前药核苷的热潮。
The ProTides Boom.
作者信息
Mehellou Youcef
机构信息
School of Pharmacy, College of Medical and Dental Sciences, University of Birmingham, Edgbaston, B15 2TT, UK.
出版信息
ChemMedChem. 2016 Jun 6;11(11):1114-6. doi: 10.1002/cmdc.201600156. Epub 2016 May 9.
Abstract
The masking of nucleoside phosphate and phosphonate groups by an aryl motif and an amino acid ester, nowadays known as the 'ProTide' technology, has proven to be effective in the discovery of nucleotide therapeutics. Indeed, this technology, which was invented by Chris McGuigan in the early 1990s, has inspired the discovery of two FDA-approved antiviral nucleotide drugs, and many more are currently undergoing (pre)clinical development. The usefulness of this technology in the discovery of nucleotide therapeutics is showcased in this Highlight by discussing the ProTides development and the various ProTides that have reached clinical trials.
摘要
如今被称为“前药核苷酸”技术的，通过芳基基序和氨基酸酯对核苷磷酸酯和膦酸酯基团进行的掩蔽，已被证明在核苷酸疗法的发现中是有效的。事实上，这项由克里斯·麦奎根在20世纪90年代初发明的技术，激发了两种获美国食品药品监督管理局批准的抗病毒核苷酸药物的发现，目前还有更多药物正在进行（前）临床开发。本综述通过讨论前药核苷酸的研发情况以及已进入临床试验的各种前药核苷酸，展示了该技术在核苷酸疗法发现中的实用性。
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