On January 11, 2021, Wiktelius, Daniel; Allgardsson, Anders; Bergstroem, Tomas; Hoster, Norman; Akfur, Christine; Forsgren, Nina; Lejon, Christian; Hedenstroem, Mattias; Linusson, Anna; Ekstroem, Fredrik published an article.Product Details of 79-07-2 The title of the article was In Situ Assembly of Choline Acetyltransferase Ligands by a Hydrothiolation Reaction Reveals Key Determinants for Inhibitor Design. And the article contained the following:
The potential drug target choline acetyltransferase (ChAT) catalyzes the production of the neurotransmitter acetylcholine in cholinergic neurons, T-cells, and B-cells. Herein, we show that arylvinylpyridiniums (AVPs), the most widely studied class of ChAT inhibitors, act as substrate in an unusual CoA-dependent hydrothiolation reaction. This in situ synthesis yields an adduct that is the actual enzyme inhibitor. The adduct is deeply buried in the active site tunnel of ChAT and interactions with a hydrophobic pocket near the choline binding site have major implications for the mol. recognition of inhibitors. Our findings clarify the inhibition mechanism of AVPs, establish a drug modality that exploits a target-catalyzed reaction between exogenous and endogenous precursors, and provide new directions for the development of ChAT inhibitors with improved potency and bioactivity. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Product Details of 79-07-2
The Article related to arylvinylpyridinium choline acetyltransferase inhibitor hydrothiolation, choline acetyltransferase, coenzyme a, drug discovery, hydrothiolation, in situ assembly, Placeholder for records without volume info and other aspects.Product Details of 79-07-2
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics