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

DMPK (Q09013) - Overview - Molecular Target Synopsis

Protein


DMPK, Myotonin-protein kinase
Enzyme Classification 2.7.11.1
UniProt Q09013

Also Known as DMPK_HUMAN, DMPK, DM1PK, MDPK

Non-receptor serine/threonine protein kinase which is necessary for the maintenance of skeletal muscle structure and function. May play a role in myocyte differentiation and survival by regulating the integrity of the nuclear envelope and the expression of muscle-specific genes. May also phosphorylate PPP1R12A and inhibit the myosin phosphatase activity to regulate myosin phosphorylation. Also critical to the modulation of cardiac contractility and to the maintenance of proper cardiac conduction activity probably through the regulation of cellular calcium homeostasis. Phosphorylates PLN, a regulator of calcium pumps and may regulate sarcoplasmic reticulum calcium uptake in myocytes. May also phosphorylate FXYD1/PLM which is able to induce chloride currents. May also play a role in synaptic plasticity. Homodimer; homodimerization stimulates the kinase activity. Interacts with HSPB2; may enhance DMPK kinase activity. Interacts with PLN; phosphorylates PLN. May interact with RAC1; may regulate DMPK kinase activity. Interacts with LMNA; may regulate nuclear envelope stability.

2VD5
STRUCTURE OF HUMAN MYOTONIC DYSTROPHY PROTEIN KINASE IN COMPLEX WITH THE BISINDOYLMALEIDE INHIBITOR BIM VIII
RCSB/PDB
Inspect Structure
See all 3D Structures for DMPK

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: DMPK is active in the following subcellular-locations: cell membrane, cytoplasm, cytosol, endoplasmic reticulum membrane, mitochondrion membrane, mitochondrion outer membrane, nucleus outer membrane, sarcoplasmic reticulum membrane.
GO terms: DMPK is active in the following subcellular-locations: cytosol, endoplasmic reticulum membrane, integral component of mitochondrial outer membrane, nuclear membrane, nuclear outer membrane, plasma membrane, sarcoplasmic reticulum membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DMPK has gain in 4 cell-lines, loss in 0 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_539, HOP_62, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DMS 53, SJCRH30, Hs 255.T

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, HSMM, BJ

(see details)

RNA Interference


DMPK was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: COV504, SKGT4. (see details)

3D Structures


For DMPK there are:
2 structures (5 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DMPK has been screened with 408 compounds (692 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (11 bioactivities). (see details)