From the configurational preference of dihydroceramide desaturase-1 towards Δ6-unsaturated substrates to the discovery of a new inhibitor

Ana Pou; José-Luís Abad; Yadira F. Ordóñez; Maria Garrido; Josefina Casas; Gemma Fabriàs; Antonio Delgado

doi:10.1039/C6CC08268H

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From the configurational preference of dihydroceramide desaturase-1 towards Δ⁶-unsaturated substrates to the discovery of a new inhibitor†

Ana Pou,^a José-Luís Abad,^a Yadira F. Ordóñez,^a Maria Garrido,^a Josefina Casas,

^a Gemma Fabriàs

*^a and Antonio Delgado

*^ab

Author affiliations

* Corresponding authors

^a Spanish National Research Council (CSIC), Institute of Advanced Chemistry of Catalonia (IQAC-CSIC), Research Unit on Bioactive Molecules (RUBAM), Department of Biomedicinal Chemistry, Jordi Girona 18-26, 08034-Barcelona, Spain
E-mail: gemma.fabrias@iqac.csic.es, delgado@rubam.net

^b University of Barcelona (UB), Faculty of Pharmacy and Food Sciences, Department of Pharmacology, Toxicology and Medicinal Chemistry, Unit of Pharmaceutical Chemistry (Associated Unit to CSIC), Avda. Joan XXIII s/n, 08028-Barcelona, Spain

Abstract

Dihydroceramide desaturase 1 (Des1) catalyzes the last step of ceramide synthesis de novo, thus regulating the physiologically relevant balance between dihydrosphingolipids and sphingolipids. Here we report on the configurational preference of Des1 towards isomeric Δ⁶-unsaturated dihydroceramide analogs and the discovery of a potent Des1 inhibitor.

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Article information

DOI: https://doi.org/10.1039/C6CC08268H
Article type: Communication
Submitted: 13 Oct 2016
Accepted: 27 Mar 2017
First published: 27 Mar 2017

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Chem. Commun., 2017,53, 4394-4397

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From the configurational preference of dihydroceramide desaturase-1 towards Δ⁶-unsaturated substrates to the discovery of a new inhibitor

A. Pou, J. Abad, Y. F. Ordóñez, M. Garrido, J. Casas, G. Fabriàs and A. Delgado, Chem. Commun., 2017, 53, 4394 DOI: 10.1039/C6CC08268H

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