SLC27A2 ligates CoA to bempedoic acid to form ETC-1002-CoA

Stable Identifier
R-HSA-9734535
Type
Reaction [transition]
Species
Homo sapiens
Compartment
ReviewStatus
5/5
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Bempedoic acid (ETC-1002) is first-in-class ATP-citrate lyase (ACLY) inhibitor used once a day for reducing LDL cholesterol levels in statin-refractory patients. ETC-1002 itself is a prodrug, which is converted to the active metabolite ETC-1002–CoA by endogenous liver acyl-CoA synthetase (SLC27A2, ACSVL1) activity (Pinkosky et al. 2016).
Literature References
PubMed ID Title Journal Year
27892461 Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis

Steinberg, GR, Pinkosky, SL, Day, EA, Newton, RS, Smith, BK, Birch, CM, Lhotak, S, Austin, RC, Filippov, S, Lalwani, ND, Groot, PHE, Ford, RJ

Nat Commun 2016
Participants
Participates
Catalyst Activity

long-chain fatty acid-CoA ligase activity of SLC27A2 [endoplasmic reticulum membrane]

Orthologous Events
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