Rat cathepsin, dipeptidyl peptidase i (dppi): crystal...

C - Chemistry – Metallurgy – 12 – N

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Details

C12N 15/57 (2006.01) A61P 11/00 (2006.01) A61P 31/00 (2006.01) C07K 1/14 (2006.01) C07K 14/435 (2006.01) C12N 9/48 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2422057

The present invention relates to structural studies of dipeptidyl peptidase I (DPPI) proteins, modified dipeptidyl peptidase I (DPPI) proteins and DPPI co- complexes. Included in the present invention is a crystal of a dipeptidyl peptidase I (DPPI) and corresponding structural information obtained by X-ray crystallography from rat and human DPPI. In addition, this invention relates to methods for using structure co-ordinates of DDPI, mutants hereof andco- complexes, to design compounds that bind to the active site or accessory binding sites of DPPI and to design improved inhibitors of DPPI or homologues of the enzyme.

L'invention concerne des études structurelles de protéines peptidase dipeptidyl I (DPPI), des protéines peptidase dipeptidyl I (DPPI) modifiées et des co-complexes DPPI. L'invention concerne également un cristal de peptidase dipeptidyl I (DPPI) et les informations structurelles correspondantes obtenues par cristallographie aux rayons X à partir de DPPI d'humain et de rat. De plus, l'invention concerne des procédés d'utilisation de coordonnées structurelles de DPPI, de mutants de ceux-ci et de co-complexes, afin de concevoir des composants qui se lient au site actif ou à des sites de liaison secondaires de DPPI et de réaliser des inhibiteurs améliorés de DPPI ou des homologues de l'enzyme.

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