Discovery of CFT8634, a Potent, Selective, and Orally Bioavailable Heterobifunctional Degrader of BRD9

The chromatin factor bromodomain-containing protein 9 (BRD9) is a genetic dependency in SMARCB1-perturbed or SMARCB1-null cancers including synovial sarcoma. In such cancers, the degradation of BRD9 is hypothesized to result in an anticancer effect. Here, we report the discovery and characterization...

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التفاصيل البيبلوغرافية
المؤلف الرئيسي:	Katrina L. Jackson (2047516) (author)
مؤلفون آخرون:	Ning Yin (460850) (author), Roman V. Agafonov (10493470) (author), Prasoon Chaturvedi (1992091) (author), Kyle Cole (22677465) (author), Scott J. Eron (1514029) (author), Andrew C. Good (1270980) (author), June A. Hart (22677468) (author), Minsheng He (1276014) (author), Christina S. Henderson (22677471) (author), Hongwei Huang (1444249) (author), R. Jason Kirby (22677474) (author), Linda Lee (163668) (author), Moses Moustakim (5792057) (author), Christopher G. Nasveschuk (334912) (author), Andrew J. Phillips (334915) (author), Roy M. Pollock (672515) (author), Laura L. Poling (14900562) (author), Gesine K. Veits (1304382) (author), Jeremy Yap (22677477) (author), Rhamy Zeid (4512625) (author), Amro Ali (22677480) (author), Adam S. Crystal (14993880) (author), Eunju Hurh (2686873) (author), Huan Liu (281351) (author), Riadh Lobbardi (15104063) (author), Leonard Reyno (15013382) (author), Stewart L. Fisher (530577) (author)
منشور في:	2025
الموضوعات:	Biochemistry Genetics Pharmacology Biotechnology Cancer Science Policy Infectious Diseases Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified tumor growth inhibition promising preclinical profile modest efficacy outcomes containing protein 9 clinical trial setting chromatin factor bromodomain robust pharmacodynamic response phase 1 study selective proteasomal degradation cft8634 </ b dependent brd9 degradation pharmacodynamic observations first study dependent increases oral dosing null tumors human exposure genetic dependency cardiac toxicities anticancer effect
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Discovery of CFT8634, a Potent, Selective, and Orally Bioavailable Heterobifunctional Degrader of BRD9

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