A novel assay for RNA targeted drugs

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$285,505.00
Award Year:
2011
Program:
STTR
Phase:
Phase I
Contract:
1R41GM097917-01A1
Award Id:
n/a
Agency Tracking Number:
R41GM097917
Solicitation Year:
2011
Solicitation Topic Code:
NIGMS
Solicitation Number:
PA10-051
Small Business Information
900 B West Faris Road, Greenville, SC, 29605-1804
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
831389122
Principal Investigator:
DEV ARYA
(864) 656-1106
dparya@clemson.edu
Business Contact:
DEV ARYA
(864) 207-0002
nubadllc@gmail.com
Research Institution:
CLEMSON UNIVERSITY

CLEMSON UNIVERSITY
OFFICE OF SPONSORED PROGRAMS 300 BRACKETT HALL BOX 345702
CLEMSON, SC, 29634-5702
() -
Nonprofit college or university
Abstract
DESCRIPTION (provided by applicant): NUBAD, LLC is a drug discovery company devoted to identifying therapeutic agents that target nucleic acids. This project is designed to synthesize and characterize a novel class of fluorescently-labeled aminoglycosidesthat exhibit a dramatic change in fluorescence upon RNA binding. Aminoglycosides are a potent class of antibiotics that block bacterial protein synthesis by binding to a conserved site on ribosomal RNA. It is the purpose of the project to develop an innovative fluorescence-based screen for A-site targeted drugs for rapid screening of RNA binding antibacterials. PUBLIC HEALTH RELEVANCE: The aminoglycoside class of antibiotics block bacterial protein synthesis by binding a conserved site on ribosomal RNA. These antibiotics are clinically important agents that combat a broad spectrum of bacterial infections but can cause serious side effects such as kidney damage and hearing loss. The emergence of antibiotic resistance and high level of toxicity associated with the current arsenal of drugs demands the development of efficient methods of screening for novel antibiotics with the desirable properties of high potency and low toxicity. NUBAD, LLC, Pendleton, SC in collaboration with PI's lab, Clemson University, SC, has recently identified a fluorescent neomycin conjugate that is being used to probe drug binding to RNA targets. This proposal describes a phase I project that will determine the technical and scientific feasibility of using a fluorescent-neomycinprobe in an innovative screen suitable for a high-throughput screen for new aminoglycoside based antibiotics. This phase I application will develop the probe for high throughput applications and then use the targeted screen to check for assay robustness. Selected compounds will then be checked for antibacterial activity and mechanism of action.

* information listed above is at the time of submission.

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