On March 9, 2020, Yamashita, Yu; Vinogradova, Ekaterina V.; Zhang, Xiaoyu; Suciu, Radu M.; Cravatt, Benjamin F. published an article.Formula: C2H4ClNO The title of the article was A Chemical Proteomic Probe for the Mitochondrial Pyruvate Carrier Complex. And the article contained the following:
Target engagement assays are crucial for establishing the mechanism-of-action of small mols. in living systems. Integral membrane transporters can present a challenging protein class for assessing cellular engagement by small mols. The chem. proteomic discovery of alpha-chloroacetamide (αCA) compounds that covalently modify cysteine-54 (C54) of the MPC2 subunit of the mitochondrial pyruvate carrier (MPC) is presented. This finding is used to create an alkyne-modified αCA, YY4-yne, that serves as a cellular engagement probe for MPC2 in click chem.-enabled western blotting or global mass spectrometry-based proteomic experiments Studies with YY4-yne revealed that UK-5099, an alpha-cyanocinnamate inhibitor of the MPC complex, engages MPC2 with remarkable selectivity in human cells. These findings support a model where UK-5099 inhibits the MPC complex by binding to C54 of MPC2 in a covalent reversible manner that can be quantified in cells using the YY4-yne probe. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Formula: C2H4ClNO
The Article related to chem proteomic probe mitochondrial pyruvate carrier complex mcp2 uk5099, chemical proteomics, cysteine, mitochondrial pyruvate complex, target engagement, α-chloroacetamide and other aspects.Formula: C2H4ClNO
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics