A new antiviral: Chimeric 3TC-AZT phosphonate efficiently inhibits HIV-1 in human tissues ex vivo

作者：Vanpouille Christophe; Khandazhinskaya Anastasia; Karpenko Inna; Zicari Sonia; Barreto de Souza Victor; Frolova Svetlana; Margolis Leonid^*; Kochetkov Sergey

来源：Antiviral Research, 2014, 109: 125-131.

DOI：10.1016/j.antiviral.2014.06.019

• HIV-1
• NRTI
• Depot form

Although more-recently developed antivirals target different molecules in the HIV-1 replication cycle, nucleoside reverse transcriptase inhibitors (NRTIs) remain central for HIV-1 therapy. Here, we test the anti-HIV activity of a phosphonate chimera of two well-known NRTIs, namely AZT and 3TC. We show that this newly synthesized compound suppressed HIV-1 infection in lymphoid tissue ex vivo more efficiently than did other phosphonates of NRTIs. Moreover, the new compound was not toxic for tissue cells, thus making the chimeric phosphonate strategy a valid approach for the development of anti HIV-1 compound heterodimers. Published by Elsevier B.V.

• 出版日期2014-9
• 单位NIH