Constitutively active histamine H3 receptor mutants and uses thereof
US7279293B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 23, 2003 |
| Grant date | Oct 9, 2007 |
| Priority date | — |
| Expiry date | Jul 30, 2023 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2500/00
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
Internal domain 3 of seven transmembrane G protein-coupled receptors is important for G protein binding or receptor activity, and is well conserved. In H3 receptors, which are a type of G protein-coupled receptor, this region is also conserved in the same way. Therefore, as a result of using PCR to introduce point mutations into sequences encoding the region in H3 receptor cDNA, H3 receptor mutants comprising extremely strong constitutive activity could be successfully produced. The present inventors further found that by using constitutively active H3 receptor mutants, drug candidate compounds such as H3 receptor inverse agonists can be screened more easily and efficiently.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.