, S., & Peng, Y. (2022) · Molecular Cancer · doi:10.1186/s12943-021-01434-3 · Cited by 389

Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes

Zhang, L., Riley-Gillis, B., Vijay, P., & Shen, Y. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-1129 · Cited by 365

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs

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An overview of PROTACs: a promising drug discovery paradigm

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Targeted protein degradation: advances in drug discovery and clinical practice

Zhong, G., Chang, X., Xie, W., & Zhou, X. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02004-x · Cited by 326

Target and tissue selectivity of PROTAC degraders

Guenette, R. G., Yang, S. W., Min, J., Pei, B., & Potts, P. R. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00200k · Cited by 324

Chemistries of bifunctional PROTAC degraders

Cao, C., He, M., Wang, L., He, Y., & Rao, Y. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00220e · Cited by 313

The PROTAC technology in drug development

Zou, Y., Ma, D., & Wang, Y. (2019) · Cell Biochemistry and Function · doi:10.1002/cbf.3369 · Cited by 312

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

Qi, S., Dong, J., Xu, Z., Cheng, X., Zhang, W., & Qin, J. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.692574 · Cited by 306

Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER)

Hu, J., Hu, B., Wang, M., Xu, F., Miao, B., Yang, C., Wang, M., Liu, Z., Hayes, D. F., Chinnaswamy, K., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01572 · Cited by 286

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00999-9 · Cited by 283

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

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

Zeng, S., Huang, W., Zheng, X., Cheng, L., Zhang, Z., Wang, J., & Shen, Z. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112981 · Cited by 264

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

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

Bricelj, A., Steinebach, C., Kuchta, R. D., Gütschow, M., & Sosič, I. (2021) · Frontiers in Chemistry · doi:10.3389/fchem.2021.707317 · Cited by 232

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

Han, X., Zhao, L., Xiang, W., Qin, C., Miao, B., Xu, T., Wang, M., Yang, C., Chinnaswamy, K., Stuckey, J. A., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01393 · Cited by 225

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

Guo, W., Qi, X., Yu, X., Liu, Y., Chung, C.-I., Bai, F., Lin, X., Lu, D., Wang, L., Chen, J., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-17997-6 · Cited by 228

Efficient targeted degradation via reversible and irreversible covalent PROTACs

Gabizon, R., Shraga, A., Gehrtz, P., Livnah, E., Gurwicz, N., Avram, L., Unger, T., Albeck, S., Shulman, Z., & London, N. (2020) · doi:10.26434/chemrxiv.11494398.v1 · Cited by 213

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

Su, S., Yang, Z., Gao, H., Yang, H., Zhu, S., An, Z., Wang, J., Li, Q., Chandarlapaty, S., Deng, H., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00871 · Cited by 210

Prey for the Proteasome: Targeted Protein Degradation—A Medicinal Chemist's Perspective

Luh, L. M., Scheib, U., Juenemann, K., Wortmann, L., Brands, M., & Cromm, P. M. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.202004310 · Cited by 201

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

Tinworth, C. P., Lithgow, H., Dittus, L., Bassi, Z. I., Hughes, S. E., Muelbaier, M., Dai, H., Smith, I. E. D., Kerr, W. J., Burley, G. A., et al. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.8b01094 · Cited by 195

Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown

Jin, Y., Lu, M., Wang, Y., Shan, W.-X., Wang, X.-Y., You, Q., & Jiang, Z. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b02058 · Cited by 189

PROTACs: A novel strategy for cancer therapy

Liu, J., Ma, J., Liu, Y., Xia, J., Li, Y., Wang, Z. P., & Wei, W. (2020) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2020.02.006 · Cited by 186

Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule

Zhao, Q., Lan, T., Su, S., & Rao, Y. (2018) · Chemical Communications · doi:10.1039/c8cc07813k · Cited by 187

Harnessing the Power of Proteolysis for Targeted Protein Inactivation

Verma, R., Mohl, D., & Deshaies, R. J. (2020) · Molecular Cell · doi:10.1016/j.molcel.2020.01.010 · Cited by 185

E3 ligase ligand chemistries: from building blocks to protein degraders

Sosič, I., Bricelj, A., & Steinebach, C. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00148a · Cited by 176

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

Bruton tyrosine kinase degradation as a therapeutic strategy for cancer

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Rationalizing PROTAC-Mediated Ternary Complex Formation Using Rosetta

Bai, N., Miller, S. A., Andrianov, G. V., Yates, M., Kirubakaran, P., & Karanicolas, J. (2021) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c01451 · Cited by 157

The role of reversible and irreversible covalent chemistry in targeted protein degradation

Kiely‐Collins, H., Winter, G. E., & Bernardes, G. J. L. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.03.005 · Cited by 160

