Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends
摘要：
The early effectiveness of combinatorial antiretroviral therapy (cART) in the treatment of has been compromised to some extent by rapid development of multi-drug-resistant strains, poor bioavailability and cumulative toxicities, and so there is a need for alternative strategies of antiretroviral drug discovery and additional therapeutic agents with novel action modes or targets. From this perspective, we firstly review current strategies of antiretroviral drug discovery and optimization, with the aid of selected examples from the recent literature. We highlight the development of phosphate -based prodrugs as a means to improve the aqueous solubility of inhibitors, and the introduction of the substrate hypothesis as a new approach for overcoming drug resistance. Finally, we discuss future directions for research, including opportunities for exploitation of novel antiretroviral targets, and the strategy of activation of latent reservoirs as a means to eradicate the virus.
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DOI：
10.1021/acs.jmedchem.5b00497
被引量：
年份：
2015
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