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Inhibition of Insul...
Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides
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- Borhade, Sanjay R (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Rosenström, Ulrika (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Sävmarker, Jonas (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Lundbäck, Thomas (author)
- Karolinska Institutet
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- Jenmalm-Jensen, Annika (author)
- Karolinska Institutet
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Sigmundsson, Kristmundur (author)
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- Axelsson, Hanna (author)
- Karolinska Institutet
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- Svensson, Fredrik (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Konda, Vivek (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Sköld, Christian (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Larhed, Mats (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi,Science for Life Laboratory, SciLifeLab
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- Hallberg, Mathias (author)
- Uppsala universitet,Institutionen för farmaceutisk biovetenskap
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(creator_code:org_t)
- 2014-11-21
- 2014
- English.
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In: ChemistryOpen. - : Wiley. - 2191-1363. ; 3:6, s. 256-263
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Abstract
Subject headings
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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
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Borhade, Sanjay ...
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Rosenström, Ulri ...
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Sävmarker, Jonas
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Lundbäck, Thomas
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Jenmalm-Jensen, ...
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Sigmundsson, Kri ...
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show more...
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Axelsson, Hanna
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Svensson, Fredri ...
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Konda, Vivek
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Sköld, Christian
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Larhed, Mats
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Hallberg, Mathia ...
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmaceutical S ...
- Articles in the publication
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ChemistryOpen
- By the university
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Uppsala University
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Karolinska Institutet