Target intelligence / Profile preview

Mitochondrial calcium uniporter (MCU) (MCU)

Target
MCU
Molecular classification
Ion channel, Transporter
01

Overview

Mitochondrial calcium uniporter (MCU) is a highly selective calcium-conducting channel located in the inner mitochondrial membrane, responsible for the primary pathway of calcium entry into the mitochondrial matrix (UniProt Q9BPX6). It functions as part of a large protein complex that includes regulatory subunits such as MICU1, MICU2, and EMRE to maintain calcium homeostasis (PMID: 21666605). By regulating mitochondrial calcium levels, MCU plays a critical role in modulating aerobic metabolism, ATP production, and cell death pathways such as apoptosis and necrosis (PMID: 30104731). Dysregulation of MCU-mediated calcium uptake is implicated in various pathologies, including myocardial infarction, where calcium overload leads to tissue damage, and neurodegenerative diseases like Alzheimer's and Parkinson's (PMID: 31434801). In cancer, MCU expression often correlates with tumor progression and chemoresistance by influencing metabolic reprogramming and survival signaling (PMID: 30610213). While several small molecules like Ru360 and DS16570511 have been developed to inhibit MCU activity in research settings, therapeutic targeting remains challenging due to the channel's essential role in systemic energy homeostasis (PMID: 32561583).

Other names
CCDC109ACoiled-coil domain-containing protein 109AMitochondrial calcium uniporter proteinMCU mRNA
02

Mechanism of action

Inhibition or activation of mitochondrial calcium uptake through the inner mitochondrial membrane.

03

Biological functions

Mitochondrial calcium homeostasisATP synthesisApoptosisSignal transductionMetabolic regulation
04

Disease associations

Cardiovascular diseaseNeurodegenerative diseaseCancerIschemia-reperfusion injuryMetabolic disorder
05

Safety considerations

Disruption of cellular energy metabolismPotential for cardiac dysfunctionSystemic toxicity due to ubiquitous expressionImpairment of calcium-dependent signaling
06

Interacting drugs

Ru360

4 more in the full profile.

07

Biomarkers

Mitochondrial calcium concentrationMitochondrial membrane potentialReactive oxygen species (ROS) levels

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