Structure-activity relationships (sars) ...
Type de document :
Article dans une revue scientifique: Article original
DOI :
PMID :
URL permanente :
Titre :
Structure-activity relationships (sars) of ?-ketothioamides as inhibitors of phosphoglycerate dehydrogenase (phgdh)
Auteur(s) :
Spillier, Quentin [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Ravez, Severine [Auteur]
Lille Neurosciences & Cognition (LilNCog) - U 1172
Lille Neurosciences & Cognition (LilNCog) - U 1172
Unterlass, Judith [Auteur]
Department of Oncology-Pathology [Karolinska Institutet]
Corbet, Cyril [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Degavre, Charline [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Feron, Olivier [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Frederick, Raphael [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Ravez, Severine [Auteur]
Lille Neurosciences & Cognition (LilNCog) - U 1172
Lille Neurosciences & Cognition (LilNCog) - U 1172
Unterlass, Judith [Auteur]
Department of Oncology-Pathology [Karolinska Institutet]
Corbet, Cyril [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Degavre, Charline [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Feron, Olivier [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Frederick, Raphael [Auteur]
Université Catholique de Louvain = Catholic University of Louvain [UCL]
Titre de la revue :
Pharmaceuticals (Basel, Switzerland)
Nom court de la revue :
Pharmaceuticals (Basel)
Numéro :
13
Pagination :
20
Éditeur :
MDPI
Date de publication :
2020-01-22
ISSN :
1424-8247
Mot(s)-clé(s) :
serine synthesis pathway inhibitors
alpha-ketothioamides
PHGDH
alpha-ketothioamides
PHGDH
Discipline(s) HAL :
Sciences du Vivant [q-bio]
Résumé en anglais : [en]
For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted ...
Lire la suite >For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted the crucial role of the serine synthetic pathway, and particularly of the phosphoglycerate dehydrogenase (PHGDH), the first enzyme of the pathway, to sustain cancer progression. Yet, because of very weak potencies usually in cell-based settings, the inhibitors reported so far failed to lay ground on the potential of this approach. In this paper, we report a structure–activity relationship study of a series of α-ketothioamides that we have recently identified. Interestingly, this study led to a deeper understanding of the structure–activity relationship (SAR) in this series and to the identification of new PHGDH inhibitors. The activity of the more potent compounds was confirmed by cellular thermal shift assays and in cell-based experiments. We hope that this research will eventually provide a new entry point, based on this promising chemical scaffold, for the development of therapeutic agents targeting PHGDHLire moins >
Lire la suite >For many years now, targeting deregulation within cancer cells’ metabolism has appeared as a promising strategy for the development of more specific and efficient cancer treatments. Recently, numerous reports highlighted the crucial role of the serine synthetic pathway, and particularly of the phosphoglycerate dehydrogenase (PHGDH), the first enzyme of the pathway, to sustain cancer progression. Yet, because of very weak potencies usually in cell-based settings, the inhibitors reported so far failed to lay ground on the potential of this approach. In this paper, we report a structure–activity relationship study of a series of α-ketothioamides that we have recently identified. Interestingly, this study led to a deeper understanding of the structure–activity relationship (SAR) in this series and to the identification of new PHGDH inhibitors. The activity of the more potent compounds was confirmed by cellular thermal shift assays and in cell-based experiments. We hope that this research will eventually provide a new entry point, based on this promising chemical scaffold, for the development of therapeutic agents targeting PHGDHLire moins >
Langue :
Anglais
Audience :
Internationale
Vulgarisation :
Non
Établissement(s) :
CHU Lille
Inserm
Université de Lille
Inserm
Université de Lille
Collections :
Équipe(s) de recherche :
Brain Biology & Chemistry (BBC)
Date de dépôt :
2021-06-23T11:42:40Z
2022-11-16T08:57:32Z
2022-11-16T08:57:32Z
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- pharmaceuticals-13-00020-v2.pdf
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