2. Academic Validation
  3. Macrocyclic Envelope Glycoprotein Antagonists that Irreversibly Inactivate HIV-1 before Host Cell Encounter

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

  • J Med Chem. 2015 Sep 24;58(18):7603-8. doi: 10.1021/acs.jmedchem.5b00935.
Adel A Rashad 1,  Ramalingam Venkat Kalyana Sundaram 1 2,  Rachna Aneja 1,  Caitlin Duffy 1,  Irwin Chaiken 1
Affiliations

Affiliations

  • 1 Department of Biochemistry and Molecular Biology, Drexel University College of Medicine , 245 North 15th Street, Philadelphia, Pennsylvania 19102 United States.
  • 2 School of Biomedical Engineering, Science and Health Systems, Drexel University , Philadelphia, Pennsylvania 19104 United States.
PMID: 26331669 DOI: 10.1021/acs.jmedchem.5b00935
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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