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Inhibition of Insul...
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Borhade, Sanjay RUppsala universitet,Avdelningen för organisk farmaceutisk kemi
(author)
Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides
- Article/chapterEnglish2014
Publisher, publication year, extent ...
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2014-11-21
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Wiley,2014
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printrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:uu-241194
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https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-241194URI
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https://doi.org/10.1002/open.201402027DOI
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http://kipublications.ki.se/Default.aspx?queryparsed=id:130310109URI
Supplementary language notes
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Language:English
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Summary in:English
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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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 ...)
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Rosenström, UlrikaUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)ulrirose
(author)
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Sävmarker, JonasUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)josav517
(author)
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Lundbäck, ThomasKarolinska Institutet
(author)
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Jenmalm-Jensen, AnnikaKarolinska Institutet
(author)
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Sigmundsson, Kristmundur
(author)
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Axelsson, HannaKarolinska Institutet
(author)
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Svensson, FredrikUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)fresv747
(author)
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Konda, VivekUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)vivko837
(author)
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Sköld, ChristianUppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)chsko021
(author)
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Larhed, MatsUppsala universitet,Avdelningen för organisk farmaceutisk kemi,Science for Life Laboratory, SciLifeLab(Swepub:uu)matslarh
(author)
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Hallberg, MathiasUppsala universitet,Institutionen för farmaceutisk biovetenskap(Swepub:uu)mha03066
(author)
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Uppsala universitetAvdelningen för organisk farmaceutisk kemi
(creator_code:org_t)
Related titles
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In:ChemistryOpen: Wiley3:6, s. 256-2632191-1363
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Axelsson, Hanna
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ChemistryOpen
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