期刊
EXPERT OPINION ON DRUG DISCOVERY
卷 16, 期 10, 页码 1149-1161出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/17460441.2021.1922385
关键词
ProTide; phosphor(n)amidate; prodrugs; pro-nucleotide; nucleoside analogues; anticancer; antiviral
资金
- Chris McGuigan's laboratory at Cardiff University
- Bristol-Myers Squibb [INX-08189]
- NuCana PLC [NUC3373, NUC7738]
- Cerecor (Ichorion Therapeutics and Demeter Therapeutics)
- Bioberica
- Inhibitex inc.
The ProTide technology, a phosphate prodrug method, has been successful in delivering new antiviral drugs and shows promise in oncology. Its application to non-nucleoside-based small molecules is emerging and proving effective in various therapeutic areas. Investigations to explain the lack of activity of certain ProTide series and comprehensive structure activity relationship studies are deemed necessary for the future development of these compounds.
Introduction: The ProTide technology is a phosphate (or phosphonate) prodrug method devised to deliver nucleoside monophosphate (or monophosphonate) intracellularly bypassing the key challenges of antiviral and anticancer nucleoside analogs. Three new antiviral drugs, exploiting this technology, have been approved by the FDA while others are in clinical studies as anticancer agents. Areas covered: The authors describe the origin and development of this technology and its incredible success in transforming the drug discovery of antiviral and anticancer nucleoside analogues. As evidence, discussion on the antiviral ProTides on the market, and those currently in clinical development are included. The authors focus on how the proven capacity of this technology to generate new drug candidates has stimulated its application to non-nucleoside-based molecules. Expert opinion: The ProTide approach has been extremely successful in delivering blockbuster antiviral medicines and it seems highly promising in oncology. Its application to non-nucleoside-based small molecules is recently emerging and proving effective in other therapeutic areas. However, investigations to explain the lack of activity of certain ProTide series and comprehensive structure activity relationship studies to identify the appropriate phosphoramidate motifs depending on the parent molecule are in our opinion mandatory for the future development of these compounds.
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