Chemistries of bifunctional PROTAC degraders

Cao, Chaoguo, He, Ming, Wang, Liguo, He, Yuna, Rao, Yu·2022·Chemical Society Reviews

Cited by (315)

Items 201–300 of 315

  1. Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation
    Wentao Zhu, Wenqian Zhang, Yinmiao Wang, Jian Chen, Fang Xu, Jiyan Pang · 2025 · JACS Au
  2. Bioorthogonal Sonodynamic Plug‐and‐Play Targeting Chimeras (SDPTAC) for Precise Targeted Protein Degradation
    Yuhan Bao, Yaojin Zhu, Xinhao Wei, Yuxin Fang, Jiayi Zhu, Fei Gao, Guoqiang Dong, Shipeng He, Chunquan Sheng · 2025 · Advanced Science
  3. Ginsenoside Rh2- functionalized liposomes enhanced BRD4-PROTAC delivery and antitumor efficacy via improved tumor targeting and ECM remodeling
    Lijuan Wen, Jialei Rao, Jiaoting Chen, Fang Li, Xixi Chen, Shenpeng Guo, Binghui Cui, 邱财生, Weiliang Chen · 2026 · Materials Today Bio
  4. Unveiling a new strategy for PDIA1 inhibition: Integration of activity-based probes profiling and targeted degradation
    Bei Zhang, Dawei Hong, Hujuan Qian, Keqing Ma, Liquan Zhu, Linye Jiang, Jingyan Ge · 2024 · Bioorganic Chemistry
  5. Correlation between Membrane Permeability and the Intracellular Degradation Activity of Proteolysis-Targeting Chimeras
    Hidetomo Yokoo, Hinata Osawa, Kosuke Saito, Yosuke Demizu · 2024 · Chemical and Pharmaceutical Bulletin
  6. Rapid and high-throughput screening of proteolysis targeting chimeras using a dual-reporter system expressing fluorescence protein and luciferase
    Shuai Meng, Yuan Meng, Xuena Yang, Wenwen Yu, Bole Li, Tianjun Liu, Jie Zhang, Xiubao Ren, Lin Zhang · 2025 · BMC Biology
  7. Design, synthesis, and biological evaluation of RIPK1-targeting PROTACs
    Hefeng Zhang, Shuonan Zhang, Tianchen Wang, Yaohan Lan, Yang Dai, Xia Peng, Yuxiang An, Xue Yi, Jing Ai, Wenhu Duan · 2025 · Molecular Diversity
  8. The Discovery of a Specific CKIP-1 Ligand for the Potential Treatment of Disuse Osteoporosis
    Yange Wei, Bo Wu, Mingqiu Liu, Chun‐Ping Cui · 2024 · International Journal of Molecular Sciences
  9. Facile Synthesis of Homodimeric Protein Ligands
    Weijun Gui, Thomas J. Kodadek · 2023 · ChemBioChem
  10. Rapid PROTAC discovery platform: nanomole scale array synthesis and direct screening of reaction mixtures to facilitate the expedited discovery and follow-up of PROTAC hits.
