Chemistries of bifunctional PROTAC degraders

Cites (270)

Items 201–270 of 270

1. Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins
   Nobumichi Ohoka, Genichiro Tsuji, Takuji Shoda, Takuma Fujisato, Masaaki Kurihara, Yosuke Demizu, Mikihiko Naito · 2019 · ACS Chemical Biology
2. Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion
   Xiaqiu Qiu, Yuan‐Qing Li, Bin Yu, Jie Ren, Huidan Huang, Min Wang, Hong Ding, Zhiyu Li, Jubo Wang, Jinlei Bian · 2020 · European Journal of Medicinal Chemistry
3. Recent advances in the development of covalent inhibitors
   Hyunsoo Kim, Yoon Soo Hwang, Mingi Kim, Seung Bum Park · 2021 · RSC Medicinal Chemistry
4. Uncoupling of PARP1 trapping and inhibition using selective PARP1 degradation
   Shuai Wang, Lei Han, Jungsoo Han, Peng Li, Qing Ding, Qing-Jun Zhang, Zhiping Liu, Chuo Chen, Yonghao Yu · 2019 · Nature Chemical Biology
5. Protein degradation through covalent inhibitor-based PROTACs
   Gang Xue, Jiahui Chen, Lihong Liu, Danli Zhou, Yingying Zuo, Tiancheng Fu, Zhengying Pan · 2020 · Chemical Communications
6. Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC
   Yang, Fang, Wen, Yalei, Wang, Chaofan, Zhou, Yuee, Zhou, Yang, Zhang, Zhi-Min, Liu, Tongzheng, Lu, Xiaoyun · 2022 · European Journal of Medicinal Chemistry
7. Mechanisms of resistance to BCR–ABL TKIs and the therapeutic strategies: A review
   Ke Yang, Liwu Fu · 2014 · Critical Reviews in Oncology/Hematology
8. Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation
   Nobumichi Ohoka, Yoko Morita, Katsunori Nagai, Kenichiro Shimokawa, Osamu Ujikawa, Ikuo Fujimori, Masahiro Ito, Youji Hayase, Keiichiro Okuhira, Norihito Shibata et al. · 2018 · Journal of Biological Chemistry
9. Targeting the Allosteric Site of Oncoprotein BCR-ABL as an Alternative Strategy for Effective Target Protein Degradation
   Kenichiro Shimokawa, Norihito Shibata, Tomoya Sameshima, Naoki Miyamoto, Osamu Ujikawa, Hiroshi Nara, Nobumichi Ohoka, Takayuki Hattori, Nobuo Cho, Mikihiko Naito · 2017 · ACS Medicinal Chemistry Letters
10. Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors
    Jianyong Chen, Longchuan Bai, Denzil Bernard, Zaneta Nikolovska‐Coleska, Cindy Gomez, Jian Zhang, Yi Han, Shaomeng Wang · 2010 · ACS Medicinal Chemistry Letters
11. Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma
    Yalin Tu, Yameng Sun, Shuang Qiao, Yao Luo, Panpan Liu, Zhong‐Xing Jiang, Yumin Hu, Zifeng Wang, Peng Huang, Shijun Wen · 2021 · Journal of Medicinal Chemistry
12. Global PROTAC Toolbox for Degrading BCR–ABL Overcomes Drug-Resistant Mutants and Adverse Effects
    Yiqing Yang, Hongying Gao, Xiuyun Sun, Yonghui Sun, Yueping Qiu, Qinjie Weng, Yu Rao · 2020 · Journal of Medicinal Chemistry
13. What Is the Right Dose? The Elusive Optimal Biologic Dose in Phase I Clinical Trials
    Alex A. Adjei · 2006 · Journal of Clinical Oncology
14. Folate Targeting Enables Durable and Specific Antitumor Responses from a Therapeutically Null Tubulysin B Analogue
    Christopher P. Leamon, Joseph A. Reddy, Marilynn Vetzel, Ryan Dorton, Elaine M. Westrick, Nikki L. Parker, Yu Wang, Iontcho R. Vlahov · 2008 · Cancer Research
15. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)
