Title :

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

Author(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]

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

25

Pages :

4447-4452

Publication date :

2015-10-15

ISSN :

0960-894X

English keyword(s) :

Valine
Farnesyltransferase
Phenothiazine
Cysteine
Methionine
Serine
CAAX inhibitor

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [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 ...
Show more >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.Show less >

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

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

Research team(s) :

Therapeutic innovation targetting inflammation

Submission date :

2019-05-17T13:14:36Z