Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T81358
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| Former ID |
TTDI02039
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| Target Name |
CDC7 protein kinase
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| Gene Name |
CDC7
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| Synonyms |
CDC7related kinase; Cell division cycle 7related protein kinase; HsCdc7; huCdc7; CDC7
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| Target Type |
Clinical Trial
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| Disease | Hematological malignancies [ICD9: 200-209; ICD10: C81-C86] | ||||
| Function |
Seems to phosphorylate critical substrates that regulate the G1/S phase transition and/or DNA replication. Can phosphorylates MCM2 and MCM3.
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| BioChemical Class |
Kinase
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.1
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| Sequence |
MEASLGIQMDEPMAFSPQRDRFQAEGSLKKNEQNFKLAGVKKDIEKLYEAVPQLSNVFKI
EDKIGEGTFSSVYLATAQLQVGPEEKIALKHLIPTSHPIRIAAELQCLTVAGGQDNVMGV KYCFRKNDHVVIAMPYLEHESFLDILNSLSFQEVREYMLNLFKALKRIHQFGIVHRDVKP SNFLYNRRLKKYALVDFGLAQGTHDTKIELLKFVQSEAQQERCSQNKSHIITGNKIPLSG PVPKELDQQSTTKASVKRPYTNAQIQIKQGKDGKEGSVGLSVQRSVFGERNFNIHSSISH ESPAVKLMKQSKTVDVLSRKLATKKKAISTKVMNSAVMRKTASSCPASLTCDCYATDKVC SICLSRRQQVAPRAGTPGFRAPEVLTKCPNQTTAIDMWSAGVIFLSLLSGRYPFYKASDD LTALAQIMTIRGSRETIQAAKTFGKSILCSKEVPAQDLRKLCERLRGMDSSTPKLTSDIQ GHASHQPAISEKTDHKASCLVQTPPGQYSGNSFKKGDSNSCEHCFDEYNTNLEGWNEVPD EAYDLLDKLLDLNPASRITAEEALLHPFFKDMSL |
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| Drugs and Mode of Action | |||||
| Drug(s) | BMS-863233 | Drug Info | Phase 1/2 | Hematological malignancies | [1], [2] |
| Modulator | BMS-863233 | Drug Info | [3] | ||
| PHA-767491 | Drug Info | ||||
| Inhibitor | compound 1 | Drug Info | [4] | ||
| compound 18 | Drug Info | [5] | |||
| compound 2 | Drug Info | [3] | |||
| compound 74 | Drug Info | [4] | |||
| compound 77 | Drug Info | [4] | |||
| compound 89S | Drug Info | [6] | |||
| Pathways | |||||
| NetPath Pathway | TGF_beta_Receptor Signaling Pathway | ||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT00838890) A Study of BMS-863233 in Patients With Hematologic Cancer. U.S. National Institutes of Health. | ||||
| REF 2 | (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. (Ligand id: 8113). | ||||
| REF 3 | Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. | ||||
| REF 4 | Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem. 2014 Jun 10;80:364-82. | ||||
| REF 5 | Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. J Med Chem. 2010 Oct 28;53(20):7296-315. | ||||
| REF 6 | First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307. | ||||
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