Discovery of Novel Potent Triple IKZF1/2/3 Degraders for the Treatment of Hematological Cancers

Immunomodulatory drugs (IMiDs) are widely utilized therapies in multiple hematological cancers; however, their clinical application is frequently constrained by drug resistance. Here, though screening of diverse cereblon (CRBN) binders, comprehensive structure–activity relationships (SAR) analyses a...

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Hlavní autor:	Ting Wei (113015) (author)
Další autoři:	Shiyang Sun (588807) (author), Xiaotong Hu (558839) (author), Pengli Wei (14641202) (author), Zhiya Fan (9411634) (author), Jian Yan (49839) (author), Yalei Wang (669779) (author), Zhenze Qi (21726058) (author), Changkai Jia (21726052) (author), Yaqiu Mao (21726055) (author), Tingting Yang (166111) (author), Xu Cai (5326745) (author), Bingkun Li (9752768) (author), Zhiyuan Zhao (1400806) (author), Min Qiao (111120) (author), Yaxin Zou (21726061) (author), Weijie Qin (1694185) (author), Xuesong Feng (754835) (author), Hongzhou Shang (21929961) (author), Pengyun Li (2685118) (author), Zhibing Zheng (9716361) (author), Song Li (65582) (author)
Vydáno:	2025
Témata:	Biophysics Biochemistry Cell Biology Genetics Molecular Biology Pharmacology Biotechnology Cancer Hematology Infectious Diseases Virology Space Science Chemical Sciences not elsewhere classified widely utilized therapies promising therapeutic candidate multiple hematological cancers marked synergistic effects admirable pharmacokinetic properties systematic degradation profiling overcame acquired resistance diffuse large b 22 </ b 50 </ sub 3 degrader featuring hematological cancer treatment dlbcl cancer cells cancer cells targeted degradation drug resistance tyrosine kinase though screening range ic phthalazinone scaffold orally administered nanomolar dc frequently constrained findings establish diverse cereblon dependent manner demonstrated nanomolar clinical application cell lymphoma bruton ’ broader applicability aml ), 3 degraders
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Discovery of Novel Potent Triple IKZF1/2/3 Degraders for the Treatment of Hematological Cancers

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