Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Cited by (965)

Items 401–500 of 965

1. Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review
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2. Characterizing the Cooperative Effect of PROTAC Systems with End-Point Binding Free Energy Calculation
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3. CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications
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4. Discovery of a bifunctional PKMYT1-targeting PROTAC empowered by AI-generation
   Yazhou Wang, Xiaomin Wang, Tingting Liu, Chao Wang, Qingshuo Meng, Fanye Meng, Jiaojiao Yu, Jinxin Liu, Yaya Fan, David G. Gennert et al. · 2025 · Nature Communications
5. Biochemical perspectives on targeting KMT2 methyltransferases in cancer
   Xiang Zhai, James E. Brownell · 2021 · Trends in Pharmacological Sciences
6. Discovery of novel VEGFR-2-PROTAC degraders based on the localization of lysine residues via recruiting VHL for the treatment of gastric cancer
   Xingrong Wang, Shuai Wang, Hong-Xia Mu, Kai-Yan Xu, Xueting Wang, Jian-Tao Shi, Qi-Hang Cui, Liwen Zhang, Shi‐Wu Chen · 2022 · European Journal of Medicinal Chemistry
7. The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents
   Shiwen Yu, Jinling Zheng, Yan Zhang, Dandan Meng, Yujue Wang, Xiaoyu Xu, Xiaoyu Xu, Shayibai Shabiti, Xu Zhang, Zixi Wang et al. · 2023 · Bioorganic & Medicinal Chemistry
8. Discovery of a selective TC-PTP degrader for cancer immunotherapy
   Jinmin Miao, Jiajun Dong, Yiming Miao, Yunpeng Bai, Zihan Qu, Brenson A. Jassim, Bo Huang, Quyen D. Nguyen, Yuan Ma, Allison A. Murray et al. · 2023 · Chemical Science
9. Targeted protein degradation in antibacterial drug discovery?
   Pooja Gopal, Thomas Dick · 2019 · Progress in Biophysics and Molecular Biology
10. Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors
    Rachael Arthur, Beatriz Valle‐Argos, Andrew J. Steele, Graham Packham · 2020 · Exploration of Targeted Anti-tumor Therapy
11. Proteome-scale induced proximity screens reveal highly potent protein degraders and stabilizers
    Juline Poirson, Akashdeep Dhillon, Hanna Cho, Mandy Hiu Yi Lam, Nader Alerasool, Jessica Lacoste, Lamisa Mizan, Mikko Taipale · 2022 · bioRxiv (Cold Spring Harbor Laboratory)
12. Advances in designing ternary complexes: Integrating in-silico and biochemical methods for PROTAC optimisation in target protein degradation
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13. PROTAC-induced protein structural dynamics in targeted protein degradation
    Kingsley Y Wu, Ta I Hung, Chia‐en A. Chang · 2024 · eLife
14. Design of PROTACs utilizing the E3 ligase GID4 for targeted protein degradation
    Yanran Li, Kaiwen Bao, Jiyue Sun, Ruixin Ge, Qiqing Zhang, Bing Zhang, Xiaojie Yan, Junlin Li, Fengying Shi, Meiling Zhang et al. · 2025 · Nature Structural & Molecular Biology
15. Scrutinizing the Therapeutic Potential of PROTACs in the Management of Alzheimer’s Disease
    Bhatia, Shiveena, Singh, Manjinder, Singh, Tanveer, Singh, Varinder · 2023 · Neurochemical Research
16. Elucidation of genome-wide understudied proteins targeted by PROTAC-induced degradation using interpretable machine learning
    Xie, Li, Xie, Lei · 2023 · PLOS Computational Biology
17. Advancing Design Strategy of PROTACs for Cancer Therapy
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18. Design, Synthesis, and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Dual Degradation of IGF-1R and Src
    Sudhakar Manda, Na Keum Lee, Dong‐Chan Oh, Jeeyeon Lee · 2020 · Molecules
19. General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex
    Wenwei Lin, Taosheng Chen · 2021 · ACS Pharmacology & Translational Science
20. The synthesis of PROTAC molecule and new target KAT6A identification of CDK9 inhibitor iCDK9
    Mingtao Ao, Jun Wu, Yin Cao, Yaohui He, Yuxiang Zhang, Xiang Gao, Yuhua Xue, Meijuan Fang, Zhen Wu · 2022 · Chinese Chemical Letters
21. Induced degradation of protein kinases by bifunctional small molecules: a next-generation strategy
    Jay Clemens Groppe · 2019 · Expert Opinion on Drug Discovery
22. A proteomic platform to identify off-target proteins associated with therapeutic modalities that induce protein degradation or gene silencing
    Liu, Xin, Zhang, Ye, Ward, Lucas D., Yan, Qinghong, Bohnuud, Tanggis, Hernandez, Rocio, Lao, Socheata, Yuan, Jing, Fan, Fan · 2021 · Scientific Reports
23. Optimization of Potent Ligands for the E3 Ligase DCAF15 and Evaluation of Their Use in Heterobifunctional Degraders
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24. Exploration of Hydrazide-Based HDAC8 PROTACs for the Treatment of Hematological Malignancies and Solid Tumors
