Hesperadin
Appearance
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Preferred IUPAC name
N-[(3Z)-2-Oxo-3-(phenyl{4-[(piperidin-1-yl)methyl]anilino}methylidene)-2,3-dihydro-1H-indol-5-yl]ethanesulfonamide | |
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3D model (JSmol)
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PubChem CID
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UNII | |
CompTox Dashboard (EPA)
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Properties | |
C29H32N4O3S | |
Molar mass | 516.66 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Hesperadin is an aurora kinase inhibitor.
The small molecule inhibits chromosome alignment and segregation by limiting the function of mitotic kinases Aurora B and Aurora A. Hesperadin causes cells to enter anaphase much faster, sometimes before the chromosomes are properly bi-oriented.[1]
Hesperadin, like other miotic inhibitors, limits and sometimes can stop the process of mitosis in cells. For this reason, some have considered hesperadin's potential as a cancer-preventing drug.[2]
Hesperadin works as an inhibitor, attaching to the active sites of Aurora A and Aurora B kinases.[2]
References
[edit]- ^ Hauf, Silke; Cole, Richard W.; LaTerra, Sabrina; Zimmer, Christine; Schnapp, Gisela; Walter, Rainer; Heckel, Armin; van Meel, Jacques; Rieder, Conly L. (2003-04-28). "The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint". The Journal of Cell Biology. 161 (2): 281–294. doi:10.1083/jcb.200208092. ISSN 0021-9525. PMC 2172906. PMID 12707311.
- ^ a b Jetton, Neal; Rothberg, Karen G.; Hubbard, James G.; Wise, John; Li, Yan; Ball, Haydn L.; Ruben, Larry (April 2009). "The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms". Molecular Microbiology. 72 (2): 442–458. doi:10.1111/j.1365-2958.2009.06657.x. ISSN 0950-382X. PMC 2697958. PMID 19320832.