Target General Infomation
Target ID
T46685
Former ID
TTDI00245
Target Name
Cdc2-like kinase 1
Gene Name
CLK1
Synonyms
CDClike kinase 1; Dual specificity protein kinase CLK1; CLK1
Target Type
Research
Function
Dual specificity kinase acting on both serine/threonine andtyrosine-containing substrates. Phosphorylates serine- and arginine-rich (SR) proteins of the spliceosomal complex and may be a constituent of a network of regulatory mechanisms that enable SR proteins to control RNA splicing. Phosphorylates: SRSF1, SRSF3 and PTPN1. Regulates the alternative splicing of tissue factor (F3) pre-mRNA in endothelial cells and adenovirus E1A pre-mRNA.
BioChemical Class
Kinase
UniProt ID
EC Number
EC 2.7.12.1
Sequence
MRHSKRTYCPDWDDKDWDYGKWRSSSSHKRRKRSHSSAQENKRCKYNHSKMCDSHYLESR
SINEKDYHSRRYIDEYRNDYTQGCEPGHRQRDHESRYQNHSSKSSGRSGRSSYKSKHRIH
HSTSHRRSHGKSHRRKRTRSVEDDEEGHLICQSGDVLSARYEIVDTLGEGAFGKVVECID
HKAGGRHVAVKIVKNVDRYCEAARSEIQVLEHLNTTDPNSTFRCVQMLEWFEHHGHICIV
FELLGLSTYDFIKENGFLPFRLDHIRKMAYQICKSVNFLHSNKLTHTDLKPENILFVQSD
YTEAYNPKIKRDERTLINPDIKVVDFGSATYDDEHHSTLVSTRHYRAPEVILALGWSQPC
DVWSIGCILIEYYLGFTVFPTHDSKEHLAMMERILGPLPKHMIQKTRKRKYFHHDRLDWD
EHSSAGRYVSRRCKPLKEFMLSQDVEHERLFDLIQKMLEYDPAKRITLREALKHPFFDLL
KKSI
Inhibitor compound 17 Drug Info [532342]
compound 2 Drug Info [531356]
compound 3b Drug Info [532250]
KH-CB19 Drug Info [531348]
leucettine L41 Drug Info [531493]
ML315 Drug Info [532342]
TG003 Drug Info [529213]
Pathways
NetPath Pathway TCR Signaling Pathway
EGFR1 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
WikiPathways mRNA Processing
References
Ref 529213Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Ref 531348Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol. 2011 Jan 28;18(1):67-76.
Ref 5313566-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3beta inhibitors. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1429-33.
Ref 531493Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem. 2011 Jun 23;54(12):4172-86.
Ref 532250Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines. Eur J Med Chem. 2013 Apr;62:728-37.
Ref 532342Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg Med Chem Lett. 2013 Jun15;23(12):3654-61.

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