    Chunlong Zhao, Jianqiu Zhang, Hangyu Zhou, Rita Setroikromo, Gerrit J. Poelarends, Frank J. Dekker · 2024 · Journal of Medicinal Chemistry
25. Dual-ligand PROTACS mediate superior target protein degradation in vitro and therapeutic efficacy in vivo
    Yong Chen, Zihan Xia, Ujjwal Suwal, Pekka Rappu, Jyrki Heino, Olivier De Wever, Bruno G. De Geest · 2024 · Chemical Science
26. Recruitment to the Proteasome Is Necessary but Not Sufficient for Chemically Induced, Ubiquitin-Independent Degradation of Native Proteins
    Madeline Balzarini, Joel Tong, Weijun Gui, Isuru M. Jayalath, Bin-Bin Schell, Thomas J. Kodadek · 2024 · ACS Chemical Biology
27. Identification of a non-inhibitory aptameric ligand to CRL2ZYG11B E3 ligase for targeted protein degradation
    Zhihao Yang, Miao Chen, Ruixin Ge, Ping Zhou, Wei Pan, Jiayi Song, Shuwen Ma, Song Chen, Chenyu Xu, Mengyu Zhou et al. · 2025 · Nature Communications
28. Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells
    Sarah D. Mahan, Kristin M. Riching, Marjeta Urh, Danette L. Daniels · 2021 · Methods in molecular biology
29. Light-Activating PROTACs in Cancer: Chemical Design, Challenges, and Applications
    Arvind Negi, Kavindra Kumar Kesari, Anne Sophie Voisin‐Chiret · 2022 · Applied Sciences
30. Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader
    Anand Divakaran, Cole R. Scholtz, Huda Zahid, Wenwei Lin, Elizabeth C. Griffith, Richard E. Lee Jr., Taosheng Chen, Daniel A. Harki, William C. K. Pomerantz · 2022 · ACS Medicinal Chemistry Letters
31. Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain
    Iván Cheng‐Sánchez, Katherine A. Gosselé, Leonardo Palaferri, Mariia S. Kirillova, Cristina Nevado · 2024 · ACS Medicinal Chemistry Letters
32. Development of a Potent Protein Degrader against Oncogenic BCR-ABL Protein
    Norihito Shibata, Nobumichi Ohoka, Takayuki Hattori, Mikihiko Naito · 2019 · Chemical and Pharmaceutical Bulletin
33. Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs)
    Daniela Tomaselli, Nicola Mautone, Antonello Mai, Dante Rotili · 2020 · European Journal of Medicinal Chemistry
34. A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes
    Pinch, Benika J., Buckley, Dennis L., Gleim, Scott, Brittain, Scott M., Tandeske, Laura, D'Alessandro, Pier Luca, Hauseman, Zachary J., Lipps, Jennifer, Xu, Lei, Harvey, Edward P. et al. · 2022 · Cell Chemical Biology
35. High‐Throughput Miniaturized Synthesis of PROTAC‐Like Molecules
    Ye Tian, Maximilian Seifermann, Liana Bauer, Charlotte Luchena, Janne J. Wiedmann, S. Schmidt, Alexander Geisel, Sergii Afonin, Julius Höpfner, Marius Brehm et al. · 2024 · Small
36. Senolytic Prodrugs: A Promising Approach to Enhancing Senescence‐Targeting Intervention
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37. ET-PROTACs: modeling ternary complex interactions using cross-modal learning and ternary attention for accurate PROTAC-induced degradation prediction
    Lijun Cai, Guanyu Yue, Yifan Chen, Li Wang, Xiaojun Yao, Quan Zou, Xiangzheng Fu, Dongsheng Cao · 2024 · Briefings in Bioinformatics
38. Frustration in the protein-protein interface plays a central role in the cooperativity of PROTAC ternary complexes
    Ning Ma, S. Bhattacharya, Sanychen Muk, Zuzana Jandová, Philipp S. Schmalhorst, Soumadwip Ghosh, Keith Le, Emelyne Diers, Nicole B. Trainor, William Farnaby et al. · 2025 · Nature Communications
39. Design, synthesis, and biological evaluation of small molecule PROTACs for potential anticancer effects
    Yang Da, Shaodong Liu, Pei Lin, Feng Wang, Renjie Yan, Yongzhi Shu, Jun Lin · 2019 · Medicinal Chemistry Research
40. The Vital Role of Proteomics in Characterizing Novel Protein Degraders
    Andrew X. Zhang, Katelyn B. Cassidy, Göran Dahl, Kévin Moreau, Fiona Pachl, Andrea M. Zuhl · 2021 · SLAS DISCOVERY
41. Systematic Exploration of Privileged Warheads for Covalent Kinase Drug Discovery
    Zheng Zhao, Philip E. Bourne · 2022 · Pharmaceuticals
42. Exploring PROTAC Cooperativity with Coarse-Grained Alchemical Methods
    Huanghao Mai, Matthew H. Zimmer, Thomas F. Miller · 2023 · The Journal of Physical Chemistry B
43. Application of PROTACs in target identification and validation
    Yang Liu, Jing Yu Liang, Rui Zhu, Yueying Yang, Yali Wang, Wenyi Wei, Hua Li, Lixia Chen · 2024 · Acta Materia Medica
44. Exploring the Ubiquitin-Proteasome System (UPS) through PROTAC Technology
    Carlotta Cecchini, Sébastien Tardy, Valentina Ceserani, Jean-Philippe Paul. Theurillat, Léonardo Scapozza · 2020 · CHIMIA International Journal for Chemistry
45. Design, Synthesis, and Biological Evaluation of HDAC Degraders with CRBN E3 Ligase Ligands
