Pace Paola, Rowley Michael
IRBM, via Pontina Km 30,600, Pomezia, Rome 00040, Italy.
Curr Opin Drug Discov Devel. 2008 Jul;11(4):471-9.
HIV-1 integrase catalyzes the insertion of HIV-1 DNA into the genome of the host cell and, therefore, represents a rational target for chemotherapeutic intervention in the treatment of HIV-1 infection. Raltegravir, marketed as Isentress, is the first integrase inhibitor to be approved by the FDA for the treatment of HIV AIDS infection. This review briefly describes the successful medicinal chemistry efforts that culminated in the discovery of raltegravir, and highlights more recent progress that has been made in the field of HIV-1 integrase inhibition.
HIV-1整合酶催化HIV-1 DNA插入宿主细胞基因组，因此是抗HIV-1感染化疗干预的合理靶点。作为Isentress上市的拉替拉韦是首个获美国食品药品监督管理局（FDA）批准用于治疗HIV艾滋病感染的整合酶抑制剂。本文简要介绍了最终促成拉替拉韦发现的成功药物化学研究工作，并重点介绍了HIV-1整合酶抑制领域的最新进展。