DeepPROTACs is a deep learning-based targeted degradation predictor for PROTACs

Li, F., Hu, Q., Zhang, X., Sun, R., Liu, Z., Wu, S., Tian, S., Ma, X., Dai, Z., Yang, X., et al. (2022) · Nature Communications · doi:10.1038/s41467-022-34807-3 · Cited by 159

Developments of CRBN-based PROTACs as potential therapeutic agents

Wang, C., Zhang, Y., Wu, Y., & Xing, D. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113749 · Cited by 158

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

Sun, Y., Ding, N., Song, Y., Yang, Z., Liu, W., Zhu, J., & Rao, Y. (2019) · Leukemia · doi:10.1038/s41375-019-0440-x · Cited by 148

Characteristic roadmap of linker governs the rational design of PROTACs

Dong, Y., Ma, T., Xu, T., Feng, Z., Li, Y., Song, L., Yao, X., Ashby, C. R., & Hao, G.-F. (2024) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2024.04.007 · Cited by 146

Heterobifunctional Molecules Induce Dephosphorylation of Kinases–A Proof of Concept Study

Yamazoe, S., Tom, J., Fu, Y., Wu, W., Zeng, L., Sun, C., Liu, Q., Lin, J. M., Lin, K., Fairbrother, W. J., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01167 · Cited by 147

Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders

Steinebach, C., Ng, Y. L. D., Sosič, I., Lee, C.-S., Chen, S., Lindner, S., Vu, L. P., Bricelj, A., Haschemi, R., Monschke, M., et al. (2020) · Chemical Science · doi:10.1039/d0sc00167h · Cited by 148

Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

Zhao, Q., Ren, C., Liu, L., Chen, J., Shao, Y., Sun, N., Sun, R., Kong, Y., Ding, X., Zhang, X., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01264 · Cited by 134

Developing potent PROTACs tools for selective degradation of HDAC6 protein

An, Z., Lv, W., Su, S., Wu, W., & Rao, Y. (2019) · Protein & Cell · doi:10.1007/s13238-018-0602-z · Cited by 133

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 129

Dysregulated Signalling Pathways Driving Anticancer Drug Resistance

Antoun, N. B., & Chioni, A. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms241512222 · Cited by 141

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

He, Y., Khan, S., Huo, Z., Lv, D., Zhang, X., Liu, X., Yuan, Y., Hromas, R., Xu, M., Zheng, G., et al. (2020) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-00924-z · Cited by 126

Update on targeted cancer therapies, single or in combination, and their fine tuning for precision medicine

Bashraheel, S. S., Dömling, A. S. S., & Goda, S. K. (2020) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2020.110009 · Cited by 128

Bivalent Ligands for Protein Degradation in Drug Discovery

Scheepstra, M., Hekking, K. F. W., Hijfte, L. V., & Folmer, R. H. A. (2019) · Computational and Structural Biotechnology Journal · doi:10.1016/j.csbj.2019.01.006 · Cited by 125

Strategies for designing proteolysis targeting chimaeras (PROTACs)

He, S., Dong, G., Cheng, J., Wu, Y., & Sheng, C. (2022) · Medicinal Research Reviews · doi:10.1002/med.21877 · Cited by 120

A chemical approach for global protein knockdown from mice to non-human primates

Sun, X., Wang, J., Yao, X., Zheng, W., Mao, Y., Lan, T., Wang, L., Sun, Y., Zhang, X., Zhao, Q., et al. (2019) · Cell Discovery · doi:10.1038/s41421-018-0079-1 · Cited by 118

PROTAC’ing oncoproteins: targeted protein degradation for cancer therapy

Kelm, J. M., Pandey, D. S., Malin, E., Kansou, H. W., Arora, S., Kumar, R., & Gavande, N. S. (2023) · Molecular Cancer · doi:10.1186/s12943-022-01707-5 · Cited by 122

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

Schiemer, J., Horst, R., Meng, Y., Montgomery, J. I., Xu, Y., Feng, X., Borzilleri, K., Uccello, D. P., Leverett, C., Brown, S., et al. (2021) · Nature Chemical Biology · doi:10.1038/s41589-020-00686-2 · Cited by 113

Protein degradation through covalent inhibitor-based PROTACs

Xue, G., Chen, J., Liu, L., Zhou, D., Zuo, Y., Fu, T., & Pan, Z. (2020) · Chemical Communications · doi:10.1039/c9cc08238g · Cited by 109

Plasticity in designing PROTACs for selective and potent degradation of HDAC6

Yang, H., Lv, W., He, M., Deng, H., Li, H., Wu, W., & Rao, Y. (2019) · Chemical Communications · doi:10.1039/c9cc08509b · Cited by 108

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 107

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

Tu, Y., Sun, Y., Qiao, S., Luo, Y., Liu, P., Jiang, Z., Hu, Y., Wang, Z., Huang, P., & Wen, S. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00460 · Cited by 103

Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance

Lin, X., Xiang, H., & Luo, G. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112689 · Cited by 104

Ibrutinib Resistance Mechanisms and Treatment Strategies for B-Cell Lymphomas

George, B., Chowdhury, S. M., Hart, A., Sircar, A., Singh, S. K., Nath, U. K., Mamgain, M., Singhal, N. K., Sehgal, L., & Jain, N. K. (2020) · Cancers · doi:10.3390/cancers12051328 · Cited by 97

NAMPT-targeting PROTAC promotes antitumor immunity via suppressing myeloid-derived suppressor cell expansion

Wu, Y., Pu, C., Fu, Y., Dong, G., Huang, M., & Sheng, C. (2021) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2021.12.017 · Cited by 97

Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality

Kostić, M., & Jones, L. H. (2020) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2020.02.006 · Cited by 100

Exploring the target scope of KEAP1 E3 ligase-based PROTACs

Du, G., Jiang, J., Henning, N. J., Safaee, N., Koide, E., Nowak, R. P., Donovan, K. A., Yoon, H., You, I., Yue, H., et al. (2022) · Cell chemical biology · doi:10.1016/j.chembiol.2022.08.003 · Cited by 97

Protein degradation technology: a strategic paradigm shift in drug discovery

Li, H., Dong, J., Cai, M., Xu, Z., Cheng, X., & Qin, J. (2021) · Journal of Hematology & Oncology · doi:10.1186/s13045-021-01146-7 · Cited by 96

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 95

An overview of kinase downregulators and recent advances in discovery approaches

Wang, B., Wu, H., Hu, C., Wang, H., Liu, J., Wang, W., & Liu, Q. (2021) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-021-00826-7 · Cited by 93

Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs

Gao, H., Wu, Y., Sun, Y., Yang, Y., Zhou, G., & Rao, Y. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00372 · Cited by 87

Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently

Yang, Z., Sun, Y., Ni, Z., Yang, C., Tong, Y., Liu, Y., Li, H., & Rao, Y. (2021) · Cell Research · doi:10.1038/s41422-021-00533-6 · Cited by 90

Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy

Pang, X., Liu, X., Liu, Y., Liu, W., Li, Y.-R., Yu, G.-X., Tian, X., Zhang, Y., Song, J., Jin, C., et al. (2021) · Molecules · doi:10.3390/molecules26144250 · Cited by 85

PROTACs as Potential Therapeutic Agents for Cancer Drug Resistance

Sun, X., & Rao, Y. (2019) · Biochemistry · doi:10.1021/acs.biochem.9b00848 · Cited by 88

PROTAC: A promising technology for cancer treatment

Zhou, X., Dong, R., Zhang, J., Zheng, X. X., & Sun, L. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112539 · Cited by 85

Site-Specific Labeling of Endogenous Proteins Using CoLDR Chemistry

Reddi, R. N., Rogel, A., Resnick, E., Gabizon, R., Prasad, P. K., Gurwicz, N., Barr, H. M., Shulman, Z., & London, N. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.1c06167 · Cited by 84

Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

Luo, G., Li, Z., Lin, X., Li, X., Chen, Y., Xi, K., Xiao, M., Wei, H., Zhu, L., & Xiang, H. (2020) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2020.11.001 · Cited by 84

The rise and rise of protein degradation: Opportunities and challenges ahead

Hughes, S. J., Testa, A., Thompson, N., & Churcher, I. (2021) · Drug Discovery Today · doi:10.1016/j.drudis.2021.08.006 · Cited by 81

Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction

Qiu, X., Sun, N., Kong, Y., Li, Y., Yang, X., & Jiang, B. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b01326 · Cited by 80

Genetic and Non-Genetic Mechanisms of Resistance to BCR Signaling Inhibitors in B Cell Malignancies

Ondrišová, L., & Mráz, M. (2020) · Frontiers in Oncology · doi:10.3389/fonc.2020.591577 · Cited by 77

Advancing targeted protein degradation for metabolic diseases therapy

Zhou, Q., Xiao, H., Yang, F., Wang, Y., Li, P., & Zheng, Z. (2022) · Pharmacological Research · doi:10.1016/j.phrs.2022.106627 · Cited by 77

Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib

Ran, F., Liu, Y., Wang, C., Xu, Z., Zhang, Y., Liu, Y., Zhao, G., & Ling, Y. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.114009 · Cited by 76

A novel cereblon modulator for targeted protein degradation

Kim, S. A., Go, A., Jo, S.-H., Park, S. J., Jeon, Y. U., Kim, J. E., Lee, H. K., Park, C. H., Lee, C.-O., Park, S. G., et al. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.01.023 · Cited by 72

A cell-permeable peptide-based PROTAC against the oncoprotein CREPT proficiently inhibits pancreatic cancer