    Yingxin Lu, Danwen Sun, Donghuai Xiao, Ying-Ying Shao, Mingbo Su, Yubo Zhou, Jia Xuan Li, Shulei Zhu, Wei Ping Lu · 2021 · Molecules
46. Identification of PDE6D as a potential target of sorafenib via PROTAC technology
    Yang Li, Qingshi Meng, Ping Wang, Xiaolei Liu, Qiuyu Fu, Yuting Xie, Yu Zhou, Xiangbing Qi, Niu Huang · 2020 · bioRxiv (Cold Spring Harbor Laboratory)
47. ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression
    Yuanfei Deng, Cuifu Yu, Lushi Chen, Xin Zhang, Qiucheng Lei, Qing Liu, Gengxi Cai, Fang Liu · 2022 · Frontiers in Pharmacology
48. Azobenzene Photoswitches in Proteolysis Targeting Chimeras: Photochemical Control Strategies and Therapeutic Benefits
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49. Targeting micro-environmental pathways by PROTACs as a therapeutic strategy
    Jing Liu, Yunhua Peng, Hiroyuki Inuzuka, Wenyi Wei · 2022 · Seminars in Cancer Biology
50. Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery
    Wentao Tang, Congcong Lin, Quanwei Yu, Dan Zhang, Yun Liu, Lele Zhang, Zhilan Zhou, Jifa Zhang, Liang Ouyang · 2023 · Journal of Medicinal Chemistry
51. Recent advances in the molecular design and applications of proteolysis targeting chimera-based multi-specific antiviral modality
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52. Ternary Complex‐Templated Dynamic Combinatorial Chemistry for the Selection and Identification of Homo‐PROTACs
    Claudia J. Diehl, Alessandra Salerno, Alessio Ciulli · 2024 · Angewandte Chemie International Edition
53. Discovery of a Meisoindigo-Derived PROTAC as the ATM Degrader: Revolutionizing Colorectal Cancer Therapy via Synthetic Lethality with ATR Inhibitors
    Tingting Liu, Qing Wang, Yuxing Zhou, Baixin Ye, Tingting Liu, Linyang Yan, Jinbao Fan, Jiahao Xu, Yingjun Zhou, Zanxian Xia et al. · 2024 · Journal of Medicinal Chemistry
54. Advanced proteomics approaches to unravel protein homeostasis
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55. Development of Human Carbonic Anhydrase II Heterobifunctional Degraders
    Conor O’Herin, Yuta W. Moriuchi, Troy A. Bemis, Alysia J. Kohlbrand, Michael D. Burkart, Seth M. Cohen · 2023 · Journal of Medicinal Chemistry
56. Discovery of Monovalent Direct Degraders of BRD4 that Act via the Recruitment of DCAF11
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57. Allostery in Disease: Anticancer Drugs, Pockets, and the Tumor Heterogeneity Challenge
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58. Ternary Complex Modeling, Induced Fit Docking and Molecular Dynamics Simulations as a Successful Approach for the Design of VHL‐Mediated PROTACs Targeting the Kinase FLT3
    Husam Nassar, Anne‐Christin Sarnow, Ismail Celik, Mohamed Abdalla M. Abdelsalam, Dina Robaa, Wolfgang Sippl · 2025 · Archiv der Pharmazie
59. Harnessing the Deubiquitinase USP1 for Targeted Protein Stabilization
    Chao Qian, Zhen Wang, Yan Xiong, Dingpeng Zhang, Yue Zhong, Hiroyuki Inuzuka, Yihang Qi, Ling Xie, Xian Chen, Wenyi Wei et al. · 2025 · Journal of the American Chemical Society
60. Targeted protein degraders of SARS-CoV-2 Mpro are more active than enzymatic inhibition alone with activity against nirmatrelvir resistant virus
    Baolong Pan, Simon J. Mountford, Maki Kiso, Danielle E. Anderson, Georgina Papadakis, Kate E. Jarman, Danielle Tilmanis, Belinda M. Maher, Thomas Tran, Jake Shortt et al. · 2025 · Communications Medicine
61. Conformational Dynamics and Binding Kinetics Drive Mutant Selective Degradation of EGFR
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62. Revolutionizing viral disease treatment: PROTACs therapy could be the ultimate weapon of the future
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63. PROTAC targeting cyclophilin A controls virus-induced cytokine storm
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64. Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors
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65. Selective and potent PROTAC degraders of c-Src kinase
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66. Towards the Targeted Protein Degradation of PRMT1
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67. Chemical Proteomics–Guided Discovery of Covalent Ligands for Cancer Proteins
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68. Enhancer reprogramming underlies therapeutic utility of a SMARCA2 degrader in SMARCA4 mutant cancer
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69. Progress toward the development of the small molecule equivalent of small interfering RNA
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70. Cellular parameters shaping pathways of targeted protein degradation
