Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T28484
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| Former ID |
TTDC00143
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| Target Name |
Kinesin-like protein KIF11
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| Gene Name |
KIF11
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| Synonyms |
Eg5; Kinesin-like protein 1; Kinesin-like spindle protein HKSP; Kinesin-related motor protein Eg5; TRIP5; Thyroid receptor interacting protein 5; KIF11
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| Target Type |
Clinical Trial
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| Disease | Acute myeloid leukemia [ICD9: 205; ICD10: C92.0] | ||||
| Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
| Head and neck cancer; Renal cell carcinoma; Ovarian cancer; Solid tumors [ICD9: 140-149, 140-199, 140-229, 183, 189, 210-229; ICD10: C07-C14, C32-C33, C56, C64, D10-D36, D3A] | |||||
| Hematological malignancies [ICD9: 200-209; ICD10: C81-C86] | |||||
| Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86] | |||||
| Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
| Function |
Motor protein required for establishing a bipolar spindle. Blocking of KIF11 prevents centrosome migration and arrest cells in mitosis with monoastral microtubule arrays.
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| BioChemical Class |
Kinesin-like protein family
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| Target Validation |
T28484
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| UniProt ID | |||||
| Sequence |
MASQPNSSAKKKEEKGKNIQVVVRCRPFNLAERKASAHSIVECDPVRKEVSVRTGGLADK
SSRKTYTFDMVFGASTKQIDVYRSVVCPILDEVIMGYNCTIFAYGQTGTGKTFTMEGERS PNEEYTWEEDPLAGIIPRTLHQIFEKLTDNGTEFSVKVSLLEIYNEELFDLLNPSSDVSE RLQMFDDPRNKRGVIIKGLEEITVHNKDEVYQILEKGAAKRTTAATLMNAYSSRSHSVFS VTIHMKETTIDGEELVKIGKLNLVDLAGSENIGRSGAVDKRAREAGNINQSLLTLGRVIT ALVERTPHVPYRESKLTRILQDSLGGRTRTSIIATISPASLNLEETLSTLEYAHRAKNIL NKPEVNQKLTKKALIKEYTEEIERLKRDLAAAREKNGVYISEENFRVMSGKLTVQEEQIV ELIEKIGAVEEELNRVTELFMDNKNELDQCKSDLQNKTQELETTQKHLQETKLQLVKEEY ITSALESTEEKLHDAASKLLNTVEETTKDVSGLHSKLDRKKAVDQHNAEAQDIFGKNLNS LFNNMEELIKDGSSKQKAMLEVHKTLFGNLLSSSVSALDTITTVALGSLTSIPENVSTHV SQIFNMILKEQSLAAESKTVLQELINVLKTDLLSSLEMILSPTVVSILKINSQLKHIFKT SLTVADKIEDQKKELDGFLSILCNNLHELQENTICSLVESQKQCGNLTEDLKTIKQTHSQ ELCKLMNLWTERFCALEEKCENIQKPLSSVQENIQQKSKDIVNKMTFHSQKFCADSDGFS QELRNFNQEGTKLVEESVKHSDKLNGNLEKISQETEQRCESLNTRTVYFSEQWVSSLNER EQELHNLLEVVSQCCEASSSDITEKSDGRKAAHEKQHNIFLDQMTIDEDKLIAQNLELNE TIKIGLTKLNCFLEQDLKLDIPTGTTPQRKSYLYPSTLVRTEPREHLLDQLKRKQPELLM MLNCSENNKEETIPDVDVEEAVLGQYTEEPLSQEPSVDAGVDCSSIGGVPFFQHKKSHGK DKENRGINTLERSKVEETTEHLVTKSRLPLRAQINL |
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| Structure |
1II6; 1Q0B; 1X88; 1YRS; 2FKY; 2FL2; 2FL6; 2FME; 2G1Q; 2GM1; 2IEH; 2PG2; 2Q2Y; 2Q2Z; 2UYI; 2UYM; 2WOG; 2X2R; 2X7C; 2X7D; 2X7E; 2XAE; 3CJO; 3HQD; 3K3B; 3K5E; 3KEN; 3L9H; 3ZCW; 4A1Z; 4A28; 4A50; 4A51; 4A5Y; 4AP0; 4AQV; 4AQW; 4AS7; 4B7B; 4BBG; 4BXN; 4CK5; 4CK6; 4CK7; 1II6; 1Q0B; 1X88; 1YRS; 2FKY; 2FL2; 2FL6; 2FME; 2G1Q; 2GM1; 2IEH; 2PG2; 2Q2Y; 2Q2Z; 2UYI; 2UYM; 2WOG; 2X2R; 2X7C; 2X7D; 2X7E; 2XAE; 3CJO; 3HQD; 3K3B; 3K5E; 3KEN; 3L9H; 3ZCW; 4A1Z; 4A28; 4A50; 4A51; 4A5Y; 4AP0; 4AQV; 4AQW; 4AS7; 4B7B;4BBG; 4BXN; 4CK5; 4CK6; 4CK7
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| Drugs and Mode of Action | |||||
| Drug(s) | ARRY-520 | Drug Info | Phase 2 | Cancer | [1] |
| AZD-4877 | Drug Info | Phase 2 | Acute myeloid leukemia | [2], [3] | |
