Ontology highlight
ABSTRACT:
SUBMITTER: Tso SC
PROVIDER: S-EPMC4110271 | biostudies-literature | 2014 Jul
REPOSITORIES: biostudies-literature
Tso Shih-Chia SC Gui Wen-Jun WJ Wu Cheng-Yang CY Chuang Jacinta L JL Qi Xiangbing X Skvora Kristen J KJ Dork Kenneth K Wallace Amy L AL Morlock Lorraine K LK Lee Brendan H BH Hutson Susan M SM Strom Stephen C SC Williams Noelle S NS Tambar Uttam K UK Wynn R Max RM Chuang David T DT
The Journal of biological chemistry 20140701 30
The mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC) is negatively regulated by reversible phosphorylation.BCKDC kinase (BDK) inhibitors that augment BCKDC flux have been shown to reduce branched-chain amino acid (BCAA) concentrations in vivo. In the present study, we employed high-throughput screens to identify compound 3,6- dichlorobenzo[b]thiophene-2-carboxylic acid (BT2) as a novel BDK inhibitor (IC(50) = 3.19 μM). BT2 binds to the same site in BDK as other known alloste ...[more]