DS16570511 is a small-molecule inhibitor of the mitochondrial calcium uniporter.

ABSTRACT: In cardiac myocytes, regulation of mitochondrial Ca²⁺ is important for cellular signaling and cardiac contraction. Ca²⁺ entry into the mitochondria is mediated by a highly selective Ca²⁺ channel called the mitochondrial calcium uniporter, which consists of a pore-forming subunit MCU and regulatory subunits such as MICU1. Although pharmacological regulation of the mitochondrial Ca²⁺ influx is a promising approach to controlling the cellular functions, a cell-permeable and specific inhibitor of the mitochondrial calcium uniporter has not yet been developed. Here, we identify a novel cell-permeable inhibitor of the uniporter by a high-throughput screening of 120 000 small-molecule compounds. In our study, DS16570511 dose-dependently inhibited serum-

SUBMITTER: Kon N 

PROVIDER: S-EPMC5511861 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature