Avoiding Drug Resistance by Substrate Envelope Guided Design: Toward Potent and Robust HCV NS3/4A Protease Inhibitors

Leveraging our knowledge of the intermolecular interaction between HCV NS3/4A protease and its natural substrates, we designed improved inhibitors that display better potency against clinically relevant resistant variants of the virus. These lessons are transferable to the design of potent and robust inhibitors against other dug targets.

2. Matthew AN, Zephyr J, Rao DN, Henes M, Kamran W, Kosovrasti K, Hedger AK, Lockbaum GJ, Timm J, Ali A, Kurt Yilmaz N*, Schiffer CA “Avoiding Drug Resistance by Substrate Envelope Guided Design: Toward Potent and Robust HCV NS3/4A Protease Inhibitors” mBio, Vol.11, Iss. 2, e00172-20 (2020). (*joint corresponding author)