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

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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Bibliographic Details
Main Author: Ting Wei (113015) (author)
Other Authors: 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)
Published: 2025
Subjects:
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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