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Tuning the properties of a cyclic RGD-containing tetrapeptide through backbone fluorination

Authors :
Zhiyong Wang
Eddy Pasquier
Flora Mansour
Renate Griffith
Xiang-Guo Hu
Yun Cheuk Leung
Luke Hunter
Johny Trinh
Christina Gonzalez
Catherine Au
Department of Pediatrics
Vanderbilt University [Nashville]
Department of Mechanics, Tianjin University
affiliation inconnue
Centre de Recherches en Oncologie biologique et Oncopharmacologie (CRO2)
Aix Marseille Université (AMU)- Hôpital de la Timone [CHU - APHM] (TIMONE)-Institut National de la Santé et de la Recherche Médicale (INSERM)
Centre de Recherche en Cancérologie de Marseille (CRCM)
Centre National de la Recherche Scientifique (CNRS)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut Paoli-Calmettes
Fédération nationale des Centres de lutte contre le Cancer (FNCLCC)-Fédération nationale des Centres de lutte contre le Cancer (FNCLCC)-Aix Marseille Université (AMU)
Aix Marseille Université (AMU)-Institut Paoli-Calmettes
Fédération nationale des Centres de lutte contre le Cancer (FNCLCC)-Fédération nationale des Centres de lutte contre le Cancer (FNCLCC)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS)
Source :
Organic and Biomolecular Chemistry, Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2019, 17 (3), pp.664-674. ⟨10.1039/c8ob02679c⟩, Organic & Biomolecular Chemistry, Organic & Biomolecular Chemistry, 2019, 17 (3), pp.664-674. ⟨10.1039/c8ob02679c⟩
Publication Year :
2019
Publisher :
HAL CCSD, 2019.

Abstract

International audience; Stereoselective fluorination is investigated as a method for modulating the properties of a cyclic RGD-containing tetrapeptide. Three key outcomes of fluorination are assessed: (i) the effect on peptide cyclisation efficiency; (ii) the ability to fine-tune the molecular conformation; and (iii) the effect on the cyclic peptides' biological activity. Fluorination is found to exert pronounced effects against all three criteria.

Details

Language :
English
ISSN :
14770520 and 14770539
Database :
OpenAIRE
Journal :
Organic and Biomolecular Chemistry, Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2019, 17 (3), pp.664-674. ⟨10.1039/c8ob02679c⟩, Organic & Biomolecular Chemistry, Organic & Biomolecular Chemistry, 2019, 17 (3), pp.664-674. ⟨10.1039/c8ob02679c⟩
Accession number :
edsair.doi.dedup.....f3b393b5a8b17f606106d8d1ed5ac912