# SPECIFICITY OF INTERCALATION REACTIONS

> **NIH NIH R01** · UNIVERSITY OF MISSISSIPPI MED CTR · 1989 · $76,452

## Abstract

The long-range goal of the proposed research is to understand in
molecular detail the sequence and conformational specificity of
intercalcation reactions involving clinically important antibiotics.
It is anticipated that information obtained in the proposed
research will be of direct use in the rational design of new
intercalating drugs with enhanced potency and specificity.  The
clinically important anthracycline antibiotics and a series of novel
anthrapyrazole antibiotics will be studied.  A quantitative
deoxyribonuclease footprinting method will be implemented and
exploited to obtain microscopic binding constants describing the
interaction of these compounds with specific DNA binding.
Stopped-flow and temperature-jump kinetic methods will be used
to obtain data of use toward formulating a pluasible reaction
mechanism describing the process by which an antibiotic molecule
finds and interacts with its specific DNA binding site.
Deoxyribonuclease footprinting and spectroscopic methods will be
used to examine the interaction of intercalators with B-Z
junctions and bends in DNA, in order to see if such regions are
high affinity binding sites for intercalating drugs.  Mechanistic
studies of intercalators as allosteric effectors of DNA
conformation will continue, emphasizing kinetic studies of the
effect of intercalcators on the B to Z transition in DNA.  The
fundamental thermodynamics and kinetics of the interaction of a
series of novel anthrapyrazole antibiotics with DNA will be
examined.  The combined results of these studies will provide
fundamental details essential for understanding the intercalation
process, an important reaction by which many clinically useful
antibiotics interact with their prime cellular target, DNA.

## Key facts

- **NIH application ID:** 3173229
- **Project number:** 5R01CA035635-05
- **Recipient organization:** UNIVERSITY OF MISSISSIPPI MED CTR
- **SAM.gov UEI:** X59NJBFL8BJ3
- **Principal Investigator:** Jonathan B. CHAIRES
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1989
- **Award amount:** $76,452
- **Award type:** 5
- **Project period:** 1984-03-01 → 1991-01-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3173229

## Citation

> US National Institutes of Health, RePORTER application 3173229, SPECIFICITY OF INTERCALATION REACTIONS (5R01CA035635-05). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3173229. Licensed CC0.

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