| Ispinesib | Drug Info | Phase 2 | Head and neck cancer; Renal cell carcinoma; Ovarian cancer; Solid tumors | [4] | |
| LY2523355 | Drug Info | Phase 2 | Acute myeloid leukemia | [5] | |
| SB-743921 | Drug Info | Phase 2 | Cancer | [6], [7] | |
| 4SC-205 | Drug Info | Phase 1 | Lymphoma | [8] | |
| ARQ 621 | Drug Info | Phase 1 | Hematological malignancies | [9] | |
| MK-0731 | Drug Info | Phase 1 | Solid tumours | [10] | |
| Inhibitor | 4SC-205 | Drug Info | [8] | ||
| Adenosine-5'-Diphosphate | Drug Info | [11] | |||
| ARRY-520 | Drug Info | [12], [13] | |||
| AZD-4877 | Drug Info | [14] | |||
| Ispinesib | Drug Info | [15], [16], [17] | |||
| MK-0731 | Drug Info | [14] | |||
| Monastrol | Drug Info | [18] | |||
| SB-743921 | Drug Info | [19] | |||
| Modulator | ARQ 621 | Drug Info | [14] | ||
| LY2523355 | Drug Info | [14] | |||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| Reactome | MHC class II antigen presentation | ||||
| Kinesins | |||||
| WikiPathways | MHC class II antigen presentation | ||||
| Kinesins | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT01989325) A Study of Filanesib (ARRY-520) and Carfilzomib in Patients With Advanced Multiple Myeloma. U.S. National Institutes of Health. | ||||
| REF 2 | ClinicalTrials.gov (NCT00661609) A Phase II Study of AZD4877 (a Novel Anti-mitotic Agent) in Advanced Bladder Cancer. U.S. National Institutes of Health. | ||||
| REF 3 | (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: 7708). | ||||
| REF 4 | ClinicalTrials.gov (NCT00095628) SB-715992 in Treating Patients With Recurrent or Metastatic Head and Neck Cancer. U.S. National Institutes of Health. | ||||
| REF 5 | ClinicalTrials.gov (NCT01416389) A Study of LY2523355 in Patients With Breast Cancer. U.S. National Institutes of Health. | ||||
| REF 6 | ClinicalTrials.gov (NCT00343564) A Study of SB-743921 in Non-Hodgkin's Lymphoma. U.S. National Institutes of Health. | ||||
| REF 7 | A first in human study of SB-743921, a kinesin spindle protein inhibitor, to determine pharmacokinetics, biologic effects and establish a recommended phase II dose. Cancer Chemother Pharmacol. 2011 Feb;67(2):447-54. | ||||
| REF 8 | 2011 Pipeline of 4SC AG. | ||||
| REF 9 | ClinicalTrials.gov (NCT00825487) Dose Escalation Study of ARQ 621 in Adult Patients With Metastatic Solid Tumors and Hematologic Malignancies. U.S. National Institutes of Health. | ||||
| REF 10 | ClinicalTrials.gov (NCT00104364) A Study of MK0731 in Patients With Advanced Solid Tumors (0731-002)(COMPLETED). U.S. National Institutes of Health. | ||||
| REF 11 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January | ||||
| REF 12 | Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Nov;29(9):625-55. | ||||
| REF 13 | Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells. Leukemia. 2009 May 21. | ||||
| REF 14 | Kinesins and cancer. Nat Rev Cancer. 2012 Jul 24;12(8):527-39. | ||||
| REF 15 | Gateways to clinical trials. July-August 2008. Methods Find Exp Clin Pharmacol. 2008 Jul-Aug;30(6):459-95. | ||||
| REF 16 | KIF11 inhibition for glioblastoma treatment: reason to hope or a struggle with the brain? BMC Cancer. 2009 Jun 22;9:196. | ||||
| REF 17 | Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. Pediatr Blood Cancer. 2009 Jun 24. | ||||
| REF 18 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 19 | Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Jan-Feb;31(1):47-57. | ||||
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