Ma, D., Zou, Y., Chu, Y., Liu, Z., Liu, G., Chu, J., Li, M., Wang, J., Sun, S., & Chang, Z. (2020) · Theranostics · doi:10.7150/thno.41677 · Cited by 71

Novel approaches for the rational design of PROTAC linkers

Zagidullin, A. A., Milyukov, V. A., Rizvanov, A. A., & Bulatov, E. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00023 · Cited by 75

Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong in vivo Antitumor Activity

Yang, L., Tu, W., Huang, L., Miao, B., Kaneshige, A., Jiang, W., Leng, L., Wang, M., Wen, B., Sun, D., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00953 · Cited by 67

The Role of Bruton’s Kinase Inhibitors in Chronic Lymphocytic Leukemia: Current Status and Future Directions

Robak, T., Witkowska, M., & Smolewski, P. (2022) · Cancers · doi:10.3390/cancers14030771 · Cited by 68

Degradation of neurodegenerative disease-associated TDP-43 aggregates and oligomers via a proteolysis-targeting chimera

Tseng, Y.-L., Lu, P.-C., Lee, C.-C., He, R., Huang, Y., Tseng, Y., Cheng, T.-J. R., Huang, J. J., & Fang, J. (2023) · Journal of Biomedical Science · doi:10.1186/s12929-023-00921-7 · Cited by 73

Discovery of Novel PDEδ Degraders for the Treatment of KRAS Mutant Colorectal Cancer

Cheng, J., Li, Y., Wang, X., Dong, G., & Sheng, C. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00929 · Cited by 69

Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations

Lu, X., Smaill, J. B., & Ding, K. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00507 · Cited by 67

Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

Farnaby, W., Koegl, M., McConnell, D. B., & Ciulli, A. (2021) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2021.02.009 · Cited by 66

Targeted protein degradation in cancers: Orthodox PROTACs and beyond

Li, J., Chen, X., Lü, A., & Liang, C. (2023) · The Innovation · doi:10.1016/j.xinn.2023.100413 · Cited by 68

A MedChem toolbox for cereblon-directed PROTACs

Steinebach, C., Sosič, I., Lindner, S., Bricelj, A., Kohl, F., Ng, Y. L. D., Monschke, M., Wagner, K. G., Krönke, J., & Gütschow, M. (2019) · MedChemComm · doi:10.1039/c9md00185a · Cited by 66

Selective Degradation of PD‐L1 in Cancer Cells by Enzyme‐Instructed Self‐Assembly

Wang, Y., Li, X., Zheng, D., Chen, Y., Zhang, Z., & Yang, Z. (2021) · Advanced Functional Materials · doi:10.1002/adfm.202102505 · Cited by 65

Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery

Pei, H., Peng, Y., Zhao, Q., & Chen, Y. (2019) · RSC Advances · doi:10.1039/c9ra03423d · Cited by 70

Discovery and biological evaluation of proteolysis targeting chimeras (PROTACs) as an EGFR degraders based on osimertinib and lenalidomide

He, K., Zhang, Z., Wang, W., Zheng, X., Wang, X., & Zhang, X. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127167 · Cited by 65

Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton’s Tyrosine Kinase for the Treatment of Lymphoma

Zhang, J., Che, J., Luo, X., Wu, M., Kan, W., Jin, Y., Wang, H., Pang, A., Li, C., Huang, W., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00324 · Cited by 63

BTK inhibitors: past, present, and future

Cool, A., Nong, T., Montoya, S., & Taylor, J. (2024) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2024.06.006 · Cited by 63

Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease

Qu, L., Li, S., Ji, L., Luo, S., Ding, M., Yin, F., Wang, C., Luo, H., Lu, D., Liu, X., et al. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113889 · Cited by 61

Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation

He, M., Lv, W., & Rao, Y. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.685106 · Cited by 63

Update on the Development of MNK Inhibitors as Therapeutic Agents

Xu, W., Kannan, S., Verma, C. S., & Nacro, K. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00368 · Cited by 63

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

Liu, J., Liang, Q., Wang, A., Zou, F., Qi, Z., Yu, K., Liu, Q., Chen, C., Liu, J. L., & Liu, Q. (2020) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-020-00309-1 · Cited by 3

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

Alinari, L., Quinion, C. D., & Blum, K. (2015) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.65 · Cited by 28

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

Sun, Y., Ding, N., Song, Y., Yang, Z., Liu, W., Zhu, J., & Rao, Y. (2019) · Leukemia · doi:10.1038/s41375-019-0440-x · Cited by 148

Pirtobrutinib shows evidence to inaugurate a third generation of BTK inhibitors

Michot, J., & Ribrag, V. (2021) · The Lancet · doi:10.1016/s0140-6736(21)00235-x · Cited by 18