Target Information

Target General Infomation
Target ID
T28713
Former ID
TTDC00010
Target Name
Serine/threonine-protein kinase Chk2
Gene Name
CHEK2
Synonyms
CHK2; Cds1; RAD53; CHEK2
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
BioChemical Class
Kinase
Target Validation
T28713
UniProt ID
O96017
EC Number
EC 2.7.11.1
Sequence
MSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTL
SSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKS
CEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKR
RPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFER
KTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIV
LELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEE
DCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFIC
LSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEA
LRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCA
AVL
Drugs and Mode of Action
Drug(s) XL844 Drug Info Discontinued in Phase 1 Solid tumours [521743]
Inhibitor 2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine Drug Info [527477]
5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole Drug Info [527477]
CCT-241533 Drug Info [525351]
Chk2 inhibitor II Drug Info [529213]
compound 25b Drug Info [531897]
DEBROMOHYMENIALDISINE Drug Info [527140]
PV-1019 Drug Info [525367]
Modulator XL844 Drug Info [1572591]
Pathways
KEGG Pathway Cell cycle
p53 signaling pathway
HTLV-I infection
Pathway Interaction Database ATM pathway
FOXM1 transcription factor network
p53 pathway
PLK3 signaling events
Reactome Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks
G2/M DNA damage checkpoint
Ubiquitin Mediated Degradation of Phosphorylated Cdc25A
WikiPathways DNA Damage Response
ATM Signaling Pathway
Integrated Pancreatic Cancer Pathway
Prostate Cancer
Integrated Breast Cancer Pathway
Integrated Cancer pathway
Cell Cycle
miRNA Regulation of DNA Damage Response
References
Ref 521743ClinicalTrials.gov (NCT00234481) Safety Study of XL844 in Subjects With Chronic Lymphocytic Leukemia. U.S. National Institutes of Health.
Ref
Ref 525351CCT241533 Is a Potent and Selective Inhibitor of CHK2 that Potentiates the Cytotoxicity of PARP Inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72.
Ref 525367Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinohydrazone)-ethyl]-phenyl}-amide]. J Pharmacol Exp Ther. 2009 Dec;331(3):816-26.
Ref 527140Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
Ref 527477J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.
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 531897Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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