    Matthäus Getlik, David V. Smil, Carlos Zepeda‐Velázquez, Yuri Bolshan, Gennady I. Poda, Hong Yang Wu, Aiping Dong, Ekaterina Kuznetsova, Richard C. Marcellus, Guillermo A. Senisterra et al. · 2016 · Journal of Medicinal Chemistry
16. Selective inhibition of Ph-positive ALL cell growth through kinase-dependent and -independent effects by CDK6-specific PROTACs
    De Dominici, Marco, Porazzi, Patrizia, Xiao, Youcai, Chao, Allen, Tang, Hsin-Yao, Kumar, Gaurav, Fortina, Paolo, Spinelli, Orietta, Rambaldi, Alessandro, Peterson, Luke F. et al. · 2020 · Blood
17. Smac mimetics: implications for enhancement of targeted therapies in leukemia
    Ellen Weisberg, Arghya Ray, Rosemary Barrett, Erik A. Nelson, Amanda L. Christie, DALE A. PORTER, Christopher Straub, Leigh S. Zawel, John F. Daley, Suzan Lazo-Kallanian et al. · 2010 · Leukemia
18. Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC)
    Fangyuan Cao, Sander de Weerd, Deng Chen, Martijn R. H. Zwinderman, Petra E. van der Wouden, Frank J. Dekker · 2020 · European Journal of Medicinal Chemistry
19. Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers
    Chao-Guo Cao, Jie Yang, Yong Xia Chen, Peiting Zhou, Yingwei Wang, Wu Du, Lifeng Zhao, Yuanwei Chen · 2020 · Journal of Medicinal Chemistry
20. Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties
    Jaime-Figueroa, Saul, Buhimschi, Alexandru D., Toure, Momar, Hines, John, Crews, Craig M. · 2020 · Bioorganic & Medicinal Chemistry Letters
21. Development of target protein-selective degradation inducer for protein knockdown
    Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Shinichi Sato, Mikihiko Naito, Yuichi Hashimoto · 2011 · Bioorganic & Medicinal Chemistry
22. Merging PROTAC and molecular glue for degrading BTK and GSPT1 proteins concurrently
    Zimo Yang, Yonghui Sun, Zhihao Ni, Celi Yang, Yan Tong, Yujie Liu, Haitao Li, Yu Rao · 2021 · Cell Research
23. Structural Insights into PROTAC-Mediated Degradation of Bcl-xL
    Chun‐wa Chung, Han Dai, Esther Fernández, Christopher P. Tinworth, Ian Churcher, Jenni Cryan, Jane C. Denyer, John D. Harling, Agnieszka Konopacka, Markus A. Queisser et al. · 2020 · ACS Chemical Biology
24. A Fluorescent Probe for Rapid, High‐Contrast Visualization of Folate‐Receptor‐Expressing Tumors In Vivo
    Koji Numasawa, Kenjiro Hanaoka, Naoko Saito, Yoshifumi Yamaguchi, Takayuki Ikeno, Honami Echizen, Masahiro Yasunaga, Toru Komatsu, Tasuku Ueno, Masayuki Miura et al. · 2020 · Angewandte Chemie International Edition
25. Development of CDK2 and CDK5 Dual Degrader TMX‐2172
    Mingxing Teng, Jie Jiang, Zhixiang He, Nicholas P. Kwiatkowski, Katherine A. Donovan, Caitlin E. Mills, Chiara Victor, John M. Hatcher, Eric S. Fischer, Peter Karl Sorger et al. · 2020 · Angewandte Chemie International Edition
26. A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo
    Lijie Zhao, Xin Han, Jianfeng Lü, Donna McEachern, Shaomeng Wang · 2020 · Neoplasia
27. Photoresponsive Surfaces with Two Independent Wavelength-Selective Functional Levels
    Petra Stegmaier, José Marı́a Alonso, Aránzazu del Campo · 2008 · Langmuir
28. Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design
