Department of Microbiology and Immunology, Rega Institute for Medical Research, Medical School University of Leuven, Belgium.
Annu Rev Pharmacol Toxicol. 2011;51:1-24. doi: 10.1146/annurev-pharmtox-010510-100228.
My search for a selective antiviral chemotherapy started more than 40 years ago with interferon inducers, then shifted to nucleoside analogs with the discovery of BVDU (brivudin), a highly selective anti-HSV-1 and anti-VZV agent, and to dideoxynucleoside analogs such as d4T (stavudine), anti-HIV agents. The search culminated in the discovery of acyclic nucleoside phosphonates (ANPs) (in collaboration with Antonin Holý), a key class of compounds active against HIV, hepatitis B virus, and DNA viruses at large; the best known of these compounds is tenofovir. Along the way, the principle of the non-nucleoside reverse transcriptase inhibitors (NNRTIs) was established. This work, initiated in collaboration with the late Paul A.J. Janssen, eventually led to the identification of rilpivirine as perhaps an "ideal" NNRTI.
我的选择性抗病毒化疗研究始于 40 多年前的干扰素诱导剂，然后随着 BVDU（溴夫定）的发现而转向核苷类似物，BVDU 是一种高度选择性的抗单纯疱疹病毒 1 型和水痘带状疱疹病毒药物，随后又转向了核苷类似物如 d4T（司他夫定）等抗 HIV 药物。研究最终以发现无环核苷膦酸酯 (ANPs)（与 Antonin Holý 合作）为高潮，这是一类对抗 HIV、乙型肝炎病毒和 DNA 病毒的关键化合物；其中最著名的化合物是替诺福韦。在此过程中，确立了非核苷逆转录酶抑制剂 (NNRTIs) 的原理。这项与已故的 Paul A.J. Janssen 合作开展的工作，最终促成了利匹韦林被确定为一种“理想”的 NNRTI。
