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Development of a PROTAC Targeting Chk1.


ABSTRACT: A series of Chk1 degraders were designed and synthesized. The degraders were developed through the conjugation of a promiscuous kinase binder and thalidomide. One of the degraders PROTAC-2 was able to decrease Chk1 levels in a concentration-dependent manner in A375 cells. The developed probes can be useful for the development of selective and more potent Chk1 degraders.

SUBMITTER: Chowdhury SR 

PROVIDER: S-EPMC10802242 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature

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Development of a PROTAC Targeting Chk1.

Chowdhury Sandipan Roy SR   Chuong Patrick P   Mgbemena Victoria E VE   Statsyuk Alexander A  

bioRxiv : the preprint server for biology 20240101


A series of Chk1 degraders were designed and synthesized. The degraders were developed through the conjugation of a promiscuous kinase binder and thalidomide. One of the degraders PROTAC-2 was able to decrease Chk1 levels in a concentration-dependent manner in A375 cells. The developed probes can be useful for the development of selective and more potent Chk1 degraders. ...[more]

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