    Chacón Simon, Selena, Wang, Feng, Thomas, Lance R., Phan, Jason, Zhao, Bin, Olejniczak, Edward T., Macdonald, Jonathan D., Shaw, J. Grace, Schlund, Caden, Payne, William et al. · 2020 · Journal of Medicinal Chemistry
29. Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology
    Chiara Borsari, Darci Jones Trader, Annalisa Tait, Maria Paola Costi · 2020 · Journal of Medicinal Chemistry
30. Sequentially Photocleavable Protecting Groups in Solid-Phase Synthesis
    Martin Kessler, Ralf Glatthar, Bernd Giese, Christian G. Bochet · 2003 · Organic Letters
31. A novel cereblon modulator for targeted protein degradation
    Kim, Sung Ah, Go, Ara, Jo, Seung-Hyun, Park, Sun Jun, Jeon, Young Uk, Kim, Ji Eun, Lee, Heung Kyoung, Park, Chi Hoon, Lee, Chong-Ock, Park, Sung Goo et al. · 2019 · European Journal of Medicinal Chemistry
32. Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders
    Brett L. Roberts, Zhi‐Xiong Ma, Ang Gao, Eric D. Leisten, Dan Yin, Wei Xu, Weiping Tang · 2020 · ACS Chemical Biology
33. Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening
    Jeremy S. Disch, Jennifer M. Duffy, Esther C. Y. Lee, Diana Gikunju, Betty Chan, Benjamin D. Levin, Michael I. Monteiro, Sarah A. Talcott, Anthony C. Lau, Fei Zhou et al. · 2021 · Journal of Medicinal Chemistry
34. The rise of covalent proteolysis targeting chimeras
    Ronen Gabizon, Nir London · 2021 · Current Opinion in Chemical Biology
35. Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer
    Thomas L. Gonzalez, Molly Hancock, Siqi Sun, Christina L. Gersch, Jose Maciel Larios, Wadie S. David, Jiantao Hu, Daniel F. Hayes, Shaomeng Wang, James Michael Rae · 2020 · Breast Cancer Research and Treatment
36. Tinkering Outside the Kinase ATP Box: Allosteric (Type IV) and Bivalent (Type V) Inhibitors of Protein Kinases
    Kurt J. Cox, Carolyn D. Shomin, Indraneel Ghosh · 2010 · Future Medicinal Chemistry
37. Discovery of Selective Small Molecule Degraders of BRAF-V600E
    Xiaoran Han, Liqun Chen, Yuanqi Wei, Weihua Yu, Yanke Chen, Chunyan Zhang, Bingyang Jiao, Tingting Shi, Lei Sun, Chao Zhang et al. · 2020 · Journal of Medicinal Chemistry
38. Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation
    Ming He, Wenxing Lv, Yu Rao · 2021 · Frontiers in Cell and Developmental Biology
39. A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions
    Le Guo, Yaxian Zhou, Xueqing Nie, Zhongrui Zhang, Zhen Zhang, Chunrong Li, Taobo Wang, Weiping Tang · 2022 · European Journal of Medicinal Chemistry
40. Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues
    Sarath Ramachandran, Alessio Ciulli · 2020 · Current Opinion in Structural Biology
41. Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation
    Haixia Liu, Xinyu Ding, Linyi Liu, Qianglong Mi, Quanju Zhao, Yubao Shao, Chaowei Ren, Jinju Chen, Ying Kong, Xing Qiu et al. · 2021 · European Journal of Medicinal Chemistry
42. Targeting KRAS Directly
    Frank P. McCormick · 2018 · Annual Review of Cancer Biology
43. SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression
    Haibin Zhou, Longchuan Bai, Renqi Xu, Donna McEachern, Krishnapriya Chinnaswamy, Ruiting Li, Bo Wen, Mi Wang, Chao‐Yie Yang, Jennifer L. Meagher et al. · 2021 · ACS Medicinal Chemistry Letters
