Macrocyclic Envelope Glycoprotein Antagonists that Irreversibly Inactivate HIV-1 before Host Cell Encounter

Journal of Medicinal Chemistry
Adel A RashadIrwin M Chaiken

Abstract

We derived macrocyclic HIV-1 antagonists as a new class of peptidomimetic drug leads. Cyclic peptide triazoles (cPTs) retained the gp120 inhibitory and virus-inactivating signature of parent PTs, arguing that cyclization locked an active conformation. The six-residue cPT 9 (AAR029b) exhibited submicromolar antiviral potencies in inhibiting cell infection and triggering gp120 shedding that causes irreversible virion inactivation. Importantly, cPTs were stable to trypsin and chymotrypsin compared to substantial susceptibility of corresponding linear PTs.

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Citations

Nov 26, 2015·Future Medicinal Chemistry·Irwin Chaiken, Adel A Rashad
Jul 12, 2016·Expert Opinion on Therapeutic Patents·Lin SunXinyong Liu
Sep 15, 2016·Chemical Reviews·Bauke Albada, Nils Metzler-Nolte
Feb 28, 2019·Journal of Peptide Science : an Official Publication of the European Peptide Society·Rachna AnejaIrwin Chaiken
Apr 20, 2019·Medicinal Research Reviews·Xiangyi JiangPeng Zhan
May 17, 2019·Expert Opinion on Drug Discovery·Xiangyi JiangPeng Zhan
Jun 8, 2021·Frontiers in Chemistry·Agnieszka StaśkiewiczRafal Latajka

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