Designing nanomolar antagonists of DC-SIGN-mediated HIV infection: ligand presentation using molecular rods

Chem Commun (Camb). 2015 Mar 4;51(18):3816-9. doi: 10.1039/c4cc09709b.

Abstract

DC-SIGN antagonists were designed combining one selective monovalent glycomimetic ligand with trivalent dendrons separated by a rigid core of controlled length. The design combines multiple multivalency effects to achieve inhibitors of HIV infection, which are active in nanomolar concentration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • CD4-Positive T-Lymphocytes / drug effects
  • CD4-Positive T-Lymphocytes / virology
  • Cell Adhesion Molecules / antagonists & inhibitors*
  • Cell Adhesion Molecules / chemistry
  • Cell Adhesion Molecules / genetics
  • Cell Line
  • Cells, Cultured
  • Dendrimers / chemistry*
  • Dendrimers / pharmacology*
  • HIV Infections / prevention & control*
  • HIV-1 / pathogenicity
  • Humans
  • Lectins, C-Type / antagonists & inhibitors*
  • Lectins, C-Type / chemistry
  • Lectins, C-Type / genetics
  • Ligands
  • Mannose / chemistry
  • Receptors, Cell Surface / antagonists & inhibitors*
  • Receptors, Cell Surface / chemistry
  • Receptors, Cell Surface / genetics
  • Serum Albumin / chemistry

Substances

  • Cell Adhesion Molecules
  • DC-specific ICAM-3 grabbing nonintegrin
  • Dendrimers
  • Lectins, C-Type
  • Ligands
  • Receptors, Cell Surface
  • Serum Albumin
  • mannose-bovine serum albumin conjugate
  • Mannose