Patent · US Active

Specific active site inhibitors of enzymes and methods of producing same

US10214570B2 · kind B2 · utility

0Cited by

8References

8Claims

0Family size

Assignee

The Governing Council of the University of Toronto · CA

Inventors

Sachdev Sidhu · Toronto, CA
Linda Beatty · Toronto, CA
Andreas Ernst · Worms, DE

Key dates

Filing date	Jun 8, 2011
Grant date	Feb 26, 2019
Priority date	—
Expiry date	Jun 17, 2031

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07K14/47
WIPO fieldPharmaceuticals
WIPO sectorChemistry

Abstract

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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.