Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
Abstract: An in cellulo method for the screening of proteasome activity-modulating agents, includes the following steps of: a) bringing into contact the candidate agent with the yeast cell expressing in their nucleus a fusion protein comprising: (i) a p21 polypeptide selected from the p21WAF1/Cip1 polypeptide and the p21[6KR]WAF1/Cip1 polypeptide; and (ii) at least one detectable protein; b) quantifying the first detectable protein in the yeast cells, at the end of at least one predetermined time interval after bringing into contact the candidate agent with the cells; c) comparing the value obtained at the step (b) with a control value obtained when the step (a) is performed in the absence of the candidate agent.
Type:
Application
Filed:
October 19, 2006
Publication date:
August 26, 2010
Applicant:
CYTOMICS SYSTEMS
Inventors:
Cécile Bougeret, Jean-Francois Briand, Patrick Zarzov, Dominique Thomas