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G-Protein Coupled Receptor Nanostructure Pharmaceutics

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 1R41GM075362-01
Agency Tracking Number: GM075362
Amount: $369,056.00
Phase: Phase I
Program: SBIR
Solicitation Topic Code: N/A
Solicitation Number: PHS2005-2
Solicitation Year: 2005
Award Year: 2005
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
Urbana, IL 61801
United States
HUBZone Owned: Unavailable
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 (217) 244-6094
Business Contact
Phone: (217) 244-7395
Research Institution

DESCRIPTION (provided by applicant): Membrane proteins play critical functions in many if not most cellular and physiological processes. Single membrane proteins and their macromolecular assemblies are essential catalysts in the metabolism and conveyance of information and energy between cells and the external environment, between cellular compartments and in the interactions of cells with viral and other agents. Membrane proteins are vital to human health, specific defects can be associated with human disease and many are the targets of a large number of pharmacologically and toxicologically active substances. Recently we demonstrated that suitable engineered "membrane scaffold proteins" (MSPs) would self-assemble phospholipids and a variety of membrane protein targets into nanoscale discoidal bilayer structures. These nominally 10 nm diameter particles, termed Nanodiscs, are rendered soluble in aqueous solution via the amphipathic helical nature of the encircling MSP. We have also shown that the model seven-trans-membrane protein bacteriorhodopsin (bR) could be functionally solubilized and incorporated into homogeneous and monodisperse Nanodiscs. In this STTR application, we seek support for a synergistic collaboration of corporate and academic entities to extend these preliminary investigations to the important class of drug targets, the G-protein coupled receptors (GPCRs) and develop and commercialize this technology for use by the academic and pharmaceutical industry. We present enabling data on the human beta-2 adrenergic receptor and provide a research plan focused on defining a simple and robust procedure for solubilizing GPCRs into functional membrane bilayer Nanodiscs for use in elucidating the structure and function of membrane proteins critical to human health.

* Information listed above is at the time of submission. *

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