Journal
NATURE REVIEWS DRUG DISCOVERY
Volume 11, Issue 1, Pages 25-36Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd3404
Keywords
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Funding
- Center for Cancer Research, the National Cancer Institute, US National Institutes of Health
- NATIONAL CANCER INSTITUTE [ZIABC006161, ZIABC006150, ZIABC007333] Funding Source: NIH RePORTER
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Interfacial inhibitors belong to a broad class of natural products and synthetic drugs that are commonly used to treat cancers as well as bacterial and HIV infections. They bind selectively to interfaces as macromolecular machines assemble and are set in motion. The bound drugs transiently arrest the targeted molecular machines, which can initiate allosteric effects, or desynchronize macromolecular machines that normally function in concert. Here, we review five archetypical examples of interfacial inhibitors: the camptothecins, etoposide, the quinolone antibiotics, the vinca alkaloids and the novel anti-HIV inhibitor raltegravir. We discuss the common and diverging elements between interfacial and allosteric inhibitors and give a perspective for the rationale and methods used to discover novel interfacial inhibitors.
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