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Kinesin-like protein KIF11
A kinesin-like protein KIF11 that is encoded in the genome of human. [PRO:DNx]
Synonyms
Kinesin-like protein 1;
Kinesin-like spindle protein HKSP;
Kinesin-related motor protein Eg5;
Thyroid receptor-interacting protein 5;
TR-interacting protein 5;
TRIP-5
Research
Bioassay Publications (32)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (21.88) | 29.6817 |
| 2010's | 25 (78.13) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (22)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 3-tritylthio-l-alanine | Homo sapiens (human) | EC50 | 1.7200 | 1 | 1 |
| k 858 | Homo sapiens (human) | Kd | 0.6645 | 1 | 1 |
| sb 743921 | Homo sapiens (human) | Kd | 7.8371 | 8 | 8 |
Synthesis of N-(1-(6-acetamido-5-phenylpyrimidin-4-yl) piperidin-3-yl) amide derivatives as potential inhibitors for mitotic kinesin spindle protein.European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Structure-based design of new KSP-Eg5 inhibitors assisted by a targeted multicomponent reaction.Chembiochem : a European journal of chemical biology, , Jul-07, Volume: 15, Issue:10, 2014
Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.European journal of medicinal chemistry, , Volume: 62, 2013
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.European journal of medicinal chemistry, , Volume: 54, 2012
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Pharmacophore identification of KSP inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 17, Issue:3, 2007
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 15, Issue:8, 2005
Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Synthetic studies on mitotic kinesin Eg5 inhibitors: synthesis and structure-activity relationships of novel 2,4,5-substituted-1,3,4-thiadiazoline derivatives.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.European journal of medicinal chemistry, , Volume: 62, 2013
[no title available]Bioorganic & medicinal chemistry, , 12-01, Volume: 27, Issue:23, 2019
Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.European journal of medicinal chemistry, , Volume: 60, 2013
Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.European journal of medicinal chemistry, , Volume: 62, 2013
De novo design, synthesis and biological evaluation of 1,4-dihydroquinolin-4-ones and 1,2,3,4-tetrahydroquinazolin-4-ones as potent kinesin spindle protein (KSP) inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones.European journal of medicinal chemistry, , Volume: 46, Issue:8, 2011
Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
New chemical tools for investigating human mitotic kinesin Eg5.Bioorganic & medicinal chemistry, , Oct-01, Volume: 15, Issue:19, 2007
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Synthesis, biological evaluation and molecular docking studies of flavone and isoflavone derivatives as a novel class of KSP (kinesin spindle protein) inhibitors.European journal of medicinal chemistry, , Volume: 70, 2013
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Pharmacophore identification of KSP inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 17, Issue:3, 2007
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Resistance by allostery: a novel perspective for eg5-targeted drug design.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
De novo design, synthesis and biological evaluation of 1,4-dihydroquinolin-4-ones and 1,2,3,4-tetrahydroquinazolin-4-ones as potent kinesin spindle protein (KSP) inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin KSP.Bioorganic & medicinal chemistry, , Jun-15, Volume: 18, Issue:12, 2010
[no title available]Bioorganic & medicinal chemistry, , 12-01, Volume: 27, Issue:23, 2019
Synthesis and anticancer activity of new dihydropyrimidinone derivatives.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
New chemical tools for investigating human mitotic kinesin Eg5.Bioorganic & medicinal chemistry, , Oct-01, Volume: 15, Issue:19, 2007
Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 28, Issue:17, 2018
Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.European journal of medicinal chemistry, , Volume: 62, 2013
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| microtubule motor activity | molecular function | A motor activity that generates movement along a microtubule, driven by ATP hydrolysis. [PMID:19686686, PMID:32684327, PMID:32842864] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| microtubule binding | molecular function | Binding to a microtubule, a filament composed of tubulin monomers. [GOC:krc] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| plus-end-directed microtubule motor activity | molecular function | A motor activity that generates movement along a microtubule toward the plus end, driven by ATP hydrolysis. [GOC:vw, PMID:32842864] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| spindle | cellular component | The array of microtubules and associated molecules that forms between opposite poles of a eukaryotic cell during mitosis or meiosis and serves to move the duplicated chromosomes apart. