WebNov 13, 2024 · Background: CC-90009 is a cereblon (CRBN) E3 ligase modulator (CELMoD) and a first-in-class small molecule that drives the binding of a novel target protein, G1 to S phase transition 1 (GSPT1), to CRBN, resulting in the proteasome-dependent degradation of GSPT1. GSPT1 plays a central role in mRNA translation, and … WebThese antibodies target GSPT1 in Human, Mouse and Rat samples. Our GSPT1 polyclonal antibodies are developed in Rabbit. These antibodies have been verified by Knockdown …
JCI - Degradation of GSPT1 causes TP53-independent cell death in ...
WebDec 1, 2024 · Recently, the CRBN E3 ligase modulator, CC90009 was reported to show potent antitumor activity in acute myeloid leukemia, leading to the identification of GSPT1 (G1 to S phase transition factor) as a CRBN neosubstrate. These findings suggest the potential of MGs to target unanticipated vulnerabilities in different malignancies. WebSep 16, 2024 · Ishoey, M. et al. Translation termination factor GSPT1 is a phenotypically relevant off-target of heterobifunctional phthalimide degraders. ACS Chem. Biol. 13 , 553–560 (2024). Article CAS ... michael fennelly touch my soul
An update on CC-885 is long overdue - InvestorVillage
Web4 Disease Target Structure Research Center, ... Compound 34f effectively induced GSPT1 degradation with a DC 50 of 0.269 nM and Dmax of >95 % at 10 nM concentration in KG-1 cells. An in vivo xenograft study showed that compound 34f effectively suppressed TMD8-driven tumor growth, suggesting a potential role in the development of novel GSPT1 ... WebAug 15, 2024 · Drugs that degrade GSPT1 via the CRL4CRBN ubiquitin ligase are a new class of cancer therapy in active clinical development with evidence of activity against … WebFeb 5, 2024 · Off-target effects can also arise from the binary engagement of the target binding ligand of the PROTAC to other proteins in the same way as the POI. ... (IKZF1 … michael fenn pinsent masons