2023-10-20
Exploring novel <scp>HIV</scp>‐1 reverse transcriptase inhibitors with drug‐resistant mutants: A double mutant surprise
2023-10-20 • Klarissa Hollander, Albert H. Chan, Kathleen M. Frey, Olivia Hunker, Joseph A. Ippolito, Krasimir A. Spasov, Yang-Hui Jimmy Yeh, William L. Jorgens...
Abstract HIV‐1 reverse transcriptase (RT) remains a key target for HIV drug development. As successful management of the disease requires lifelong treatment, the emergence of resistance mutations is inevitable, making development of new RT inhibitors, which remain effective against resistant variants crucial. To this end, previous computationally guided drug design efforts have resulted in catechol diether compounds, which inhibit wildtype RT with picomolar affinities and appear to be promising preclinical candida…