Target intelligence / Profile preview

Membrane-bound ghrelin O-acyltransferase (MBOAT4)

Target
MBOAT4
Molecular classification
Enzyme, Acyltransferase, Membrane enzyme
01

Overview

Membrane-bound ghrelin O-acyltransferase (MBOAT4, also known as GOAT) is an integral membrane enzyme primarily located in the endoplasmic reticulum that catalyzes the acylation of ghrelin at serine 3, using medium-chain acyl-CoA donors—most commonly octanoyl-CoA—which is essential for the biological activity of ghrelin, a peptide hormone involved in appetite regulation, energy homeostasis, and body weight control[1][5][6]. MBOAT4 belongs to the membrane-bound O-acyltransferase (MBOAT) family and plays a critical role in peptide hormone metabolism and post-translational modification[1][2][6]. Genetic and pharmacological inhibition of MBOAT4 has been investigated as a potential therapeutic approach for obesity and metabolic disorders, although no approved drugs directly targeting MBOAT4 are currently available[1][2]. Inhibition or dysfunction of this enzyme may affect metabolic balance and appetite, thus representing both a therapeutic opportunity and a safety concern in metabolism-related diseases[1][5].

Other names
Ghrelin O-acyltransferaseGOATO-acyltransferase domain-containing protein 4OACT4FKSG89
02

Mechanism of action

Enzyme inhibition (inhibitors prevent ghrelin acylation); Modulation of ghrelin signaling via post-translational modification

03

Biological functions

Peptidyl-serine octanoylationGhrelin acylationPeptide hormone metabolismPost-translational modification (hormone activation)
04

Disease associations

Obesity (by modulating body mass index)Metabolic diseaseLeptin deficiency or dysfunctionEnergy balance disorders
05

Safety considerations

Impaired ghrelin signaling (potential effects on appetite, metabolism, growth hormone release if excessively inhibited)Risk of metabolic derangements due to chronic inhibition
06

Interacting drugs

No approved drugs; several investigational small molecule inhibitors are described in the literature, but none are clinically approved as of 2025
07

Biomarkers

Acylated ghrelin levels (used as a proxy for enzyme activity)Body mass index in the context of pathway modulation

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