1,4‐Dihydropyridinebutyrolactone‐derived ring‐opened ester and amide analogs targeting BET bromodomains
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200288
Abstract: Based on a previously reported 1,4‐dihydropyridinebutyrolactone virtual screening hit, nine lactone ring‐opened ester and seven amide analogs were prepared. The analogs were designed to provide interactions with residues at the entrance of the ZA loop… read more here.
Keywords: bet; bet bromodomains; amide analogs; opened ester ... See more keywords
Metabolically Derived Lysine Acylations and Neighboring Modifications Tune the Binding of the BET Bromodomains to Histone H4.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemistry"
DOI: 10.1021/acs.biochem.7b00595
Abstract: Recent proteomic studies discovered histone lysines are modified by acylations beyond acetylation. These acylations derive from acyl-CoA metabolites, potentially linking metabolism to transcription. Bromodomains bind lysine acylation on histones and other nuclear proteins to influence… read more here.
Keywords: binding bet; bet bromodomains; bet; metabolically derived ... See more keywords
Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains.
Sign Up to like & getrecommendations! Published in 2019 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00414
Abstract: Fragment-based ligand discovery has been successful in targeting diverse proteins. Despite drug-like molecules having more 3D character, traditional fragment libraries are largely composed of flat, aromatic fragments. The use of 3D-enriched fragments for enhancing library… read more here.
Keywords: bet bromodomains; bet; advantages using; enriched fragments ... See more keywords