Target Information

Target General Infomation
Target ID
T36959
Former ID
TTDC00338
Target Name
Activin receptor-like kinase-1
Gene Name
ACVRL1
Synonyms
ACVRLK1; ALK-1; Activin receptor-like kinase 1; SKR3; Serine/threonine-protein kinase receptor R3; TGF-B superfamily receptor type I; TSR-I; ACVRL1
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Type I receptor for TGF-beta family ligands BMP9/GDF2 and BMP10 and important regulator of normal blood vessel development. On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. May bindactivin as well.
BioChemical Class
Kinase
UniProt ID
P37023
EC Number
EC 2.7.11.30
Sequence
MTLGSPRKGLLMLLMALVTQGDPVKPSRGPLVTCTCESPHCKGPTCRGAWCTVVLVREEG
RHPQEHRGCGNLHRELCRGRPTEFVNHYCCDSHLCNHNVSLVLEATQPPSEQPGTDGQLA
LILGPVLALLALVALGVLGLWHVRRRQEKQRGLHSELGESSLILKASEQGDSMLGDLLDS
DCTTGSGSGLPFLVQRTVARQVALVECVGKGRYGEVWRGLWHGESVAVKIFSSRDEQSWF
RETEIYNTVLLRHDNILGFIASDMTSRNSSTQLWLITHYHEHGSLYDFLQRQTLEPHLAL
RLAVSAACGLAHLHVEIFGTQGKPAIAHRDFKSRNVLVKSNLQCCIADLGLAVMHSQGSD
YLDIGNNPRVGTKRYMAPEVLDEQIRTDCFESYKWTDIWAFGLVLWEIARRTIVNGIVED
YRPPFYDVVPNDPSFEDMKKVVCVDQQTPTIPNRLAADPVLSGLAQMMRECWYPNPSARL
TALRIKKTLQKISNSPEKPKVIQ
Drugs and Mode of Action
Drug(s) PF-03446962 Drug Info Phase 2 Cancer [523946]
Inhibitor compound 13a Drug Info [532338]
compound 13d Drug Info [532338]
compound 13r Drug Info [532338]
LDN-214117 Drug Info [532914]
ML347 Drug Info [532338]
Modulator PF-03446962 Drug Info [544182]
Pathways
PANTHER Pathway TGF-beta signaling pathway
Pathway Interaction Database ALK1 pathway
ALK1 signaling events
References
Ref 523946ClinicalTrials.gov (NCT01620970) PF-03446962 in Relapsed or Refractory Urothelial Cancer. U.S. National Institutes of Health.
Ref 532338Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.
Ref 532914Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15.
Ref 544182ALK1 as an emerging target for antiangiogenic therapy of cancer. Blood. 2011 June 30; 117(26): 6999-7006.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.