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The ProTide prodrug technology: from the concept to the clinic

Mehellou, Youcef, Rattan, Hardeep S. and Balzarini, Jan 2018. The ProTide prodrug technology: from the concept to the clinic. Journal of Medicinal Chemistry 61 (6) , pp. 2211-2226. 10.1021/acs.jmedchem.7b00734

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The ProTide technology is a prodrug approach developed for the efficient intracellular delivery of nucleoside analogue monophosphates and monophosphonates. In this approach, the hydroxyls of the monophosphate or monophosphonate groups are masked by an aromatic group and an amino acid ester moiety, which are enzymatically cleaved-off inside cells to release the free nucleoside monophosphate and monophosphonate species. Structurally, this represents the current end-point of an extensive medicinal chemistry endeavor that spans almost three decades. It started from the masking of nucleoside monophosphate and monophosphonate groups by simple alkyl groups and evolved into the sophisticated ProTide system as known today. This technology has been extensively employed in drug discovery, and it has already led to the discovery of two FDA-approved (antiviral) ProTides. In this work, we will review the development of the ProTide technology, its application in drug discovery, and its role in the improvement of drug delivery and efficacy.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Publisher: American Chemical Society
ISSN: 0022-2623
Date of First Compliant Deposit: 10 August 2017
Date of Acceptance: 9 August 2017
Last Modified: 18 Oct 2019 15:15

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