SPECIFIC ACTIVE SITE INHIBITORS OF ENZYMES OR SUBSTRATE BINDING PARTNERS AND METHODS OF PRODUCING SAME
摘要
The present disclosure provides a method of producing enzyme- specific inhibitors or substrate binding partners comprising: identifying active site residues of the substrate in the enzyme substrate complex or in substrate binding partner-substrate complex; randomizing the active site residues to produce a combinatorial library of substrate variants; and selecting substrate variants that inhibit enzyme activity or bind substrate as substrate-specific binding partners. The present disclosure also provides ubiquitin enzyme specific inhibitors and ubiquitin variants that bind ubiquitin interaction motifs.
申请公布号
WO2012020289(A2)
申请公布日期
2012.02.16
申请号
WO2011IB01663
申请日期
2011.06.08
申请人
THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO;SIDHU, SACHDEV;BEATTY, LINDA;ERNST, ANDREAS