SwePub
Sök i LIBRIS databas

  Extended search

WFRF:(Brown Andrew R.)
 

Search: WFRF:(Brown Andrew R.) > (2005-2009) > Inhibition of dynam...

  • Hill, Timothy A (author)

Inhibition of dynamin mediated endocytosis by the dynoles : synthesis and functional activity of a family of indoles

  • Article/chapterEnglish2009

Publisher, publication year, extent ...

  • 2009-05-21
  • American Chemical Society (ACS),2009
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:uu-124854
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-124854URI
  • https://doi.org/10.1021/jm900036mDOI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Screening identified two bisindolylmaleimides as 100 microM inhibitors of the GTPase activity of dynamin I. Focused library approaches allowed development of indole-based dynamin inhibitors called dynoles. 100-Fold in vitro enhancement of potency was noted with the best inhibitor, 2-cyano-3-(1-(2-(dimethylamino)ethyl)-1H-indol-3-yl)-N-octylacrylamide (dynole 34-2), a 1.3 +/- 0.3 microM dynamin I inhibitor. Dynole 34-2 potently inhibited receptor mediated endocytosis (RME) internalization of Texas red-transferrin. The rank order of potency for a variety of dynole analogues on RME in U2OS cells matched their rank order for dynamin inhibition, suggesting that the mechanism of inhibition is via dynamin. Dynoles are the most active dynamin I inhibitors reported for in vitro or RME evaluations. Dynole 34-2 is 15-fold more active than dynasore against dynamin I and 6-fold more active against dynamin mediated RME (IC(50) approximately 15 microM; RME IC(50) approximately 80 microM). The dynoles represent a new series of tools to better probe endocytosis and dynamin-mediated trafficking events in a variety of cells.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Gordon, Christopher P (author)
  • McGeachie, Andrew B (author)
  • Venn-Brown, Barbara (author)
  • Odell, Luke RUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)lucod220 (author)
  • Chau, Ngoc (author)
  • Quan, Annie (author)
  • Mariana, Anna (author)
  • Sakoff, Jennette A (author)
  • Chircop, Megan (author)
  • Robinson, Phillip J (author)
  • McCluskey, Adam (author)
  • Uppsala universitetAvdelningen för organisk farmaceutisk kemi (creator_code:org_t)

Related titles

  • In:Journal of Medicinal Chemistry: American Chemical Society (ACS)52:12, s. 3762-37730022-26231520-4804

Internet link

Find in a library

To the university's database

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

 
pil uppåt Close

Copy and save the link in order to return to this view