Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab of Tim Mitchison. Monastrol was shown to inhibit the kinesin-5 (also known as KIF11, Kinesin Eg5), a motor protein important for spindle bipolarity.[1]
Monastrol binds to a long loop that is specific to the Eg5 (also known as KIF11 or kinesin-5) kinesin family, and allosterically inhibits ATPase activity of the kinesin [2]
Referencesedit
^Thomas U. Mayer; Tarun M. Kapoor; Stephen J. Haggarty; Randall W. King; Stuart L. Schreiber; Timothy J. Mitchison (1999). "Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype-Based Screen". Science. 286 (5441): 971–974. doi:10.1126/science.286.5441.971. PMID 10542155. S2CID 15348455.
^Maliga Z, Kapoor TM, Mitchison TJ (September 2002). "Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5". Chem. Biol. 9 (9): 989–96. doi:10.1016/S1074-5521(02)00212-0. PMID 12323373.
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monastrol, cell, permeable, small, molecule, inhibitor, discovered, thomas, mayer, mitchison, shown, inhibit, kinesin, also, known, kif11, kinesin, motor, protein, important, spindle, bipolarity, namesiupac, name, ethyl, hydroxyphenyl, methyl, sulfanylidene, d. Monastrol is a cell permeable small molecule inhibitor discovered by Thomas U Mayer in the lab of Tim Mitchison Monastrol was shown to inhibit the kinesin 5 also known as KIF11 Kinesin Eg5 a motor protein important for spindle bipolarity 1 Monastrol NamesIUPAC name ethyl 4 3 hydroxyphenyl 6 methyl 2 sulfanylidene 3 4 dihydro 1H pyrimidine 5 carboxylateOther names MonastrolIdentifiersCAS Number 329689 23 8 N3D model JSmol Interactive imageChEBI CHEBI 75382 YChEMBL ChEMBL236789 YChemSpider 2259791 YPubChem CID 2987927CompTox Dashboard EPA DTXSID10388124InChI InChI 1S C14H16N2O3S c1 3 19 13 18 11 8 2 15 14 20 16 12 11 9 5 4 6 10 17 7 9 h4 7 12 17H 3H2 1 2H3 H2 15 16 20 NKey LOBCDGHHHHGHFA UHFFFAOYSA N YInChI 1 C14H16N2O3S c1 3 19 13 18 11 8 2 15 14 20 16 12 11 9 5 4 6 10 17 7 9 h4 7 12 17H 3H2 1 2H3 H2 15 16 20 Key LOBCDGHHHHGHFA UHFFFAOYAOSMILES CCOC O C1 C NC S NC1C2 CC CC C2 O CPropertiesChemical formula C14H16N2O3SMolar mass 292 35344Except where otherwise noted data are given for materials in their standard state at 25 C 77 F 100 kPa N verify what is Y N Infobox referencesMechanism of action edit nbsp Monastrol inhibits Eg5Monastrol binds to a long loop that is specific to the Eg5 also known as KIF11 or kinesin 5 kinesin family and allosterically inhibits ATPase activity of the kinesin 2 References edit Thomas U Mayer Tarun M Kapoor Stephen J Haggarty Randall W King Stuart L Schreiber Timothy J Mitchison 1999 Small Molecule Inhibitor of Mitotic Spindle Bipolarity Identified in a Phenotype Based Screen Science 286 5441 971 974 doi 10 1126 science 286 5441 971 PMID 10542155 S2CID 15348455 Maliga Z Kapoor TM Mitchison TJ September 2002 Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5 Chem Biol 9 9 989 96 doi 10 1016 S1074 5521 02 00212 0 PMID 12323373 nbsp This pharmacology related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Monastrol amp oldid 1182789051, wikipedia, wiki, book, books, library,