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71. Therapeutic targeting of ubiquitin-specific protease 7 (USP7): Mechanistic insights, dysregulation, and advances in drug discovery
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72. Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells
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73. Sunitinib-based Proteolysis Targeting Chimeras (PROTACs) reduced the protein levels of FLT-3 and c-KIT in leukemia cell lines
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74. HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development
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75. Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity
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76. PIM1 targeted degradation prevents the emergence of chemoresistance in prostate cancer
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77. Development of Ligands and Degraders Targeting MAGE-A3
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78. Discovery and Functional Characterization of a Potent, Selective, and Metabolically Stable PROTAC of the Protein Kinases DYRK1A and DYRK1B
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79. Discovery of High-Affinity SMARCA2/4 Bromodomain Ligands and Development of Potent and Exceptionally Selective SMARCA2 PROTAC Degraders
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80. Photoactive Bifunctional Degraders: Precision Tools To Regulate Protein Stability
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81. Designed, synthesized and biological evaluation of proteolysis targeting chimeras (PROTACs) as AR degraders for prostate cancer treatment
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82. Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1
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83. A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination
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84. Unveiling the hidden interactome of CRBN molecular glues with chemoproteomics
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85. Chemoproteomics-Enabled De Novo Proteolysis Targeting Chimera Discovery Platform Identifies a Metallothionein Degrader to Probe Its Role in Cancer
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86. Expanding the druggable zinc-finger proteome defines properties of drug-induced degradation
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87. Load and lock: An emerging class of therapeutics that influence macromolecular dissociation
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88. New PROTAC Designs for Targeted Protein Degradation in 2021–2025: Novel E3 Ligases and Pre-PROTACs
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89. The Ubiquitination-Dependent and -Independent Functions of Cereblon in Cancer and Neurological Diseases
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90. Discovery of novel EGFR-PROTACs capable of degradation of multiple EGFR-mutated proteins
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91. A cell-based screening method using an intracellular antibody for discovering small molecules targeting the translocation protein LMO2
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92. Proteolysis Targeting Chimeras for BTK Efficiently Inhibit B-Cell Receptor Signaling and Can Overcome Ibrutinib Resistance in CLL Cells
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93. Bivalent target-binding bioPROTACs induce potent degradation of oncogenic SHP2
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94. Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-Loaded KRAS(On) Alleles
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95. A general approach to identify cell-permeable and synthetic anti-CRISPR small molecules
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96. Synthesis and Biological Activity of a VHL-Based PROTAC Specific for p38α
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97. Regulation of eDHFR-tagged proteins with trimethoprim PROTACs
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98. Perspectives of autophagy-tethering compounds (ATTECs) in drug discovery
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99. Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor
    Zuli Hu, Qiangsheng Zhang, Zulong Li, Hongling Yang, Xin Chen, Qi Zhang, Tianqiong Yang, Xiaojie He, Qiang Feng, Jun He et al. · 2024 · European Journal of Medicinal Chemistry
100. Proteolysis-targeting Chimeras for Targeting Protein for Degradation
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