Document Report Card

ID: ALA3351843

Journal: J Med Chem

Title: Noncovalent fluorescent probes of human immuno- and constitutive proteasomes.

Authors: Desvergne A, Cheng Y, Grosay-Gaudrel S, Maréchal X, Reboud-Ravaux M, Genin E, Vidal J.

Abstract: We report here the synthesis and biological evaluation of fluorescent probes functioning as inhibitors that noncovalently block human immuno- and constitutive proteasomes. These cell-penetrating linear analogues of the natural cyclopeptide TMC-95A were efficient on cells at the nanomolar level and assessed by confocal microscopy and flow cytometry. They may constitute an alternative to previously reported fluorescent probes that all bind covalently to proteasomes.

CiteXplore: 25333324

DOI: 10.1021/jm5011429