44. Inhibitor of apoptosis proteins as therapeutic targets in multiple myeloma
    Vijay G. Ramakrishnan, Utkarsh Painuly, Teresa K. Kimlinger, Janine Haug, S. Vincent Rajkumar, Shaji Kunnathu Kumar · 2014 · Leukemia
45. Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)
    Soňa Krajčovičová, Radek Jorda, Denisa Hendrychová, Vladimı́r Kryštof, Miroslav Soural · 2018 · Chemical Communications
46. First small-molecule PROTACs for G protein-coupled receptors: inducing 1A-adrenergic receptor degradation
    Zhenzhen Li, Yuxing Lin, Hui Song, Xiaojun Qin, Zhongxia Yu, Zheng Zhang, Gaopan Dong, Xiang Li, Xiaodong Shi, Lüpei Du et al. · 2020 · Acta Pharmaceutica Sinica B
47. Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders
    Xufen Yu, Jia Xu, Ling Xie, Li Wang, Yudao Shen, Kaitlyn M. Cahuzac, Xian Chen, Jing Liu, Ramon E. Parsons, Jian Jun Jin · 2021 · Journal of Medicinal Chemistry
48. Risk factors for progression to castration-resistant prostate cancer in metastatic prostate cancer patients
    Tingting Lin, Ye‐Hui Chen, Yu‐Peng Wu, Shaozhan Chen, Xiaodong Li, Yun‐Zhi Lin, Shao‐Hao Chen, Qing‐Shui Zheng, Yong Wei, Ning Xu et al. · 2019 · Journal of Cancer
49. Proteasome Inhibition Causes Regression of Leukemia and Abrogates BCR-ABL–Induced Evasion of Apoptosis in Part through Regulation of Forkhead Tumor Suppressors
    Zainab Jagani, Keli Song, Jeffery Lorne Kutok, M. Rajan Dewar, Armelle Melet, Tanya Santos, Alexandra R. Grassian, Saghi Ghaffari, Catherine J. Wu, Ruibao Ren et al. · 2009 · Cancer Research
50. X-ray structure determination of (2S, 3R)-3-amino-2-hydroxy-4-phenylbutanoic acid, a new amino acid component of bestatin.
    Hikaru Nakamura, Hiroyuki Suda, TOMOHISA TAKITA, TAKAAKI AOYAGI, HAMAO UMEZAWA, Yöichi Iitaka · 1976 · The Journal of Antibiotics
51. Nuclear cIAP1 overexpression is a tumor stage- and grade-independent predictor of poor prognosis in human bladder cancer patients
    Xiangyu Che, Deyong Yang, Huafeng Zong, Jianbo Wang, Xiancheng Li, Feng Chen, Xiaochi Chen, Xishuang Song · 2011 · Urologic Oncology Seminars and Original Investigations
52. Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1)
    Zhimin Zhang, Xinyue Chang, Chixiao Zhang, Shenxin Zeng, Meihao Liang, Zhen Ma, Zunyuan Wang, Wenhai Huang, Zhengrong Shen · 2020 · Journal of Enzyme Inhibition and Medicinal Chemistry
53. Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC)
    Zhenzhen Li, Siyue Ma, Xingye Yang, Ling Zhang, Liang Dong, Gaopan Dong, Lüpei Du, Zhenghua Lv, Minyong Li · 2021 · European Journal of Medicinal Chemistry
54. The Role of MDM2 in Promoting Genome Stability versus Instability
    Mohammad Reza Saadatzadeh, Adily N. Elmi, Pankita H. Pandya, Khadijeh Bijangi‐Vishehsaraei, Jixin Ding, Christopher W. Stamatkin, Aaron Cohen‐Gadol, Karen E. Pollok · 2017 · International Journal of Molecular Sciences
55. Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation
    Liang Jiang, Yuting Wang, Qian Li, Zhengchao Tu, Sihua Zhu, Sanfang Tu, Zhang Zhang, Ke Ding, Xiaoyun Lu · 2020 · Acta Pharmaceutica Sinica B
56. Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure–Activity Relationship Studies
