Abstract: Farnesyl pyrophosphate, the metabolically active form of farnesol, is a key precursor in the synthesis of cholesterol, carotenoids, steroid hormones, bile acids and other molecules involved in cellular growth and metabolism. A nuclear receptor has been identified that is transcriptionally activated by farnesol and related molecules. This novel signaling pathway can be modulated by the use of key metabolic intermediates (or analogs and/or derivatives thereof) as transcriptional regulatory signals.
Type:
Grant
Filed:
October 24, 2000
Date of Patent:
July 9, 2002
Assignees:
The Salk Institute for Biological Studies, Ligand Pharmaceuticals, Inc., The Government of the United States of America
Inventors:
Ronald M. Evans, Barry M. Forman, Cary A. Weinberger
Abstract: In accordance with the present invention, there are provided new members of the steroid receptor superfamily of receptors, a representative member of which has been designated XOR-6. Invention receptors are responsive to hydroxy, mercapto or amino benzoates, and are expressed, for example, in Xenopus laevis embryos. XOR-6 is most closely, although distantly, related to the vitamin D3 receptor (VDR). The proteins are about 73% identical in amino acid sequence in the DNA-binding domains and about 42% identical in the ligand binding domain. Like VDR, XOR-6 has an extended D region between the DNA and ligand binding domains. Notably, the region amino-terminal to the XOR-6 DNA-binding domain is extremely acidic. This may influence its ability to activate target genes. XOR-6 is not restricted to Xenopus because southern blots show the presence of XOR-6-related sequences in a variety of other vertebrates. Indeed, a human genomic clone for an XOR-6 related gene has recently been isolated.
Type:
Grant
Filed:
July 17, 1997
Date of Patent:
May 21, 2002
Assignee:
The Salk Institute for Biological Studies
Inventors:
Ronald M. Evans, Bruce Blumberg, Kazuhiko Umesono
Abstract: Methods are presented whereby regional pain relief is achieved through the periodic topical administration of compositions comprising NMDA receptor antagonists, by applying said compositions to the skin above areas affected by pain.