Titre :

Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds

Auteur(s) :

Dumitriu, Gina-Mirabela [Auteur]
Bicu, Elena [Auteur]
Belei, Dalila [Auteur]
Rigo, Benoit [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]

Titre de la revue :

Bioorganic & Medicinal Chemistry Letters

Nom court de la revue :

Bioorg. Med. Chem. Lett.

Numéro :

25

Pagination :

4447-4452

Date de publication :

2015-10-15

ISSN :

0960-894X

Mot(s)-clé(s) en anglais :

Valine
Farnesyltransferase
Phenothiazine
Cysteine
Methionine
Serine
CAAX inhibitor

Discipline(s) HAL :

Sciences du Vivant [q-bio]

Résumé en anglais : [en]

A new family of CaaX competitive inhibitors of human farnesyltransferase based on phenothiazine and carbazole skeleton bearing a l-cysteine, l-methionine, l-serine or l-valine moiety was designed, synthesized and biologically ...
Lire la suite >A new family of CaaX competitive inhibitors of human farnesyltransferase based on phenothiazine and carbazole skeleton bearing a l-cysteine, l-methionine, l-serine or l-valine moiety was designed, synthesized and biologically evaluated. Phenothiazine derivatives proved to be more active than carbazole-based compounds. Phenothiazine 1b with cysteine residue was the most promising inhibitor of human farnesyltransferase in the current study.Lire moins >

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286

Équipe(s) de recherche :

Therapeutic innovation targetting inflammation

Date de dépôt :

2019-05-17T13:14:36Z