Dual-pharmacophore DNA-encoded chemical libraries

Curr Opin Chem Biol. 2015 Jun:26:99-103. doi: 10.1016/j.cbpa.2015.02.021. Epub 2015 Mar 13.

Abstract

In contrast to single-pharmacophore DNA-encoded libraries, where only one chemical moiety is linked to DNA, dual-pharmacophore DNA-encoded chemical libraries feature the display of two independent small-molecules in close proximity. This, in principle, allows to explore adjacent epitopes on a pharmaceutical target of choice and hence the discovery of simultaneously binding pairs of fragments, by virtue of the chelate effect.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetazolamide / chemical synthesis
  • Acetazolamide / pharmacology
  • Antigens, Neoplasm / chemistry*
  • Antigens, Neoplasm / metabolism
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Carbonic Anhydrase IX
  • Carbonic Anhydrase Inhibitors / chemical synthesis
  • Carbonic Anhydrase Inhibitors / pharmacology
  • Carbonic Anhydrases / chemistry*
  • Carbonic Anhydrases / metabolism
  • Carcinoma, Renal Cell / drug therapy
  • Carcinoma, Renal Cell / enzymology
  • Carcinoma, Renal Cell / pathology
  • Combinatorial Chemistry Techniques
  • DNA / chemistry*
  • DNA / metabolism
  • Drug Discovery
  • Fluorescent Dyes / chemistry
  • Gene Expression
  • Gene Library*
  • Humans
  • Kidney Neoplasms / drug therapy
  • Kidney Neoplasms / enzymology
  • Kidney Neoplasms / pathology
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / chemistry*

Substances

  • Antigens, Neoplasm
  • Antineoplastic Agents
  • Carbonic Anhydrase Inhibitors
  • Fluorescent Dyes
  • Small Molecule Libraries
  • DNA
  • CA9 protein, human
  • Carbonic Anhydrase IX
  • Carbonic Anhydrases
  • Acetazolamide