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

LCAT (P04180) - Overview - Molecular Target Synopsis

Protein


LCAT, Phosphatidylcholine-sterol acyltransferase
Enzyme Classification 2.3.1.43
UniProt P04180

Also Known as LCAT_HUMAN, LCAT

Central enzyme in the extracellular metabolism of plasma lipoproteins. Synthesized mainly in the liver and secreted into plasma where it converts cholesterol and phosphatidylcholines (lecithins) to cholesteryl esters and lysophosphatidylcholines on the surface of high and low density lipoproteins (HDLs and LDLs) (PubMed:10329423, PubMed:19065001, PubMed:26195816). The cholesterol ester is then transported back to the liver. Has a preference for plasma 16:0-18:2 or 18:O-18:2 phosphatidylcholines (PubMed:8820107). Also produced in the brain by primary astrocytes, and esterifies free cholesterol on nascent APOE-containing lipoproteins secreted from glia and influences cerebral spinal fluid (CSF) APOE- and APOA1 levels. Together with APOE and the cholesterol transporter ABCA1, plays a key role in the maturation of glial-derived, nascent lipoproteins. Required for remodeling high-density lipoprotein particles into their spherical forms (PubMed:10722751).

6MVD
CRYSTAL STRUCTURE OF LECITHIN:CHOLESTEROL ACYLTRANSFERASE (LCAT) IN COMPLEX WITH ISOPROPYL DODEC-11-ENYLFLUOROPHOSPHONATE (IDFP) AND A SMALL MOLECULE ACTIVATOR
RCSB/PDB
Inspect Structure
See all 3D Structures for LCAT

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: LCAT is active in the following subcellular-locations: secreted.
GO terms: LCAT is active in the following subcellular-locations: extracellular exosome, extracellular region, extracellular space, high-density lipoprotein particle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project LCAT has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_H522, OVCAR_8, SNB_75

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SiHa, C3A, Hep G2

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: SK-N-SH, K562, IMR-90

(see details)

3D Structures


For LCAT there are:
6 structures (15 chains) solved
6 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


LCAT has been screened with 7 compounds (7 bioactivities), 3 compounds have bioactivities that show binding affinity of <= 500nM (3 bioactivities). (see details)