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

LYPLA1 (O75608) - Overview - Molecular Target Synopsis

Protein


LYPLA1, Acyl-protein thioesterase 1
Enzyme Classification 3.1.2.-
UniProt O75608

Also Known as LYPA1_HUMAN, LYPLA1, APT1, LPL1

Hydrolyzes fatty acids from S-acylated cysteine residues in proteins such as trimeric G alpha proteins or HRAS. Has depalmitoylating activity toward KCNMA1. Has low lysophospholipase activity. Homodimer.

5SYM
COCRYSTAL STRUCTURE OF THE HUMAN ACYL PROTEIN THIOESTERASE 1 WITH AN ISOFORM-SELECTIVE INHIBITOR, ML348
RCSB/PDB
Inspect Structure
See all 3D Structures for LYPLA1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: LYPLA1 is active in the following subcellular-locations: cytoplasm.
GO terms: LYPLA1 is active in the following subcellular-locations: cytoplasm, cytosol, extracellular exosome.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project LYPLA1 has gain in 7 cell-lines, loss in 4 cell-lines and no signal in 994 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_ADR_RES, LOXIMVI, CAKI_1

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: 59M, Hs 746T, Okajima

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: HMEC, NHEK, NHLF

(see details)

3D Structures


For LYPLA1 there are:
2 structures (4 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


LYPLA1 has been screened with 30 compounds (33 bioactivities), 7 compounds have bioactivities that show binding affinity of <= 500nM (8 bioactivities). (see details)