Target Information

Target General Infomation
Target ID
T68766
Former ID
TTDI02257
Target Name
mRNA of DMPK
Gene Name
DMPK
Synonyms
DM1 protein kinase (mRNA); DMK (mRNA); DMPK (mRNA); DMkinase (mRNA); MTPK (mRNA); Myotonic dystrophy protein kinase (mRNA); Myotoninprotein kinase (mRNA); DMPK
Target Type
Clinical Trial
Disease Myotonic dystrophy [ICD10: G71.1]
Function
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.
BioChemical Class
Target of antisense drug
UniProt ID
Q09013
EC Number
EC 2.7.11.1
Sequence
MSAEVRLRRLQQLVLDPGFLGLEPLLDLLLGVHQELGASELAQDKYVADFLQWAEPIVVR
LKEVRLQRDDFEILKVIGRGAFSEVAVVKMKQTGQVYAMKIMNKWDMLKRGEVSCFREER
DVLVNGDRRWITQLHFAFQDENYLYLVMEYYVGGDLLTLLSKFGERIPAEMARFYLAEIV
MAIDSVHRLGYVHRDIKPDNILLDRCGHIRLADFGSCLKLRADGTVRSLVAVGTPDYLSP
EILQAVGGGPGTGSYGPECDWWALGVFAYEMFYGQTPFYADSTAETYGKIVHYKEHLSLP
LVDEGVPEEARDFIQRLLCPPETRLGRGGAGDFRTHPFFFGLDWDGLRDSVPPFTPDFEG
ATDTCNFDLVEDGLTAMVSGGGETLSDIREGAPLGVHLPFVGYSYSCMALRDSEVPGPTP
MELEAEQLLEPHVQAPSLEPSVSPQDETAEVAVPAAVPAAEAEAEVTLRELQEALEEEVL
TRQSLSREMEAIRTDNQNFASQLREAEARNRDLEAHVRQLQERMELLQAEGATAVTGVPS
PRATDPPSHLDGPPAVAVGQCPLVGPGPMHRRHLLLPARVPRPGLSEALSLLLFAVVLSR
AAALGCIGLVAHAGQLTAVWRRPGAARAP
Drugs and Mode of Action
Drug(s) ISIS-DMPK Drug Info Phase 1/2 Myotonic dystrophy [525022]
Inhibitor RKI-1447 Drug Info [532172]
References
Ref 525022ClinicalTrials.gov (NCT02312011) A Safety andTolerability Study of Multiple Doses of ISIS-DMPKRx in Adults With Myotonic Dystrophy Type 1. U.S. National Institutes of Health.
Ref 532172Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm. 2012 Jun 1;3(6):699-709. Epub 2012 Jan 27.
Ref 543435(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1505).
Ref 551943Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.

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