C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/00 (2006.01) C07K 14/47 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2429196
The present invention discloses characterization of interactions between ligands and Hsp90 proteins, including GRP94, wherein ligand binding to the N- terminal nucleotide binding domain of GRP94 elicits a conformational change that converts the GRP94 from an inactive to an active conformation, and wherein the chaperone and peptide-binding activities of the GRP94 are markedly stimulated. Also disclosed are purification, screening, and therapeutic methods pertaining to the biological activity of GRP94, and in some instances HSP90, based upon the characterization of ligand interactions of Hsp90 peptide- binding proteins, including GRP94.
La présente invention concerne la caractérisation d'interactions entre des ligands et des protéines Hsp90, telles que GRP94. Le ligand se liant au domaine de liaison nucléotidique N-terminal de GRP94 entraîne une modification conformationnelle qui convertit la conformation inactive de GRP94 en une conformation active, les activités de liaison peptidique et de la chaperone de GRP94 étant fortement stimulées. L'invention concerne également des méthodes de purification, de criblage et de traitement associées à l'activité de GRP94, et dans certains cas de HSP90, sur la base de la caractérisation des interactions de ligands avec des protéines de liaison peptidique Hsp90, telles que GRP94.
Nicchitta Christopher V.
Reed Robyn C.
Rosser Meredith F. N.
Wassenberg James J.
Duke University
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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