Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T28713
|
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| Former ID |
TTDC00010
|
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| Target Name |
Serine/threonine-protein kinase Chk2
|
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| Gene Name |
CHEK2
|
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| Synonyms |
CHK2; Cds1; RAD53; CHEK2
|
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| Target Type |
Clinical Trial
|
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| Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
| Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
| BioChemical Class |
Kinase
|
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| Target Validation |
T28713
|
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.1
|
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| Sequence |
MSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTL
SSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKS CEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKR RPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFER KTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIV LELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEE DCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFIC LSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEA LRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCA AVL |
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| Drugs and Mode of Action | |||||
| Drug(s) | XL844 | Drug Info | Discontinued in Phase 1 | Solid tumours | [1] |
| Inhibitor | 2-(4-Phenoxy-phenyl)-1H-benzoimidazol-5-ylamine | Drug Info | [2] | ||
| 5-Nitro-2-(4-phenoxy-phenyl)-1H-benzoimidazole | Drug Info | [2] | |||
| CCT-241533 | Drug Info | [3] | |||
| Chk2 inhibitor II | Drug Info | [4] | |||
| compound 25b | Drug Info | [5] | |||
| DEBROMOHYMENIALDISINE | Drug Info | [6] | |||
| PV-1019 | Drug Info | [7] | |||
| Modulator | XL844 | Drug Info | [8] | ||
| 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 1 | ClinicalTrials.gov (NCT00234481) Safety Study of XL844 in Subjects With Chronic Lymphocytic Leukemia. U.S. National Institutes of Health. | ||||
| REF 2 | J Med Chem. 2005 Mar 24;48(6):1873-85.Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. | ||||
| REF 3 | CCT241533 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 4 | Proc 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 5 | Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93. | ||||
| REF 6 | Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. | ||||
| REF 7 | Cellular 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 8 | Interpreting 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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