Assay to identify human C5a antagonists and agonists
US5614370A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 18, 1994 |
| Grant date | Mar 25, 1997 |
| Priority date | — |
| Expiry date | Mar 18, 2014 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K38/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention is an assay, including a series of peptides, which allow screening for inhibitors of C5a binding targeted to the subsite on the C5a receptor occupied by the C-terminus of C5a. These peptides allow compound testing efforts to be targeted to this same subsite so that C5a agonists and antagonists can be identified. These peptides have much greater affinity (Ki<10 nM) than does the natural C-terminus of C5a (Ki=300 .mu.M) and have been labeled to allow for detection of molecules which inhibit binding of these peptides at this receptor subsite. The invention is useful to develop agonists, partial agonists, and antagonists of C5a, and the invention includes compounds identified according to the method of this invention and methods of their use.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.