Literature DB >> 20307982

Identification of very potent inhibitor of human aminopeptidase N (CD13).

Renata Grzywa1, Józef Oleksyszyn, Guy S Salvesen, Marcin Drag.   

Abstract

In this Letter we describe broad comparision studies toward rat, pig, and human aminopeptidase N (CD13) orthologs using phosphinate inhibitors related in structure to hydroxamic acids. This SAR approach yielded a very potent inhibitor of human aminopeptidase N: alpha(1)-amino-3-phenylpropyl(alpha(2)-hydroxy-3-phenylpropyl)phosphinic acid with an IC(50)=60 nM. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20307982     DOI: 10.1016/j.bmcl.2010.02.111

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Comparison of protease and aminopeptidase activities in meconium: A pilot study.

Authors:  Ewa Skarżyńska; Paulina Wilczyńska; Bartosz Kiersztyn; Joanna Żytyńska-Daniluk; Artur Jakimiuk; Barbara Lisowska-Myjak
Journal:  Biomed Rep       Date:  2020-06-09

2.  Phosphonic Acid Analogues of Phenylglycine as Inhibitors of Aminopeptidases: Comparison of Porcine Aminopeptidase N, Bovine Leucine Aminopeptidase, Tomato Acidic Leucine Aminopeptidase and Aminopeptidase from Barley Seeds.

Authors:  Weronika Wanat; Michał Talma; Małgorzata Pawełczak; Paweł Kafarski
Journal:  Pharmaceuticals (Basel)       Date:  2019-09-17

3.  Establishment of a screening protocol for identification of aminopeptidase N inhibitors.

Authors:  Miaomiao Niu; Fengzhen Wang; Fang Li; Yaru Dong; Yueqing Gu
Journal:  J Taiwan Inst Chem Eng       Date:  2014-12-31       Impact factor: 5.876

4.  Phosphonic Acid Analogs of Fluorophenylalanines as Inhibitors of Human and Porcine Aminopeptidases N: Validation of the Importance of the Substitution of the Aromatic Ring.

Authors:  Weronika Wanat; Michał Talma; Błażej Dziuk; Jean-Luc Pirat; Paweł Kafarski
Journal:  Biomolecules       Date:  2020-04-09
  4 in total

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