d(TGGGAG) with 5'-nucleobase-attached large hydrophobic groups as potent inhibitors for HIV-1 envelop proteins mediated cell-cell fusion

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5762-4. doi: 10.1016/j.bmcl.2011.08.007. Epub 2011 Aug 8.

Abstract

The Hotoda's sequence substituted with TBDPS via 5'-end nucleobase existed as parallel quadruplex structure and exhibited inhibitory activities in an HIV-1 envelop proteins mediated cell-cell fusion assay. This result demonstrated that the 5'-aromatic groups of the Hotoda's sequence are allowed to have a large spatial freedom and remain to be optimized for its role in the binding to HIV-1 envelop proteins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Base Composition
  • Cell Fusion*
  • G-Quadruplexes*
  • HIV Fusion Inhibitors / chemical synthesis*
  • HIV Fusion Inhibitors / chemistry
  • HIV Fusion Inhibitors / metabolism
  • HIV Fusion Inhibitors / pharmacology*
  • HIV-1 / drug effects*
  • HIV-1 / physiology
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Membrane Fusion
  • Protein Binding
  • Structure-Activity Relationship
  • env Gene Products, Human Immunodeficiency Virus / antagonists & inhibitors*
  • env Gene Products, Human Immunodeficiency Virus / chemistry
  • env Gene Products, Human Immunodeficiency Virus / metabolism

Substances

  • HIV Fusion Inhibitors
  • env Gene Products, Human Immunodeficiency Virus