激酶的遗传变异和核苷酸类似物逆转录酶抑制剂替诺福韦的激活。
Genetic variation of kinases and activation of nucleotide analog reverse transcriptase inhibitor tenofovir.
机构信息
Department of Medicine (Division of Clinical Pharmacology), Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA.
出版信息
Pharmacogenomics. 2019 Jan;20(2):105-111. doi: 10.2217/pgs-2018-0140. Epub 2019 Jan 10.
Abstract
As antiretroviral therapy has become more accessible across the world and coformulations have improved patient compliance; the morbidity and mortality of HIV/AIDS has decreased. However, there is still a substantial gap in knowledge regarding the impact of genetic variation on the metabolism of and response to some of the most commonly prescribed antiretrovirals, including the nucleotide reverse transcriptase inhibitor tenofovir. While it has been scientifically established that tenofovir must be activated to be efficacious against HIV, the enzymes responsible for this activation have not been well characterized. The purpose of this review is to summarize and clarify the scientific knowledge regarding the enzymes that phosphorylate and activate this clinically important drug.
摘要
随着抗逆转录病毒疗法在全球范围内的普及和复方制剂提高了患者的依从性，艾滋病毒/艾滋病的发病率和死亡率已经下降。然而，对于遗传变异对一些最常用的抗逆转录病毒药物（包括核苷酸逆转录酶抑制剂替诺福韦）的代谢和反应的影响，仍存在很大的知识差距。虽然已经从科学上确定替诺福韦必须被激活才能有效地对抗艾滋病毒，但负责这种激活的酶尚未得到很好的描述。本综述的目的是总结和澄清有关使这种临床重要药物磷酸化和激活的酶的科学知识。
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