    Mateusz P. Plesniak, Emilia K. Taylor, Frederik Eisele, Christopher M. B. K. Kourra, Iacovos N. Michaelides, Alice Oram, Johan Wernevik, Zulma Santisteban Valencia, Hannah Rowbottom, Nadia Mann et al. · 2023 · ChemRxiv
  11. Continuous Flow Synthesis of Amides in Bio-Derived Solvent GVL
    Xu-Yang Mu, Rui Zhu, Li-Jie Yu, Wenlong Wang · 2024 · Letters in Organic Chemistry
  12. Unveiling New Triazoloquinoxaline‐Based PROTACs Designed for the Selective Degradation of the ncBAF Chromatin Remodeling Subunit BRD9
    Martina Pierri, Guglielmo Bove, Erica Gazzillo, Ester Colarusso, Francesca Scala, Giacomo Pepe, Stefania Terracciano, Maria Giovanna Chini, Nicla Simonelli, Ines Bruno et al. · 2025 · Chemistry - A European Journal
  13. Research progress of dual-targeting CDKs regulators for cancer therapy
    Fei-Xia Yue, Yalan Wang, Rui-Yan, Guoqing Chen, Xiaoting Li, Qing‐Kun Shen · 2025 · Bioorganic Chemistry
  14. De Novo Design of Hexamer‐Linker Dual‐Action Nano‐PROTAC for Tumor‐Specific Ferroptosis
    Ni‐Yuan Zhang, Zhuan Wen, Ming‐Ze Cai, Ke‐Ting Zhou, Hao‐Ze Li, Yixuan Liu, Shang Wei Wu, Yu Xia, Hong‐Wei An, Hao Wang · 2025 · Angewandte Chemie
  15. Split‐Deliver‐Click: Tumor‐Specific Protein Degradation via “AND” Logic‐Gated In‐Cell Bioorthogonal Clicking of PROTACs
    He Dong, Cilong Chu, Ihsan Ullah, Qing Xu, Zhenhai Pan, Youyong Yuan · 2026 · Angewandte Chemie
  16. Proteolysis-targeting chimera (PROTAC) in cancer: design principles and applications on “undruggable” targets
    Xun Lu, Jianliang Qin, Shuilin Dong, Yue Yuan, Zhanguo Zhang, B Zhang, Xiaoping Chen, Xiaoli Gan, Huifang Liang, Furong Liu · 2026 · Biomarker Research
  17. Pretargeted PROTAC Strategy Enables Precise Tumor Target Degradation via Self-Assembling Peptides
    Qianqian Wu, Chen Zhang, Yuanheng Li, Miao Zhang, Hao Yan, Naihan Xu, Chunyan Tan, Ying Tan · 2026 · ACS Applied Materials & Interfaces
  18. A Type II CDK6 Degrader Enables Cellular Targeting beyond the Limits of Type II Inhibition
    Ji Hyeon Kim, Caitlin E. Mills, Zuzanna Kozicka, Daniel C. Scott, Cyrus Jin, Zixuan Jiang, Brendan G. Dwyer, Qixiang Geng, Sean T. Toenjes, Woong Sub Byun et al. · 2026 · Journal of the American Chemical Society
  19. The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer
    Xin Lin, Hua Xiang, Guoshun Luo · 2026 · Drug Discovery Today
  20. Efficient, multi-hundred-gram scale access to E3 ubiquitin ligase ligands for degrader development
    Mark S. Cooper, Mark C. Norley, Simon Armitage, Joel O. Cresser-Brown, Anthony K. Edmonds, Sean Goggins, Jonathan P. Hopewell, Burhan Karadogan, Kevin A. Knights, Toby J. Nash et al. · 2023 · Organic & Biomolecular Chemistry
  21. Design and evaluation of anaplastic lymphoma kinase degraders using a covalent fumarate handle
    Namsik Yu, Ji‐Eun Lee, Seulki Park, Su Kyeong Yun, Do Hyun Ryu, Jung‐Ae Kim, Jeong‐Hoon Kim, Jong Yeon Hwang · 2024 · Bioorganic & Medicinal Chemistry Letters
  22. Spatiotemporally Controllable Covalent Bonding of RNA for Multi‐Protein Interference
    Hao Fang, Tingting Wang, Jun Dai, Jingjing Hu, Zhaojun Chen, Lizhen Yuan, Yuning Hong, Fan Xia, Xiaoding Lou · 2024 · Advanced Healthcare Materials
  23. Enzyme‐Activated Orthogonal Proteolysis Chimeras for Tumor Microenvironment‐Responsive Immunomodulation
    Caixia Sun, Songhan Liu, Jun Wei Lau, Hanyu Yang, Yun Chen, Bengang Xing · 2025 · Angewandte Chemie
  24. Transcription factor degraders
    Manni Wang, Yuhao Wei, Xiaoling Ma · 2025 · Elsevier eBooks
  25. HerTACs Enable Tumor‐Selective Lysosomal Degradation of Membrane and Extracellular Proteins via HER2 Trafficking
    Shipeng He, Wenjing Huang, Yaojin Zhu, Fei Gao, Yuxin Fang, Jiayi Zhu, Yuhan Bao, Guoqiang Dong, Chunquan Sheng · 2025 · Angewandte Chemie
