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Mutations in the G Protein Coupled Receptor (GPCR) Gene Family in Melanoma

Posted Feb 03 2013 7:00pm

Description of Invention:
Using exon capture and next generation sequencing approaches to analyze the entire G protein coupled receptor (GPCR) gene family in melanoma, the researchers at the NIH have identified several novel somatic (e.g., tumor-specific) alterations. GPCRs play an integral part in regulating physiological functions and the importance of these molecules is evident by the fact that approximately half of the current FDA approved therapeutics target GPCRs or their direct downstream signaling components.

Many of the GPCR gene mutations identified by the NIH researchers were mutated in a large portion of melanoma patients and already have inhibitors, the most notable being the Glutamate Receptor Metabotropic 3 (GRM3) mutation which could be functionally signification for melanoma tumorigenesis. Therefore, this technology could aid in the development of specific inhibitors of GRM3 as well as the pathway it activates, mitogen-activated protein kinase (MEK), for the treatment of melanoma patients with these mutations. To complement these findings, human melanoma metastatic cell lines harboring GRM3 mutations are also available for licensing.

  • Diagnostic array for the detection of GRM3 mutations.
  • Method of identifying GRM3 inhibitors as therapeutic agents to treat malignant melanoma patients.
  • In vitro and in vivo cell model for the GRM3 mutation in melanoma. This is a useful tool for investigating GRM3 phenotype biology, including growth, motility, invasion, and metabolite production.

  • GPCR mutations, GRM3 in particular, are frequent in melanomas.
  • Several inhibitors to GPCR and MEK are already in clinical trials, thus this technology may prove useful for the development of novel diagnostic tests and therapeutics.
  • Associated cell lines derived from melanoma patients are available.

Development Status:

Yardena R Samuels (NHGRI)
Todd D Prickett (NHGRI)
Steven A Rosenberg (NCI)

Patent Status:
HHS, Reference No. E-244-2010/0
PCT, Application No. PCT/US2011/052032 filed 16 Sep 2011
HHS, Reference No. E-029-2012/0 — Research Tool. Patent protection is not being pursued for the GRM3 melanoma metastatic cell lines.

Related Technologies:
US, Application No. 61/462,471 filed 02 Feb 2011, Reference No. E-013-2011/0
PCT, Application No. PCT/US2012/022687 filed 26 Jan 2012, Reference No. E-013-2011/0
EIR, Reference No. E-024-2012/0 — Research Tool. Patent protection is not being pursued for this technology.
US, Application No. 61/199,156 filed 12 Nov 2008, Reference No. E-272-2008/0
US, Application No. 13/128,125 filed 06 May 2011, Reference No. E-272-2008/0
EIR, Reference No. E-229-2010/0 — Research Tool. Patent protection is not being pursued for this technology.
EIR, Reference No. E-232-2010/0 — Research Tool. Patent protection is not being pursued for this technology.

Relevant Publication:
  1. Prickett TD, et al. [ PMID 21946352 ]

Collaborative Research Opportunity:
The NHGRI is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize this technology. For collaboration opportunities, please contact Claire Driscoll, Director, NHGRI Technology Transfer Office, at or 301-594-2235.

For Licensing Information Please Contact:
Whitney Hastings
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-451-7337
Fax: 301-402-0220

Ref No: 2520

Updated: 02/2013

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