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Monastrol

From Wikipedia, the free encyclopedia
Monastrol
Names
IUPAC name
ethyl 4-(3-hydroxyphenyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxylate
Other names
Monastrol
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
  • 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) ☒N
    Key: LOBCDGHHHHGHFA-UHFFFAOYSA-N checkY
  • InChI=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-UHFFFAOYAO
  • CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C
Properties
C14H16N2O3S
Molar mass292.35344
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)
Chemical compound

Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab ofTim Mitchison. Monastrol was shown to inhibit thekinesin-5 (also known asKIF11, Kinesin Eg5), amotor protein important for spindle bipolarity.[1]

Mechanism of action

[edit]
Monastrol inhibits Eg5

Monastrol binds to a long loop that is specific to the Eg5 (also known asKIF11 or kinesin-5) kinesin family, and allosterically inhibits ATPase activity of the kinesin[2]

References

[edit]
  1. ^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.
  2. ^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.
Ionotropic
GABAATooltip γ-Aminobutyric acid A receptor
GABAA-ρTooltip γ-Aminobutyric acid A-rho receptor
Metabotropic
GABABTooltip γ-Aminobutyric acid B receptor
Receptor
(ligands)
GHBRTooltip GHB receptor
GABABTooltip γ-Aminobutyric acid B receptor
Transporter
(blockers)
MCTsTooltip Monocarboxylate transporters
SMCTsTooltip Sodium-coupled monocarboxylate transporters
VIATTTooltip Vesicular inhibitory amino acid transporter
Enzyme
(inhibitors)
SSRTooltip Succinic semialdehyde reductase
GHBDHTooltip 4-Hydroxybutyrate dehydrogenase
HOTTooltip Hydroxyacid-oxoacid transhydrogenase
ADHTooltip Alcohol dehydrogenase
ALDHTooltip Aldehyde dehydrogenase


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