    Xufen Yu, Jia Xu, Yudao Shen, Kaitlyn M. Cahuzac, Kwang‐Su Park, Brandon Dale, Jing Liu, Ramon E. Parsons, Jian Jun Jin · 2022 · Journal of Medicinal Chemistry
57. Increased Conformational Flexibility of a Macrocycle–Receptor Complex Contributes to Reduced Dissociation Rates
    Adrian Glas, Eike‐Christian Wamhoff, Dennis M. Krüger, Christoph Rademacher, Tom N. Grossmann · 2017 · Chemistry - A European Journal
58. Scaffold hopping enables direct access to more potent PROTACs with in vivo activity
    George M. Burslem, Daniel P. Bondeson, Craig M. Crews · 2020 · Chemical Communications
59. Folate Receptor-Targeted Multimodality Imaging of Ovarian Cancer in a Novel Syngeneic Mouse Model
    Meltem Ocak, Andrea G. Gillman, Jamee Bresee, Lixin Zhang, Anda Vlad, Cristina Müller, Roger Schibli, Wilson Barry Edwards, Carolyn J. Anderson, H. Michael Gach · 2014 · Molecular Pharmaceutics
60. MicroRNA501‐5p induces p53 proteasome degradation through the activation of the mTOR/MDM2 pathway in ADPKD cells
    Lucia de Stephanis, Alessandra Mangolini, Miriam Servello, Peter C. Harris, Lucio Dell’Atti, Paolo Pinton, Gianluca Aguiari · 2018 · Journal of Cellular Physiology
61. PROTAC-Mediated Degradation of Estrogen Receptor in the Treatment of Cancer
    Robert B. Kargbo · 2019 · ACS Medicinal Chemistry Letters
62. Construction of an IMiD-based azide library as a kit for PROTAC research
    Haixia Liu, Renhong Sun, Chaowei Ren, Xing Qiu, Xiaobao Yang, Biao Jiang · 2020 · Organic & Biomolecular Chemistry
63. Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs
    Shinichi Sato, Hiroshi Aoyama, Hiroyuki Miyachi, Mikihiko Naito, Yuichi Hashimoto · 2008 · Bioorganic & Medicinal Chemistry Letters
64. Neocortical-Like Organization of Avian Auditory ‘Cortex’
    J. Martin Wild, Nils O.E. Krützfeldt · 2010 · Brain Behavior and Evolution
65. Development of a Potent Protein Degrader against Oncogenic BCR-ABL Protein
    Norihito Shibata, Nobumichi Ohoka, Takayuki Hattori, Mikihiko Naito · 2019 · Chemical and Pharmaceutical Bulletin
66. Immunochemical identification of the cell surface bound leucine aminopeptidase, the target enzyme for the immunostimulant bestatin.
    Gabriele Leyhausen, Monika Gramzow, Rudolf Karl Zahn, Renate Steffen, HAMAO UMEZAWA, WERNER E. G. MÜTLLER · 1983 · The Journal of Antibiotics
67. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-AblT315I mutant
    Xiaoyun Lu, Zhang Zhang, Xiaomei Ren, Xiaofeng Pan, Deping Wang, Xiaoxi Zhuang, Jingfeng Luo, Rongmin Yu, Ke Ding · 2015 · Bioorganic & Medicinal Chemistry Letters
68. Exocytosis provides the membrane for protrusion, at least in migrating fibroblasts
    Mark S. Bretscher · 2008 · Nature Reviews Molecular Cell Biology
69. Molecular cloning and tissue-specific expression ofMrad9, a murine orthologue of theSchizosaccharomyces pombe rad9+ checkpoint control gene
    Haiying Hang, Sarah J. Rauth, Kevin M. Hopkins, Scott K. Davey, Howard B. Lieberman · 1998 · Journal of Cellular Physiology
70. Epigenetics during EMT in lung cancer: EZH2 as a potential therapeutic target
    Anastasios Dimou, Toros A. Dincman, Emilie Evanno, Robert M. Gemmill, Joëlle Roche, Harry A. Drabkin · 2017 · Cancer Treatment and Research Communications