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| microtubule | cellular component | Any of the long, generally straight, hollow tubes of internal diameter 12-15 nm and external diameter 24 nm found in a wide variety of eukaryotic cells; each consists (usually) of 13 protofilaments of polymeric tubulin, staggered in such a manner that the tubulin monomers are arranged in a helical pattern on the microtubular surface, and with the alpha/beta axes of the tubulin subunits parallel to the long axis of the tubule; exist in equilibrium with pool of tubulin monomers and can be rapidly assembled or disassembled in response to physiological stimuli; concerned with force generation, e.g. in the spindle. [ISBN:0879693568] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| mitotic spindle | cellular component | A spindle that forms as part of mitosis. Mitotic and meiotic spindles contain distinctive complements of proteins associated with microtubules. [GOC:mah, GOC:vw, PMID:11408572, PMID:18367542, PMID:8027178] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| mitotic spindle | cellular component | A spindle that forms as part of mitosis. Mitotic and meiotic spindles contain distinctive complements of proteins associated with microtubules. [GOC:mah, GOC:vw, PMID:11408572, PMID:18367542, PMID:8027178] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| kinesin complex | cellular component | Any complex that includes a dimer of molecules from the kinesin superfamily, a group of related proteins that contain an extended region of predicted alpha-helical coiled coil in the main chain that likely produces dimerization. The native complexes of several kinesin family members have also been shown to contain additional peptides, often designated light chains as all of the noncatalytic subunits that are currently known are smaller than the chain that contains the motor unit. Kinesin complexes generally possess a force-generating enzymatic activity, or motor, which converts the free energy of the gamma phosphate bond of ATP into mechanical work. [GOC:mah, http://www.proweb.org/kinesin//KinesinMotility.html, http://www.proweb.org/kinesin//KinesinStructure.html] |
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| mitotic cell cycle | biological process | Progression through the phases of the mitotic cell cycle, the most common eukaryotic cell cycle, which canonically comprises four successive phases called G1, S, G2, and M and includes replication of the genome and the subsequent segregation of chromosomes into daughter cells. In some variant cell cycles nuclear replication or nuclear division may not be followed by cell division, or G1 and G2 phases may be absent. [GOC:mah, ISBN:0815316194, Reactome:69278] |
| microtubule-based movement | biological process | A microtubule-based process that results in the movement of organelles, other microtubules, or other cellular components. Examples include motor-driven movement along microtubules and movement driven by polymerization or depolymerization of microtubules. [GOC:cjm, ISBN:0815316194] |
| spindle organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of the spindle, the array of microtubules and associated molecules that forms between opposite poles of a eukaryotic cell during DNA segregation and serves to move the duplicated chromosomes apart. [GOC:go_curators, GOC:mah] |
| mitotic spindle organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of the microtubule spindle during a mitotic cell cycle. [GOC:go_curators, GOC:mah] |
| mitotic centrosome separation | biological process | Separation of duplicated centrosome components at the beginning of mitosis. The centriole pair within each centrosome becomes part of a separate microtubule organizing center that nucleates a radial array of microtubules called an aster. The two asters move to opposite sides of the nucleus to form the two poles of the mitotic spindle. [ISBN:0815316194] |
| regulation of mitotic centrosome separation | biological process | Any process that modulates the frequency, rate or extent of the separation of duplicated centrosome components at the beginning of mitosis. [GOC:ai] |
| cell division | biological process | The process resulting in division and partitioning of components of a cell to form more cells; may or may not be accompanied by the physical separation of a cell into distinct, individually membrane-bounded daughter cells. [GOC:di, GOC:go_curators, GOC:pr] |
| mitotic spindle assembly | biological process | Mitotic bipolar spindle assembly begins with spindle microtubule nucleation from the separated spindle pole body, includes spindle elongation during prometaphase, and is complete when all kinetochores are stably attached the spindle, and the spindle assembly checkpoint is satisfied. [GOC:tb, GOC:vw] |
| spindle elongation | biological process | The cell cycle process in which the distance is lengthened between poles of the spindle. [GOC:ai] |