Fiscal Year:
2001
Title:
DEVELOPMENT OF MULTI-RECEPTOR LC STATIONARY PHASES
Agency:
HHS
Contract:
PHS2001-2
Award Amount:
$100,000.00
Abstract:
DESCRIPTION: (Applicant's description) Combinatorial methods for the synthesis
of new drug substances require high throughput techniques for evaluation of
structure-activity relationships. Microliter plates with immobilized target
receptors can rapidly reduce thousands of possibilities to hundreds of
candidates. The next level of screening has proven to be more difficult and
tedious. The goal of this project is the creation of an on-line screening
approach to expedite secondary screening. The new technology involves
immobilized bipolymer HPLC columns (IBCs)containing immobilized multiple
receptors. Test compounds will be injected onto the IBC and chromatographed
using standard HPLC techniques. The compounds will differentially adhere to the
IBC according to their relative affinity for the immobilized receptors, i.e.
compounds with little or no affinity to their relative affinity will wash
through the IBC while those with moderate affinities will be displaced by ones
with higher binding constants. The bipolymer-bound compounds will be
sequentially displaced using a characterized ligand and the liberated compounds
directed on-line into a mass spectrometer. Thus a large series of compounds can
be rapidly screened for their relative affinities for the immobilized receptors
with concurrent identification of molecular structures. The objective of this
project is to develop prototypic IBCs using GABA, and nicotinic receptors.
PROPOSED COMMERCIAL APPLICATION:
The immobilized bipolymer columns (IBC's) developed in this project represent a new
product for use in the pharmaceutical industry. A series of IBC's will be created for use
in combinatorial screens and should find a substantial market as part of a high-throughput
screen for new drug substances.
Small Business Information at Submission:
MOLECULAR DESIGN INTERNATIONAL
BOX 41777, 131 GAYOSO LN MEMPHIS, TN 38174 MEMPHIS, TN 38103
EIN/Tax ID:
621019562
DUNS:
N/A
Number of Employees:
N/A
Woman-Owned:
No
Minority-Owned:
No
HUBZone-Owned:
No
Research Institution Information:
GEORGETOWN UNIVERSITY MEDICAL CENTER
GEORGETOWN UNIVERSITY MEDICAL CENTER
WASHINGTON, DC 20057
RI Type:
Nonprofit college or university