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词条 Hesperadin
释义

  1. References

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| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 443873334
| ImageFile=hesperadin.svg
| ImageSize=200px
| IUPACName=N-[(3Z)-2-Oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide
| OtherNames=
|Section1={{Chembox Identifiers
| CASNo=422513-13-1
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| PubChem=10142586
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| ChemSpiderID = 8318096
| InChI = 1/C29H32N4O3S/c1-2-37(35,36)32-24-15-16-26-25(19-24)27(29(34)31-26)28(22-9-5-3-6-10-22)30-23-13-11-21(12-14-23)20-33-17-7-4-8-18-33/h3,5-6,9-16,19,30,32H,2,4,7-8,17-18,20H2,1H3,(H,31,34)/b28-27-
| InChIKey = GLDSKRNGVVYJAB-DQSJHHFOBF
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 1S/C29H32N4O3S/c1-2-37(35,36)32-24-15-16-26-25(19-24)27(29(34)31-26)28(22-9-5-3-6-10-22)30-23-13-11-21(12-14-23)20-33-17-7-4-8-18-33/h3,5-6,9-16,19,30,32H,2,4,7-8,17-18,20H2,1H3,(H,31,34)/b28-27-
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| StdInChIKey = GLDSKRNGVVYJAB-DQSJHHFOSA-N
| SMILES=CCS(=O)(=O)NC1=CC2=C(C=C1)NC(=O)C2=C(C3=CC=CC=C3)NC4=CC=C(C=C4)CN5CCCCC5
|Section2={{Chembox Properties
| C=29 | H=32 | N=4 | O=3 | S=1
| Appearance=
| Density=
| MeltingPt=
| BoilingPt=
| Solubility=
|Section3={{Chembox Hazards
| MainHazards=
| FlashPt=
| AutoignitionPt =
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Hesperadin is an aurora kinase inhibitor.

The small molecule inhibits chromosome alignment and segregation by limiting the function of miotic kinases Aurora B and Aurora A Hesperadin causes cells to enter Anaphase much faster, sometimes before the chromosomes are properly mono-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.

References

1. ^{{Cite journal|last=Hauf|first=Silke|last2=Cole|first2=Richard W.|last3=LaTerra|first3=Sabrina|last4=Zimmer|first4=Christine|last5=Schnapp|first5=Gisela|last6=Walter|first6=Rainer|last7=Heckel|first7=Armin|last8=van Meel|first8=Jacques|last9=Rieder|first9=Conly L.|date=2003-04-28|title=The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint|journal=The Journal of Cell Biology|volume=161|issue=2|pages=281–294|doi=10.1083/jcb.200208092|issn=0021-9525|pmc=2172906|pmid=12707311}}
2. ^{{Cite journal|last=Jetton|first=Neal|last2=Rothberg|first2=Karen G.|last3=Hubbard|first3=James G.|last4=Wise|first4=John|last5=Li|first5=Yan|last6=Ball|first6=Haydn L.|last7=Ruben|first7=Larry|date=April 2009|title=The cell cycle as a therapeutic target againstTrypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms|journal=Molecular Microbiology|volume=72|issue=2|pages=442–458|doi=10.1111/j.1365-2958.2009.06657.x|issn=0950-382X|pmc=2697958|pmid=19320832}}
{{pharma-stub}}

4 : Protein kinase inhibitors|Sulfonamides|Piperidines|Lactams

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