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

DAPK2 (Q9UIK4) - Overview - Molecular Target Synopsis

Protein


DAPK2, Death-associated protein kinase 2
Enzyme Classification 2.7.11.1
UniProt Q9UIK4

Also Known as DAPK2_HUMAN, DAPK2

Calcium/calmodulin-dependent serine/threonine kinase involved in multiple cellular signaling pathways that trigger cell survival, apoptosis, and autophagy. Regulates both type I apoptotic and type II autophagic cell death signals, depending on the cellular setting. The former is caspase-dependent, while the latter is caspase-independent and is characterized by the accumulation of autophagic vesicles. Acts as a mediator of anoikis and a suppressor of beta-catenin-dependent anchorage-independent growth of malignant epithelial cells. May play a role in granulocytic maturation (PubMed:17347302). Regulates granulocytic motility by controlling cell spreading and polarization (PubMed:24163421)., Isoform 2 is not regulated by calmodulin. It can phosphorylate MYL9. It can induce membrane blebbing and autophagic cell death. Homodimer in its autoinhibited state. Active as monomer (By similarity). Isoform 2 but not isoform 1 can interact with ATF4. Interacts with 14-3-3 proteins YWHAB, YWHAE, YWHAG, YWHAH, YWHAQ, YWHAZ and SFN; the interaction requires DAPK2 phosphorylation at Thr-369 and suppresses DAPK2 kinase activity and DAPK2-induced apoptosis (PubMed:26047703).

2CKE
HUMAN DEATH-ASSOCIATED DRP-1 KINASE IN COMPLEX WITH INHIBITOR
RCSB/PDB
Inspect Structure
See all 3D Structures for DAPK2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DAPK2 is active in the following subcellular-locations: autophagosome lumen, cytoplasm, cytoplasmic vesicle.
GO terms: DAPK2 is active in the following subcellular-locations: autophagosome lumen, cytoplasm, cytoplasmic vesicle, Golgi apparatus, intracellular membrane-bounded organelle, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DAPK2 has gain in 1 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, MOLT_4, OVCAR_5

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC1482, LN-18, NCI-H1581

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, NHLF, HSMM

(see details)

RNA Interference


DAPK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: TE10, HCC1954. (see details)

3D Structures


For DAPK2 there are:
8 structures (37 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DAPK2 has been screened with 311 compounds (551 bioactivities), 10 compounds have bioactivities that show binding affinity of <= 500nM (18 bioactivities). (see details)