Methods and compositions for identifying receptor effectors

Details Methods and compositions for identifying receptor effectors Methods and compositions for identifying receptor effectors

C - Chemistry, Metallurgy

12

N

C12N 15/62 (2006.01) C07K 7/06 (2006.01) C07K 14/39 (2006.01) C07K 19/00 (2006.01) C12N 15/31 (2006.01) C12N 15/81 (2006.01) C12Q 1/02 (2006.01) C12Q 1/37 (2006.01) C12Q 1/68 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2266543

The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular protein, e.g., a receptor or ion channel. The subject assay enables rapid screening of large numbers of compounds to identify those which act as an agonist or antagonist to the bioactivity of the cellular protein. The subject assay is particularly amenable for identifying surrogate ligands for receptors especially from small molecule or peptide libraries or from peptides produced by an autocrine system. Identification can be achieved via activation of a yeast signalling pathway, specially the yeast pheromone system pathway.

L'invention concerne un essai rapide et efficace pour le criblage et l'identification de composés pharmaceutiquement efficaces ayant une intéraction spécifique avec l'activité d'une protéine cellulaire et modulant cette activité (par exemple, récepteur ou canal ionique). L'essai en question permet de cribler rapidement un grand nombre de composés, pour identifier parmi eux les agonistes ou les antagonistes de la bioactivité d'une protéine cellulaire. Ce type d'essai est particulièrement approprié à l'identification de substituts de ligands pour récepteurs, en particulier parmi les banques de molécules ou de peptides de petite taille ou parmi les peptides émanant d'un système autocrine.

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