  26. Synthesis and degradation effect of PROTACs targeting EGFR triple mutants
    Xiao-Xiao Xi, Hongyi Zhao, Minhang Xin, Shuai Mao, San‐Qi Zhang · 2025 · Bioorganic & Medicinal Chemistry
  27. PROTACs as novel therapeutics against Mycobacterium tuberculosis: Current progress and future directions
    Deepthi Ramesh, Ahammed Ameen Thottasseri · 2026 · European Journal of Medicinal Chemistry
  28. PROTAC-based protein degradation: a window of opportunity for melanoma therapy
    Giulia Gentile, Simona D’Aguanno, Marta Di Martile, Adele Petricca, Elisabetta Valentini, Stefano Scalera, Donatella Del Bufalo · 2026 · Journal of Biomedical Science
  29. Design, synthesis, and pharmacological evaluation of novel PROTAC degraders targeting 11β-HSD1 for metabolic disease intervention
    Liguo Wang, Xue Tao, Ming He, Yu Lu, Yuji Wang, Juanjuan Zhu · 2026 · Bioorganic Chemistry
  30. Autonomously Motile Nano‐PROTACs Act as Protein‐Sweeping Robots to Enhance Targeted Protein Degradation
    Xiang Yang Lu, Furui Qiu, Huijie Liang, Xiaomin Wang, Meng Xue, Jianghao Wang, Jinjin Shi, Hongling Zhang, B L Wang · 2026 · Advanced Materials
  31. Discovery of Effective Dual PROTAC Degraders with Synergistic Antitumor Activity for Overcoming Tamoxifen-Resistant Breast Cancer
    Lilan Xin, Jing Liu, Xinyi Guo, S Li, Zhangxiao Guo, Hongli Wang, Zemin Song, Xiaofei Deng, C Wang, P H Fang et al. · 2026 · Journal of Medicinal Chemistry
  32. RIMTAC: A Novel Degrader Design Platform by Indirect VHL-Recruitment via RIPK1
    Chang Shen, HD Sun, Ruining Li, Raghupathi Mutyala, Xinjian Tian, Chaoqun Huang, Jinglei Hu, Jie An, Lin Li, Tao Zhang et al. · 2026 · Journal of Medicinal Chemistry
  33. Programmable nanomedicine via bioorthogonal molecular engineering
    Sunwoo Im, Seyoung Koo, Jong Seung Kim · 2026 · Nano Convergence
  34. Feasibility and Advantages of Designing Proteolysis Targeting Chimeras Targeting Peroxisome Proliferator-activated Receptors for Cancer Treatment
    Sihan Zhang, Zhipeng Yao, Na Zeng, Zheng Liu, Qi‐Dong Xia, Shao-Gang Wang · 2024 · Exploratory Research and Hypothesis in Medicine
  35. PROTACs in the Management of Prostate Cancer
    Deepa S. Mandlik, Satish K. Mandlik · 2024 · Springer eBooks
  36. Discovery of Alkenyl Oxindole as a Novel PROTAC Moiety for Targeted Protein Degradation via CRL4 DCAF11 Recruitment
    Ying Wanga, Tianzi Wei, Man Zhao, Aima Huang, Fan Sun, Lu Chen, Risheng Lin, Yubao Xie, Ming Zhang, Shiyu Xu et al. · 2024 · bioRxiv (Cold Spring Harbor Laboratory)
  37. DNA-templated spatially controlled proteolysis targeting chimeras for CyclinD1-CDK4/6 complex protein degradation
    Rong Zheng, Abhay Prasad, Deeksha Satyabola, Yang Xu, Hao Yan · 2024 · bioRxiv (Cold Spring Harbor Laboratory)
  38. Degradation of intrinsically disordered proteins using proteolysis targeting nanobody conjugate
    Xiaofeng Sun, Dinglan Wu, Chengjian Zhou, Simin Xia, Xi Chen · 2024 · bioRxiv (Cold Spring Harbor Laboratory)
  39. Proteolysis‐Targeting Chimeras (PROTACs)
    Liang Shen · 2025
  40. De novo designed bifunctional proteins for targeted protein degradation
    Bram Mylemans, Bogusława Korona, Amanda M. Acevedo‐Jake, Ailsa MacRae, Thomas A. Edwards, Danny T. C. Huang, Andrew John Wilson, Laura S. Itzhaki, Derek N. Woolfson · 2025 · bioRxiv (Cold Spring Harbor Laboratory)
  41. Ruthenium-catalysed C‒H amidation for the late-stage synthesis of PROTACs
    Daniele Antermite, Stig D. Friis, Johan R. Johansson, Okky Dwichandra Putra, Lutz Ackermann, Magnus J. Johansson · 2023 · ChemRxiv
  42. Computational strategies for the design of proteolysis targeting chimera degraders: Artificial intelligence enabled PROTAC design
