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Published on: December 27, 2016
Minor groove binders as anti-infective agents
Michael P Barrett1, Curtis G Gemmell, Colin J Suckling
1Wellcome Trust Centre for Molecular Parasitology, Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, Sir Graeme Davies Building University of Glasgow, 120 University Place, Glasgow, G12 8TA, Scotland, United Kingdom. michael.barrett@glasgow.ac.uk
Pharmacology & Therapeutics
|March 20, 2013
Summary
Minor groove binders are DNA-interacting molecules with growing therapeutic applications. Their structural diversity allows for selective targeting of various infectious organisms, offering promising anti-infective drug development prospects.
Area of Science:
- Medicinal Chemistry
- Molecular Biology
- Pharmacology
Background:
- Minor groove binders are small molecules that interact with the DNA minor groove.
- Structural classes include distamycin/netropsin analogues, oligoamides, and bis-amidines.
- These molecules exhibit helical structures complementary to DNA minor groove curvature.
Purpose of the Study:
- To review the pharmaceutical significance of minor groove binders.
- To highlight their applications in anti-cancer and anti-infective therapies.
- To discuss the growing sophistication and potential of oligoamide-based binders.
Main Methods:
- Review of existing literature on minor groove binders.
- Analysis of structural diversity and DNA binding selectivity.
- Examination of therapeutic applications and emerging trends.
Main Results:
- Minor groove binders show significant anti-cancer and anti-infective properties.
- Oligoamide class binders demonstrate increasing sequence selectivity and diverse activities (antibacterial, antifungal, antiviral, antiparasitic).
- Structural variations influence activity and selectivity, with differing optimal structures for various pathogens.
Conclusions:
- Minor groove binders represent a promising class of therapeutic agents.
- Advancements in oligoamide design enable high sequence selectivity for targeted therapies.
- Further research into mechanisms of action and cell penetration is crucial for developing novel anti-infective drugs.
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