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mitochondrial pyruvate carrier 2

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Target id: 3023

Nomenclature: mitochondrial pyruvate carrier 2

Systematic Nomenclature: SLC54A2

Family: SLC54 Mitochondrial pyruvate carriers

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 3 127 1q24.2 MPC2 mitochondrial pyruvate carrier 2 1,4
Mouse 3 127 1 H2.2 Mpc2 mitochondrial pyruvate carrier 2 1,4
Rat 3 127 13q23 Mpc2 mitochondrial pyruvate carrier 2
Previous and Unofficial Names Click here for help
brain protein 44 | BRP44 | solute carrier family 54 member 2 | SLC54A2
Database Links Click here for help
Specialist databases
Bioparadigms SLC Tables SLC54A2 (Hs)
RESOLUTE MPC2 (Hs)
Other databases
Alphafold O95563 (Hs), Q9D023 (Mm), P38718 (Rn)
ChEMBL Target CHEMBL4295686 (Hs)
Ensembl Gene ENSG00000143158 (Hs), ENSMUSG00000026568 (Mm), ENSRNOG00000003150 (Rn)
Entrez Gene 25874 (Hs), 70456 (Mm), 100359982 (Rn)
Human Protein Atlas ENSG00000143158 (Hs)
KEGG Gene hsa:25874 (Hs), mmu:70456 (Mm), rno:100359982 (Rn)
OMIM 614737 (Hs)
Pharos O95563 (Hs)
UniProtKB O95563 (Hs), Q9D023 (Mm), P38718 (Rn)
Wikipedia MPC2 (Hs)
Substrates and Reaction Kinetics Click here for help
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
Pyruvate N/A - - 1,4

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
UK-5099 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Inhibition 7.3 pIC50 3
⤷ pIC50 7.3 (IC50 5x10-8 M) [3]
α-cyanocinnamate Small molecule or natural product Click here for species-specific activity table Rn Inhibition 6.7 pIC50 3
⤷ pIC50 6.7 (IC50 2x10-7 M) [3]
α-Cyano-5-phenyl-2,4-pentadienic acid Small molecule or natural product Click here for species-specific activity table Rn Inhibition 6.7 pIC50 3
⤷ pIC50 6.7 (IC50 2x10-7 M) [3]
zaprinast Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.5 pIC50 6
⤷ pIC50 6.5 (IC50 3x10-7 M) [6]
entacapone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 6
⤷ pIC50 6.2 (IC50 6x10-7 M) [6]
mitoglitazone Small molecule or natural product Click here for species-specific activity table Mm Inhibition 5.9 pIC50 2
⤷ pIC50 5.9 (IC50 1.3x10-6 M) [2]
α-cyano-4-hydroxycinnamate Small molecule or natural product Click here for species-specific activity table Rn Inhibition 5.8 pIC50 3
⤷ pIC50 5.8 (IC50 1.5x10-6 M) [3]
lonidamine Small molecule or natural product Rn Inhibition 5.6 pIC50 5
⤷ pIC50 5.6 (IC50 2.5x10-6 M) [5]
nitrofurantoin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.5 pIC50 6
⤷ pIC50 5.5 (IC50 3.3x10-6 M) [6]
lonidamine Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.3 pIC50 6
⤷ pIC50 5.3 (IC50 4.6x10-6 M) [6]
View species-specific inhibitor tables
Antagonist Comments
The inhibitory potency of UK5099 in human MPC1L/MPC2 proteoliposomes is 53 nM [6]. The potency of mitoglitazone (MSDC-0160) in the same system is 2.7 μM [6].
General Comments
MPC2 forms an ~150kDa oligomeric complex with MPC1. This protein complex (the mitochondrial pyruvate carrier) is involved in the transport of pyruvate across the inner membrane of mitochondria, into the mitochondrial matrix for oxidative phosphorylation

References

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1. Bricker DK, Taylor EB, Schell JC, Orsak T, Boutron A, Chen YC, Cox JE, Cardon CM, Van Vranken JG, Dephoure N et al.. (2012) A mitochondrial pyruvate carrier required for pyruvate uptake in yeast, Drosophila, and humans. Science, 337 (6090): 96-100. [PMID:22628558]

2. Divakaruni AS, Wiley SE, Rogers GW, Andreyev AY, Petrosyan S, Loviscach M, Wall EA, Yadava N, Heuck AP, Ferrick DA et al.. (2013) Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier. Proc Natl Acad Sci U S A, 110 (14): 5422-7. [PMID:23513224]

3. Halestrap AP. (1975) The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J, 148 (1): 85-96. [PMID:1156402]

4. Herzig S, Raemy E, Montessuit S, Veuthey JL, Zamboni N, Westermann B, Kunji ER, Martinou JC. (2012) Identification and functional expression of the mitochondrial pyruvate carrier. Science, 337 (6090): 93-6. [PMID:22628554]

5. Nancolas B, Guo L, Zhou R, Nath K, Nelson DS, Leeper DB, Blair IA, Glickson JD, Halestrap AP. (2016) The anti-tumour agent lonidamine is a potent inhibitor of the mitochondrial pyruvate carrier and plasma membrane monocarboxylate transporters. Biochem J, 473 (7): 929-36. [PMID:26831515]

6. Tavoulari S, Schirris TJJ, Mavridou V, Thangaratnarajah C, King MS, Jones DTD, Ding S, Fearnley IM, Kunji ERS. (2022) Key features of inhibitor binding to the human mitochondrial pyruvate carrier hetero-dimer. Mol Metab, 60: 101469. [PMID:35278701]

Contributors

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