Synthesis, evaluation and molecular modelling of piceatannol analogues as arginase inhibitors

Author:

Muller J.1234ORCID,Cardey B.5234ORCID,Zedet A.1234,Desingle C.1234,Grzybowski M.678,Pomper P.678,Foley S.5234,Harakat D.910114,Ramseyer C.5234,Girard C.1234,Pudlo M.1234ORCID

Affiliation:

1. PEPITE EA4267

2. Univ. Bourgogne Franche-Comté

3. F-25000 Besançon

4. France

5. Laboratoire Chrono-environnement (UMR CNRS 6249)

6. OncoArendi Therapeutics

7. PL02089 Warsaw

8. Poland

9. Institut de Chimie Moléculaire de Reims (UMR CNRS 7312)

10. Univ. Reims Champagne Ardenne

11. F-51000 Reims

Abstract

A quantum chemistry guided optimisation (leading to piceatannol analogue 3t) with a good understanding of the catechol binding mode to the bimanganese cluster of arginase.

Funder

Conseil régional de Bourgogne-Franche-Comté

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Reference41 articles.

1. Cloning and Characterization of the Human Type II Arginase Gene

2. J. Steppan , D.Nyhan and D. E.Berkowitz , Development of Novel Arginase Inhibitors for Therapy of Endothelial Dysfunction. Front Immunol . 2013 , [cité 29 oct 2019];4. Disponible sur: http://journal.frontiersin.org/article/10.3389/fimmu.2013.00278/abstract

3. The Emerging Role of Arginase in Endothelial Dysfunction in Diabetes

4. Arginase: an old enzyme with new tricks

5. Arginase expression modulates nitric oxide production in Leishmania (Leishmania) amazonensis

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