Identification of chemical inhibitors of protein-kinase CK2 subunit interaction. - Inserm - Institut national de la santé et de la recherche médicale Access content directly
Journal Articles Molecular and Cellular Biochemistry Year : 2008

Identification of chemical inhibitors of protein-kinase CK2 subunit interaction.

Abstract

Protein kinase CK2 is a multi-subunit complex whose dynamic assembly appears as a crucial point of regulation. The ability to interfere with specific protein-protein interactions has already provided powerful means of influencing the functions of selected proteins within the cell. CK2beta-derived cyclopeptides that target a well-defined hydrophobic pocket on CK2alpha have been previously characterized as potent inhibitors of CK2 subunit assembly [9]. As a first step toward the rational design of low molecular weight CK2 antagonists, we have in the present study screened a collection of podophyllotoxine indolo-analogues to identify chemical inhibitors of the CK2 subunit interaction. We report the identification of a podophyllotoxine indolo-analogue as a chemical ligand that binds to the CK2alpha/CK2beta interface inducing selective disruption of the CK2alpha/CK2beta assembly and concomitant inhibition of CK2alpha activity.

Domains

Cancer

Dates and versions

inserm-00413239 , version 1 (03-09-2009)

Identifiers

Cite

Béatrice Laudet, Virginie Moucadel, Renaud Prudent, Odile Filhol, Yung-Sing Wong, et al.. Identification of chemical inhibitors of protein-kinase CK2 subunit interaction.. Molecular and Cellular Biochemistry, 2008, 316 (1-2), pp.63-9. ⟨10.1007/s11010-008-9821-6⟩. ⟨inserm-00413239⟩
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