Target intelligence / Profile preview

Membrane-bound glycerophospholipid O-acyltransferase 1 (MBOAT1)

Target
MBOAT1
Molecular classification
Enzyme, Membrane protein, Acyltransferase, Lysophospholipid acyltransferase, Member of the membrane-bound O-acyltransferase (MBOAT) superfamily
01

Overview

Membrane-bound glycerophospholipid O-acyltransferase 1 (MBOAT1) is a multi-pass transmembrane enzyme of the membrane-bound O-acyltransferase superfamily, localized to the endoplasmic reticulum. Its primary function is to catalyze the transfer of an acyl group from acyl-CoA (preferentially oleoyl-CoA) to lysophospholipids such as lysophosphatidylethanolamine (LPE), lysophosphatidylserine (LPS), and to a lesser extent lysophosphatidylcholine (LPC), forming various phospholipids and participating in the reacylation step of the phospholipid remodeling pathway (Lands cycle). MBOAT1 also plays a role in inhibiting ferroptosis, a regulated form of cell death related to lipid peroxidation, particularly in hormone-responsive cancers and tissues. Its activity and expression are influenced by estrogen and androgen receptor signaling, making it a possible therapeutic target and biomarker for several cancers. Disruption of the MBOAT1 gene is associated with developmental disorders like brachydactyly-syndactyly syndrome. Research suggests a potential role for MBOAT1 in neurite outgrowth and neuronal differentiation. At present, there are no approved drugs directly targeting MBOAT1, but its family is actively investigated for drug development in cancer and other diseases.

Other names
Membrane-bound O-acyltransferase domain-containing protein 1MBOAT1OACT1LPSATLPLAT1LPLAT14LPEAT1Lyso-PS acyltransferaseLysophosphatidylethanolamine acyltransferase 11-acylglycerophosphocholine O-acyltransferase1-acylglycerophosphoethanolamine O-acyltransferase1-acylglycerophosphoserine O-acyltransferaseLysophosphatidylserine acyltransferaseLysophospholipid acyltransferase 1Lysophospholipid acyltransferase 14MGC44669dJ434O11.1
02

Mechanism of action

Small molecule inhibition of acyltransferase activity (reduction of phospholipid remodeling; theoretical for therapeutic development). Sensitization to ferroptosis via hormone receptor antagonists that downregulate MBOAT1 expression.

03

Biological functions

Phospholipid remodeling (Lands cycle)Acyl group transfer from acyl-CoA to lysophospholipidsNeuronal differentiation (neurite outgrowth)Regulation of ferroptosis
04

Disease associations

Cancer (breast, prostate, ovarian, endometrial)Brachydactyly-syndactyly syndromeOther fertility and neurodevelopmental diseases (based on expression and functional studies)
05

Safety considerations

Enzyme is expressed in multiple cell types, including neurons and reproductive organs, so off-target effects are possible if systemically inhibitedPotential neurodevelopmental side effects due to role in neuronal differentiationPossible impact on fertility, given sex-hormone regulation
06

Interacting drugs

Androgen receptor (AR) antagonists

2 more in the full profile.

07

Biomarkers

MBOAT1 gene/protein expression levels (potential biomarker for breast, ovarian, endometrial and prostate cancer sensitivity to ferroptosis inducers or hormone therapies)Lysophospholipid composition in cellular membranes (reflects enzymatic activity; research stage)

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