Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

FADS1 (O60427) - Overview - Molecular Target Synopsis

Protein


FADS1, Acyl-CoA (8-3)-desaturase
Enzyme Classification 1.14.19.44
UniProt O60427

Also Known as FADS1_HUMAN, FADS1, FADSD5

Isoform 1: Acts as a front-end fatty acyl-coenzyme A (CoA) desaturase that introduces a cis double bond at carbon 5 located between a preexisting double bond and the carboxyl end of the fatty acyl chain. Involved in biosynthesis of highly unsaturated fatty acids (HUFA) from the essential polyunsaturated fatty acids (PUFA) linoleic acid (LA) (18:2n-6) and alpha-linolenic acid (ALA) (18:3n-3) precursors. Specifically, desaturates dihomo-gamma-linoleoate (DGLA) (20:3n-6) and eicosatetraenoate (ETA) (20:4n-3) to generate arachidonate (AA) (20:4n-6) and eicosapentaenoate (EPA) (20:5n-3), respectively (PubMed:10601301, PubMed:10769175). As a rate limiting enzyme for DGLA (20:3n-6) and AA (20:4n-6)-derived eicosanoid biosynthesis, controls the metabolism of inflammatory lipids like prostaglandin E2, critical for efficient acute inflammatory response and maintenance of epithelium homeostasis. Contributes to membrane phospholipid biosynthesis by providing AA (20:4n-6) as a major acyl chain esterified into phospholipids. In particular, regulates phosphatidylinositol-4,5-bisphosphate levels, modulating inflammatory cytokine production in T-cells (By similarity). Also desaturates (11E)-octadecenoate (trans-vaccenoate)(18:1n-9), a metabolite in the biohydrogenation pathway of LA (18:2n-6)., Isoform 2: Does not exhibit any catalytic activity toward 20:3n-6, but it may enhance FADS2 activity.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: FADS1 is active in the following subcellular-locations: endoplasmic reticulum membrane, mitochondrion.
GO terms: FADS1 is active in the following subcellular-locations: endoplasmic reticulum membrane, integral component of membrane, intracellular membrane-bounded organelle, membrane, mitochondrion.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project FADS1 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 1005 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: K_562, SN12C, NCI_H460

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: H322T, A-673, EBC-1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: HeLa-S3, NHLF, K562

(see details)


Screening and Chemistry


FADS1 has been screened with 108 compounds (109 bioactivities), 22 compounds have bioactivities that show binding affinity of <= 500nM (22 bioactivities). (see details)