Pin1 peptidyl-prolyl isomerase polypeptides, their crystal...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/90 (2006.01)

Patent

CA 2491591

Polypeptides containing the PIN1 peptidyl-prolyl isomerase domain but not containing the PIN1 WW domain are described. Also described are crystal structures of these polypeptides, including the crystal structure of a PIN1 PPlaseaigand complex. The structure coordinate data derived from these crystals provides a three-dimensional description of the substrate-binding site of PIN1 peptidyl-prolyl isomerase useful in drug discovery and design for the identification and design of modulators of PIN1 peptidyl-prolyl isomerase activity.

L'invention concerne des polypeptides contenant le domaine d'isomérase peptidyl-prolyl PIN1 mais ne contenant pas le domaine WW PIN1. L'invention concerne également des structures cristallines de ces polypeptides, notamment la structure cristalline d'un complexe PPIase:ligand PIN1. Les coordonnées structurales dérivées desdits cristaux permettent d'obtenir une description tridimensionnelle du site de liaison du substrat de l'isomérase peptidyl-prolyl PIN1 utile dans la découverte et la conception de médicaments permettant d'identifier et de concevoir des modulateurs de l'activité d'isomérase peptidyl-prolyl PIN1.

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