    Rajamanikkam Kamaraj, Radim Nencka, Petr Pávek · 2024 · Annual reports in medicinal chemistry
  43. Discovery of the First Potent Ror1 Degrader for the Treatment of Non-Small Cell Lung Cancer
    Fengtao Zhou, Jinlin Li, Lin Li, Caiyun Hou, Zhaodi Tian, Yang Zhou, Jinwei Zhang, Xiaomei Ren, Zhen Wang, Weixue Huang et al. · 2024 · SSRN Electronic Journal
  44. Integrating PROTAC technology with natural product research: A new frontier in target identification
    Baoyu Wei, Jinyun Dong, Yi Liang, Jiang‐Jiang Qin, Guoyin Kai · 2025 · Elsevier eBooks
  45. Harnessing the power of traditional Chinese medicine for targeted protein degradation
    Zheng Wu, Bo Zhu, Yiwen Shou, Hongwei Guo · 2025 · Elsevier eBooks
  46. The Functions and Regulatory Chemicals of Human Leucine Zipper Transcription Factors (LZ TFs)
    Hanming Yang, Shuyang Bi, Biao Yu, Pengfei Fang, Jing Wang · 2025 · 化学学报
  47. Degradation of Cyclin-Dependent Kinase: A New Weapon for Cancer Therapy
    Xing Tian, Xiaojie Dai, Ye Zhong, Maosheng Cheng, Yang Liu · 2025 · Pharmaceutical Fronts
  48. Surf2Spot: A Surface-Informed Geometry-Aware Model for Predicting Binder and Nanobody Design Hotspots
    Anwen Zhao, Yu Li, Tianhao Wu, Ran Fu, Zixuan Wang, Yanfen Xu, Xuliang Han, Yuxuan Lou, Wenying Wang, Jun Yan et al. · 2026 · bioRxiv (Cold Spring Harbor Laboratory)
  49. Synthesis and anticancer activity of parthenolide-based PROTACs for IKKβ degradation
    Zhenxi Su, Yiwu Wu, Yijie Su, Yuhan He, Jieyin Liu, Deng‐Gao Zhao · 2026 · Bioorganic & Medicinal Chemistry Letters
  50. Efficient green synthesis of the targeted proteolysis system component
    Maria Zakharova, М. В. Чудинов, Maxim E. Zhuravlev, Alexei Lukin · 2026 · Mendeleev Communications
  51. Design and Synthesis of Pyrrolo[3,4- d ]pyrimidine-Based ATR Degraders for Effective Treatment of Colorectal Cancer in Mouse Model
    Nian‐Dong Mao, Zi Hui, Chen-Chen Wang, Meng-Lan He, Shun-Ran Li, Meng-Qian Yu, Lulu Ye, Jiawei Zhou, Zong-Hao Wang, Bo-Qun Du et al. · 2026 · Journal of Medicinal Chemistry
  52. Molecular Glue Degraders Redefining Targeted Therapies From Discovery to Therapeutic Applications
    Jiaye Wen, Jingtian Yu, Wuqiang Wen, Baishan Jiang · 2026 · MedComm – Oncology
  53. Kinase degrader: a new era of drug development
    Chao Zhang, Yu Rao · 2026 · Elsevier eBooks
  54. Targeting taurine metabolism via PROTAC-mediated SLC6A6 degradation potentiates photodynamic therapy and reverses immunosuppression in cholangiocarcinoma
    Jingjin Zhu, Tianhao Zou, Weimin Wang, Jianjun Xu, Xuan Li, Lei Liu, Bohan Yang, Zifang Song, Yang Gao · 2026 · Journal of Nanobiotechnology
  55. Design, synthesis, and biological evaluation of HSP70-mediated HEMTACs as novel androgen receptor degraders
    Zhenzhen Li, Xinru Han, Shuxian Guo, Lüpei Du · 2026 · European Journal of Medicinal Chemistry
  56. PROTAC-based nanoassemblies targeting BRD4 for potentiate FLASH radiosensitization therapy
    Ruiling Xu, Xiaowen Han, Yunfei Sun, Chaofan Ma, Shuqing Liao, Ruo Tang, Yinquan Pu, Xueting Zheng, Jie Zhang, Wen Yang et al. · 2026 · Materials Today Bio
  57. Microneedle‐Assisted Systems for the Delivery of Proteolysis Targeting Chimeras (PROTACs)
    Pooja Tiwary, Krishil Oswal, Aishwarya Shirke, Heena V. Maithania, Ryan Varghese, Lalitkumar K. Vora · 2026 · Advanced Therapeutics
  58. Discovery of a potent PROTAC targeting G9a suppresses proliferation of triple-negative breast cancer cells and psoriasis-like keratinocytes
    Mingxia Liu, Lian Wang, Zhaoping Pan, Jing Ye, Fengbo Wu, Gu He, Yujuan Chen · 2026 · European Journal of Medicinal Chemistry
  59. Integrative structural and computational analysis reveals potential design principles for efficient PROTAC degraders
