SwePub
Sök i LIBRIS databas

  Extended search

onr:"swepub:oai:DiVA.org:uu-241194"
 

Search: onr:"swepub:oai:DiVA.org:uu-241194" > Inhibition of Insul...

  • 1 of 1
  • Previous record
  • Next record
  •    To hitlist
  • Borhade, Sanjay RUppsala universitet,Avdelningen för organisk farmaceutisk kemi (author)

Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides

  • Article/chapterEnglish2014

Publisher, publication year, extent ...

  • 2014-11-21
  • Wiley,2014
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:uu-241194
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-241194URI
  • https://doi.org/10.1002/open.201402027DOI
  • http://kipublications.ki.se/Default.aspx?queryparsed=id:130310109URI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

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

Notes

  • The inhibition of insulin-regulated aminopeptidase (IRAP, EC 3.4.11.3) by angiotenesin IV is known to improve memory and learning in rats. Screening 10 500 low-molecular-weight compounds in an enzyme inhibition assay with IRAP from Chinese Hamster Ovary (CHO) cells provided an arylsulfonamide (N-(3-(1H-tetrazol-5-yl)phenyl)-4-bromo-5-chlorothiophene-2-sulfonamide), comprising a tetrazole in the meta position of the aromatic ring, as a hit. Analogues of this hit were synthesized, and their inhibitory capacities were determined. A small structure-activity relationship study revealed that the sulfonamide function and the tetrazole ring are crucial for IRAP inhibition. The inhibitors exhibited a moderate inhibitory potency with an IC50=1.1±0.5 μm for the best inhibitor in the series. Further optimization of this new class of IRAP inhibitors is required to make them attractive as research tools and as potential cognitive enhancers.

Subject headings and genre

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

  • Rosenström, UlrikaUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)ulrirose (author)
  • Sävmarker, JonasUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)josav517 (author)
  • Lundbäck, ThomasKarolinska Institutet (author)
  • Jenmalm-Jensen, AnnikaKarolinska Institutet (author)
  • Sigmundsson, Kristmundur (author)
  • Axelsson, HannaKarolinska Institutet (author)
  • Svensson, FredrikUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)fresv747 (author)
  • Konda, VivekUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)vivko837 (author)
  • Sköld, ChristianUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)chsko021 (author)
  • Larhed, MatsUppsala universitet,Avdelningen för organisk farmaceutisk kemi,Science for Life Laboratory, SciLifeLab(Swepub:uu)matslarh (author)
  • Hallberg, MathiasUppsala universitet,Institutionen för farmaceutisk biovetenskap(Swepub:uu)mha03066 (author)
  • Uppsala universitetAvdelningen för organisk farmaceutisk kemi (creator_code:org_t)

Related titles

  • In:ChemistryOpen: Wiley3:6, s. 256-2632191-1363

Internet link

Find in a library

To the university's database

  • 1 of 1
  • Previous record
  • Next record
  •    To hitlist

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