Selecting ligand agonists and antagonists
US5506107A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 29, 1993 |
| Grant date | Apr 9, 1996 |
| Priority date | — |
| Expiry date | Sep 29, 2013 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2333/61
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
We have discovered that growth hormones form ternary complexes with their receptors in which site 1 on the hormone first binds to one molecule of receptor and then hormone site 2 then binds to another molecule of receptor, thereby producing a 1:2 complex. We believe this phenomenon is shared by other ligands having similar conformational structure. Assays based on this phenomenon are useful for identifying ligand agonists and antagonists. Sites 1 and 2 are structurally identified to facilitate generation of amino acid sequence variants of ternary complex-forming ligands. Novel variants of growth hormone, prolactin placental lactogen and other related ligands are provided. As a result of our studies with the ternary complex we have determined that selected antibodies to the receptor for these ligands are capable of acting as ligand agonists or antagonists. Novel growth hormones and novel uses for anti-growth hormone receptor antibodies are described.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.