    Yi Zhou, Yu Cao, Xinyue Ma, Hao Yang, Siyuan Tian, Chenjia Zhu, Yilin Tang, Ran Zhang, José N. Onuchic, Fang Bai · 2026 · Cell Reports Physical Science
  60. Sprayable androgen receptor PROTAC degrader for immunomodulation and accelerated skin regeneration
    Se Youn Jang, Byeongmin Park, Eunbyeol Ko, 신동원, Yeongji Jang, Won Suk Lee, Jae-Hyeon Lee, Ansoo Lee, Jooho Park, S P Lee et al. · 2026 · Chemical Engineering Journal
  61. Discovery of novel cereblon-recruiting PRMT5 degraders with in vivo efficacy against triple-negative breast cancer
    Yuzhan Li, Yaxun Guo, Dazhao Mi, Fubing Li, Jingfeng Song, Qiansen Zhang, Ceshi Chen, Zhigang Yu, Yihua Chen · 2026 · European Journal of Medicinal Chemistry
  62. Development of Hydrophobic Tag Based HDAC6 Degrader for Ulcerative Colitis Treatment
    Daoran Lu, Rongfeng Liu, Congcong Zheng, Yueyi Sun, Jianjun Gao, Yepeng Luan · 2026 · Journal of Medicinal Chemistry
  63. De Novo-Designed Bifunctional Proteins for Targeted Protein Degradation
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  64. A review of deep learning-based molecular generation
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  65. Discovery of BRD9 PROTAC/IMiD Bifunctional Molecules as Potent Therapeutics for Hematologic Malignancies
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  66. Transdermal STING Degradation Reprograms Innate‐Adaptive Immunity Crosstalk for Relapse‐Free Psoriasis and Comorbid Arthritis Therapy
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  67. Design, synthesis, and biological evaluation of the first fibroblast growth factor receptor 4 PROTAC degrader
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  68. Proteolysis-Targeting Chimera-Loaded Hydrogel Dressings Orchestrate Immunoregulation and Angiogenesis to Promote Tissue Regeneration in Large Diabetic Wounds
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  69. Hsc70-Mediated Targeting Chimeras for Targeted Protein Degradation via Chaperone-Mediated Autophagy
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  70. Branched DNA Nanoplatform-Based Multivalent PROTACs for Tumor Microenvironment-Responsive Degradation of Telomere-Binding Proteins in Tumor Therapy
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  71. Targeted dual degradation of GPC-3 and VEGFR with multivalent DNA nanoflower-based LYTACs for hepatocellular carcinoma therapy
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  72. Micellar LYTAC-engineered bionic coatings abrogate RANK-dependent osteocatabolism and boost fibrillogenesis-mimetic mineral accretion for empowering osteoporotic osseointegration
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  73. A Versatile DNA‐Encoded Library Platform for the Discovery of Highly Cooperative Chemical Inducers of Proximity
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  74. Recent Advances in Nanotechnology for Targeted Protein Degradation
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  75. Alendronate-mineralized nanoparticles loaded with ALK-PROTAC reverse the resistance and rebound effects of ALK+ NSCLC to PROTAC therapy by disrupting the mitochondria-linked feedback
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  76. Surf2Spot: a surface-informed geometry-aware model for predicting partner-independent binder and nanobody design hotspots
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  77. PROTACs in personalized and precision medicine: transforming targeted therapy with advances in selectivity and patient stratification
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  78. Proteoform-Resolved Interaction Mapping of Target Protein Complexes in Living Cells via Tracelessly Releasable Cross-Linking
