Hesperadin

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 mono-oriented.[1]

Hesperadin
Names
IUPAC name
N-[(3Z)-2-Oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide
Identifiers
3D model (JSmol)
ChemSpider
UNII
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).
N verify (what is YN ?)
Infobox references

Hesperadin is an aurora kinase inhibitor.

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.

References

  1. 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.
  2. 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 againstTrypanosoma 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.


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.