Rational Design of Antibiotics Targeted at the Ribosome

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$1,205,000.00
Award Year:
2004
Program:
SBIR
Phase:
Phase II
Contract:
2R44AI051104-02A1
Award Id:
60497
Agency Tracking Number:
AI051104
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
3115 MERRYFIELD ROW, SAN DIEGO, CA, 92121
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
THOMAS HERMANN
(858) 530-3659
THERMANN@ANADYSPHARMA.COM
Business Contact:
KLEANTHIS XANTHOPOULOS
(858) 530-3600
KGX@ANADYSPHARMA.COM
Research Institution:
n/a
Abstract
DESCRIPTION (provided by applicant): Rapid and widespread emergence of antibiotics-resistant pathogens creates an urgent need for concerted approaches towards novel antiinfectives. The long-term objective of this proposal is the development of novel potent antibacterials that target the ribosomal RNA (rRNA) of antibiotics-resistant bacteria. Specifically, a lead series of small molecules that recognize the ribosomal decoding-site RNA (A-site) will be developed to select an antibacterial drug candidate by iterative rounds of synthesis and testing for target binding, inhibition of protein synthesis and bacterial growth. The ribosomal A-site constitutes a prime target for antibiotics, validated by the naturally occurring aminoglycosides and a novel series of chemically unrelated antibacterials that we have discovered recently. Rational structure-based design along with multi-dimensional drug optimization, using testing data from a range of biochemical and biological assays, will allow us to develop a novel class of antibiotics that are not susceptible to known bacterial resistance mechanisms. These novel antibacterial A-site ligands will constitute the first class of antibiotics that has been developed by a rational approach of drug discovery specifically directed at an RNA component of the bacterial ribosome.

* information listed above is at the time of submission.

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