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  79. Protein degraders targeting JAK/STAT3 signaling pathway are emerging therapeutic modalities for human cancers
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  80. PROTAC-Loaded Nanoparticles Induce a “ROS Storm” through Targeted Degradation of GPX4 in Combination with a Mild Photothermal/Fenton-like Reaction for the Treatment of Triple-Negative Breast Cancer
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  81. Discovery of Tricyclic Oxazinoquinolinone-Based BCL6 PROTAC Degraders with Potent Activity Against Diffuse Large B-Cell Lymphoma
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  82. Identification of selective FGFR2/4 degraders with potent antiproliferative activity
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  83. Discovery of Threonine Tyrosine Kinase (TTK) Degraders Utilizing an Electrophilic Monomethyl Fumarate Handle
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  84. BindingDB Entry 50021764: Casitas b cell lymphoma‑B (Cbl-b): A new therapeutic avenue for small-molecule immunotherapy.
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  86. BindingDB Entry 50023674: Discovery of the first potent ROR1 degrader for the treatment of non-small cell lung cancer.
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  87. BindingDB Entry 50023713: MALT1 Inhibitors and Degraders: Strategies for NF-κB-Driven Malignancies.
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  88. BindingDB Entry 50023756: Discovery and Characterization of RP03707: A Highly Potent and Selective KRASG12D PROTAC.
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  89. BindingDB Entry 50022782: Modulating Phosphorylation by Proximity-Inducing Modalities for Cancer Therapy.
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  90. BindingDB Entry 50022106: Targeting kelch-like (KLHL) proteins: achievements, challenges and perspectives.
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  91. BindingDB Entry 50020673: Discovery of Potent and Highly Selective Interleukin-2-Inducible T-Cell Kinase Degraders with
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  92. BindingDB Entry 50021145: Annual review of PROTAC degraders as anticancer agents in 2022.
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  93. BindingDB Entry 50023017: Discovery of the first selective and potent PROTAC degrader for the pseudokinase TRIB2.
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  94. BindingDB Entry 50021231: Recent advances of targeting nicotinamide phosphoribosyltransferase (NAMPT) for cancer drug discovery.
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  95. BindingDB Entry 50020994: Facilitating the development of molecular glues: Opportunities from serendipity and rational design.
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  96. BindingDB Entry 50023673: Rational Design, Synthesis, and Biological Evaluation of Novel c-Met Degraders for Lung Cancer Therapy.
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  97. BindingDB Entry 50021852: Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment.
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  98. BindingDB Entry 50021125: Development of de-novo coronavirus 3-chymotrypsin-like protease (3CLpro) inhibitors since COVID-19 outbreak: A strategy to tackle challenges of persistent virus infection.
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  99. BindingDB Entry 50020221: Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).
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  100. BindingDB Entry 50021847: Distinct Amino Acid-Based PROTACs Target Oncogenic Kinases for Degradation in Non-Small Cell Lung Cancer (NSCLC).
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