Target Information

Target General Infomation
Target ID
T28484
Former ID
TTDC00143
Target Name
Kinesin-like protein KIF11
Gene Name
KIF11
Synonyms
Eg5; Kinesin-like protein 1; Kinesin-like spindle protein HKSP; Kinesin-related motor protein Eg5; TRIP5; Thyroid receptor interacting protein 5; KIF11
Target Type
Clinical Trial
Disease Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Hematological malignancies [ICD9: 200-209; ICD10: C81-C86]
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]
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.
BioChemical Class
Kinesin-like protein family
Target Validation
T28484
UniProt ID
P52732
Sequence
MASQPNSSAKKKEEKGKNIQVVVRCRPFNLAERKASAHSIVECDPVRKEVSVRTGGLADK
SSRKTYTFDMVFGASTKQIDVYRSVVCPILDEVIMGYNCTIFAYGQTGTGKTFTMEGERS
PNEEYTWEEDPLAGIIPRTLHQIFEKLTDNGTEFSVKVSLLEIYNEELFDLLNPSSDVSE
RLQMFDDPRNKRGVIIKGLEEITVHNKDEVYQILEKGAAKRTTAATLMNAYSSRSHSVFS
VTIHMKETTIDGEELVKIGKLNLVDLAGSENIGRSGAVDKRAREAGNINQSLLTLGRVIT
ALVERTPHVPYRESKLTRILQDSLGGRTRTSIIATISPASLNLEETLSTLEYAHRAKNIL
NKPEVNQKLTKKALIKEYTEEIERLKRDLAAAREKNGVYISEENFRVMSGKLTVQEEQIV
ELIEKIGAVEEELNRVTELFMDNKNELDQCKSDLQNKTQELETTQKHLQETKLQLVKEEY
ITSALESTEEKLHDAASKLLNTVEETTKDVSGLHSKLDRKKAVDQHNAEAQDIFGKNLNS
LFNNMEELIKDGSSKQKAMLEVHKTLFGNLLSSSVSALDTITTVALGSLTSIPENVSTHV
SQIFNMILKEQSLAAESKTVLQELINVLKTDLLSSLEMILSPTVVSILKINSQLKHIFKT
SLTVADKIEDQKKELDGFLSILCNNLHELQENTICSLVESQKQCGNLTEDLKTIKQTHSQ
ELCKLMNLWTERFCALEEKCENIQKPLSSVQENIQQKSKDIVNKMTFHSQKFCADSDGFS
QELRNFNQEGTKLVEESVKHSDKLNGNLEKISQETEQRCESLNTRTVYFSEQWVSSLNER
EQELHNLLEVVSQCCEASSSDITEKSDGRKAAHEKQHNIFLDQMTIDEDKLIAQNLELNE
TIKIGLTKLNCFLEQDLKLDIPTGTTPQRKSYLYPSTLVRTEPREHLLDQLKRKQPELLM
MLNCSENNKEETIPDVDVEEAVLGQYTEEPLSQEPSVDAGVDCSSIGGVPFFQHKKSHGK
DKENRGINTLERSKVEETTEHLVTKSRLPLRAQINL
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
Drugs and Mode of Action
Drug(s) ARRY-520 Drug Info Phase 2 Cancer [524532]
AZD-4877 Drug Info Phase 2 Acute myeloid leukemia [522297], [542683]
Ispinesib Drug Info Phase 2 Head and neck cancer; Renal cell carcinoma; Ovarian cancer; Solid tumors [521617]
LY2523355 Drug Info Phase 2 Acute myeloid leukemia [523589]
SB-743921 Drug Info Phase 2 Cancer [521846], [530907]
4SC-205 Drug Info Phase 1 Lymphoma [551497]
ARQ 621 Drug Info Phase 1 Hematological malignancies [522550]
MK-0731 Drug Info Phase 1 Solid tumours [521631]
Inhibitor 4SC-205 Drug Info [551497]
Adenosine-5'-Diphosphate Drug Info [551391]
ARRY-520 Drug Info [536588], [537357]
AZD-4877 Drug Info [531974]
Ispinesib Drug Info [536879], [537505], [537526]
MK-0731 Drug Info [531974]
Monastrol Drug Info [551393]
SB-743921 Drug Info [537212]
Modulator ARQ 621 Drug Info [531974]
LY2523355 Drug Info [531974]
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 521617ClinicalTrials.gov (NCT00095628) SB-715992 in Treating Patients With Recurrent or Metastatic Head and Neck Cancer. U.S. National Institutes of Health.
Ref 521631ClinicalTrials.gov (NCT00104364) A Study of MK0731 in Patients With Advanced Solid Tumors (0731-002)(COMPLETED). U.S. National Institutes of Health.
Ref 521846ClinicalTrials.gov (NCT00343564) A Study of SB-743921 in Non-Hodgkin's Lymphoma. U.S. National Institutes of Health.
Ref 522297ClinicalTrials.gov (NCT00661609) A Phase II Study of AZD4877 (a Novel Anti-mitotic Agent) in Advanced Bladder Cancer. U.S. National Institutes of Health.
Ref 522550ClinicalTrials.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 523589ClinicalTrials.gov (NCT01416389) A Study of LY2523355 in Patients With Breast Cancer. U.S. National Institutes of Health.
Ref 524532ClinicalTrials.gov (NCT01989325) A Study of Filanesib (ARRY-520) and Carfilzomib in Patients With Advanced Multiple Myeloma. U.S. National Institutes of Health.
Ref 530907A 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 542683(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 5514972011 Pipeline of 4SC AG.
Ref 531974Kinesins and cancer. Nat Rev Cancer. 2012 Jul 24;12(8):527-39.
Ref 536588Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Nov;29(9):625-55.
Ref 536879Gateways to clinical trials. July-August 2008. Methods Find Exp Clin Pharmacol. 2008 Jul-Aug;30(6):459-95.
Ref 537212Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Jan-Feb;31(1):47-57.
Ref 537357Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells. Leukemia. 2009 May 21.
Ref 537505KIF11 inhibition for glioblastoma treatment: reason to hope or a struggle with the brain? BMC Cancer. 2009 Jun 22;9:196.
Ref 537526Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. Pediatr Blood Cancer. 2009 Jun 24.
Ref 551391DrugBank 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 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 5514972011 Pipeline of 4SC AG.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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