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

CASP3 (P42574) - Overview - Molecular Target Synopsis

Protein


CASP3, Caspase-3
Enzyme Classification 3.4.22.56
UniProt P42574

Also Known as CASP3_HUMAN, CASP3, CPP32

Involved in the activation cascade of caspases responsible for apoptosis execution. At the onset of apoptosis it proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp-|-Gly-217' bond. Cleaves and activates sterol regulatory element binding proteins (SREBPs) between the basic helix-loop-helix leucine zipper domain and the membrane attachment domain. Cleaves and activates caspase-6, -7 and -9. Involved in the cleavage of huntingtin. Triggers cell adhesion in sympathetic neurons through RET cleavage. Heterotetramer that consists of two anti-parallel arranged heterodimers, each one formed by a 17 kDa (p17) and a 12 kDa (p12) subunit. Interacts with BIRC6/bruce.

6CKZ
HUMAN CASPASE-3 IN COMPLEX WITH AC-DW3-KE
RCSB/PDB
Inspect Structure
See all 3D Structures for CASP3

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
277ENSG00000164305ENST00000308394, ENST00000523916ENSP00000311032, ENSP00000428929P42574-1
123ENSG00000164305ENST00000447121ENSP00000407142

Sub-cellular localization


UniProt: CASP3 is active in the following subcellular-locations: cytoplasm.
GO terms: CASP3 is active in the following subcellular-locations: cytoplasm, cytosol, death-inducing signaling complex, membrane raft, neuronal cell body, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CASP3 has gain in 0 cell-lines, loss in 11 cell-lines and no signal in 994 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, NCI_H226, CCRF_CEM

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MOLP-2, SK-N-FI, Hs 746T

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: NHLF, SK-N-SH, HSMM

(see details)

3D Structures


For CASP3 there are:
116 structures (259 chains) solved
21 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CASP3 has been screened with 1683 compounds (2526 bioactivities), 702 compounds have bioactivities that show binding affinity of <= 500nM (1124 bioactivities). (see details)