Patent ID: 7625731
Filing Date: 2009-12-01
Classification: C07K,C12N,C30B

Abstract:
1. A crystallized polypeptide-ligand complex, comprising: a human aggrecanase-2 polypeptide comprising amino acid residues 262 to 628 of SEQ ID NO:3, and a ligand having the structure: wherein D and E represent an amide or a mimic thereof; wherein R 11 is methyl, ethyl or propyl, and wherein R 12 , R 13 , and R 14 is selected from the group consisting of a C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycyl, heterocyclyl, aryl, heteroaryl cyclyloxy, heterocyclyloxy, aryloxy, heteroaryloxy, cyclylthio, heterocyclylthio, arylthio, heteroarylthio, cyclylalkyl, heterocyclylalkyl, arylalkyl, and heteroarylalkyl; and G is a metal chelating moiety selected from the group consisting of a carboxylic acid, carboxylic amide and hydroxamic acid; and wherein the crystallized polypeptide-ligand complex has space group P3 1 and unit cell dimensions a=93.64 Å, b=93.64 Å, c=92.59 Å, and γ=120°.