Recommended Tool Compounds: Thienotriazolodiazepines-Derivatized Chemical Probes to Target BET Bromodomains DOI Creative Commons
Chuhui Huang, Claire L. Harris, Ghizal Siddiqui

et al.

ACS Pharmacology & Translational Science, Journal Year: 2025, Volume and Issue: 8(4), P. 978 - 1012

Published: March 14, 2025

Thienotriazolodiazepines, including (+)-JQ1 (4), are well-known inhibitors of the bromodomain (BD) and extra-terminal domain (BET) family proteins. Despite suboptimal physicochemical properties as a drug candidate, such poor solubility half-life, (4) has proven an effective chemical probe with high target potency selectivity. (+)-JQ1-derived probes have played vital role in biology discovery over past decade, which is demonstrated by number impactful research studies published since disclosure 2010. In this review, we discuss development (+)-JQ1-derivatized decade their significant contribution to scientific research. Specifically, will summarize innovative label-free labeled probes, bivalent, covalent, photoaffinity well protein degraders, focus on design these probes.

Language: Английский

Discovery of novel JQ1 derivatives as dual ferroptosis and apoptosis inducers for the treatment of triple-negative breast cancer DOI
Ran Ding, Lijie Tang, Daniel Zeng

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 286, P. 117275 - 117275

Published: Jan. 11, 2025

Language: Английский

Citations

0
Recommended Tool Compounds: Thienotriazolodiazepines-Derivatized Chemical Probes to Target BET Bromodomains DOI Creative Commons
Chuhui Huang, Claire L. Harris, Ghizal Siddiqui

et al.

ACS Pharmacology & Translational Science, Journal Year: 2025, Volume and Issue: 8(4), P. 978 - 1012

Published: March 14, 2025

Thienotriazolodiazepines, including (+)-JQ1 (4), are well-known inhibitors of the bromodomain (BD) and extra-terminal domain (BET) family proteins. Despite suboptimal physicochemical properties as a drug candidate, such poor solubility half-life, (4) has proven an effective chemical probe with high target potency selectivity. (+)-JQ1-derived probes have played vital role in biology discovery over past decade, which is demonstrated by number impactful research studies published since disclosure 2010. In this review, we discuss development (+)-JQ1-derivatized decade their significant contribution to scientific research. Specifically, will summarize innovative label-free labeled probes, bivalent, covalent, photoaffinity well protein degraders, focus on design these probes.

Language: Английский

Citations

0