# BETA-LACTAMASES--ACTIVE SITE CHEMISTRY

> **NIH NIH R01** · WESLEYAN UNIVERSITY · 1989 · $114,914

## Abstract

Bacterial resistance to Beta-lactam antibiotics continues to become more
prevalent and more clinically important.  It is likely, however, that a
large part of the resistance can be understood and investigated
experimentally in terms of the chemistry of the interactions of Beta-lactam
antibiotics with the active sites of two groups of bacterial enzymes, the
Beta-lactamases on one hand, which catalyse the hydrolysis of the
antibiotics, and the D-alanyl-D-alanine transpeptidase/carbgoxypeptidases
on the other, which catalyze the synthesis and maintenance of the peptide
cross-links of bacterial cell walls, and which are inhibited by Beta-lactam
antibiotics.  There is now good reasons to believe that all of the
Beta-lactam binding sites have much in common.  An understanding of the
structure and function of the sites and of the relationship between them is
fundamental to future antibiotic design -- both Beta-lactam and otherwise.
The object of the proposed research is to explore further the chemical
functionality and conformational adaptability of a series of the active
sites, using a number of modified substrates, novel inhibitors, and
potential effectors.  These studies should lead to a more useful picture of
Beta-lactamase active sites, a better idea as to their relationship to
D-alanyl-D-alanine transpeptidase sites, and thus to new directions of
antibiotic development.

## Key facts

- **NIH application ID:** 3127596
- **Project number:** 5R01AI017986-08
- **Recipient organization:** WESLEYAN UNIVERSITY
- **SAM.gov UEI:** ZETJL6DKF963
- **Principal Investigator:** REX F PRATT
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1989
- **Award amount:** $114,914
- **Award type:** 5
- **Project period:** 1982-09-30 → 1990-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3127596

## Citation

> US National Institutes of Health, RePORTER application 3127596, BETA-LACTAMASES--ACTIVE SITE CHEMISTRY (5R01AI017986-08). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3127596. Licensed CC0.

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