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Ghrelin O-acyltransferase (GOAT)
- Target
- GOAT
- Molecular classification
- Enzyme, Acyltransferase, Membrane-bound enzyme
01
Overview
Ghrelin O-acyltransferase (GOAT) is an enzyme responsible for the post-translational modification of ghrelin, a peptide hormone involved in regulating appetite, metabolism, and energy balance. GOAT catalyzes the attachment of an acyl group to the serine residue at position 3 of proghrelin, converting it into its active form. This acylation is essential for ghrelin to bind and activate its receptor, growth hormone secretagogue receptor type 1a (GHSR1a). Inhibiting GOAT has been proposed as a therapeutic strategy for obesity and diabetes mellitus.
- Other names
- MBOAT4Membrane-bound O-acyltransferase domain-containing protein 4
02
Mechanism of action
Inhibition of GOAT prevents ghrelin acylation, thus blocking the activation of GHSR1a and reducing appetite and improving glucose control.
03
Biological functions
Ghrelin acylationRegulation of appetiteRegulation of metabolismRegulation of growth hormone releaseRegulation of glucose homeostasisLipid modification
04
Disease associations
ObesityDiabetes mellitusMetabolic disordersHypoglycemia
05
Safety considerations
Potential for disrupting energy balanceHypoglycemia riskOff-target effects of inhibitors
06
Interacting drugs
GOAT inhibitors (synthetic)
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