An overview of ProTide technology and its implications to drug discovery

Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910 and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101 2021. An overview of ProTide technology and its implications to drug discovery. Expert Opinion on Drug Discovery 16 (10) , 1149--1161. 10.1080/17460441.2021.1922385

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Abstract

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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy Chemistry
Publisher:	Taylor and Francis
ISSN:	1746-0441
Date of First Compliant Deposit:	18 June 2021
Date of Acceptance:	22 April 2021
Last Modified:	03 May 2023 21:18
URI:	https://orca.cardiff.ac.uk/id/eprint/141977

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