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Hydroxyl radical mapping of protein interfaces

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: PHS2001-2
Agency Tracking Number: 1R41GM064318-01
Amount: $100,000.00
Phase: Phase I
Program: STTR
Solicitation Topic Code: N/A
Solicitation Number: N/A
Timeline
Solicitation Year: N/A
Award Year: 2001
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
344 VIRGINIA AVE SAN MATEO, CA 94402
SAN MATEO, CA 94402
United States
DUNS: N/A
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 VERNON ANDERSON
 (216) 368-2599
 VEA@PO.CWRU.EDU
Business Contact
Phone: (650) 344-2664
Email: DHOUCK@CARTAPHARMA.COM
Research Institution
N/A
Abstract

DESCRIPTION (provided by applicant): Identifying amino acid residues of a
protein that form the binding site for a drug, or that are present at the
interface in a protein-protein complex are difficult to identify from the
crystal structures of the individual partner proteins. Carta Proteomics is
committed to the premise that monitoring isotope exchange into proteins by mass
spectrometry will permit the rapid identification of contact residues of
proteins that form macromolecular complexes. Prior work and proprietary
development has established amide-proton solvent exchange as one facet of Carta
Proteomics. This proposal is to develop a complementary method of hydroxyl
radical (-OH) induced 1I-TJ2H exchange into the aliphatic carbons of the amino
acid side chains. This proposal takes advantage of the basic underlying
chemistry that has been recently well characterized.
The goal of this proposal is to demonstrate the capability of this
chemistry to use the multiple binding sites present on thrombin to validate the
ability of this methodology to correctly identify the active site in a BABIM
thrombin complex and to identify the allosteric binding site for hirudin, an
inhibitory oligopeptide. This demonstration will validate the application of
the method to inhibitors identified from combinatorial chemistry screens.

PROPOSED COMMERCIAL APPLICATION:
Structure based drug design is severely hampered by the lack of a low-cost, rapid method of determining structure. Our technology of determining structures of a small molecule/protein target interaction can be easily adapted to high throughput and very fast turn-around at very low cost. Because of these unique features we expect the technology to be readily integrated into the small molecule drug discovery process. Carta Proteomics will participate by providing the proprietary expertise through research partnership agreements.

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

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