Generalizing the Concept of Specific Compound Formulation Additives towards Non-Fluorescent Drugs: A Solubilization Study on Potential Anti-Alzheimer-Active Small-Molecule Compounds

Angew Chem Int Ed Engl. 2016 Jul 18;55(30):8752-6. doi: 10.1002/anie.201601147. Epub 2016 Jun 10.

Abstract

Tailor-made compound formulation additives enable the testing of potential drugs with undesirable pharmacological profiles. A combinatorial approach using Raman microscopy as the readout method is presented to select peptide sequences from large one-bead-one-compound libraries. The resulting peptide-PEG conjugates solubilize potential prophylactic and therapeutic anti-Alzheimer compounds and can be used as specific additives not only for fluorescent but also for non-fluorescent compounds.

Keywords: Alzheimer's disease; Tau protein; bioconjugates; combinatorial screening; precision polymers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / drug therapy
  • Drug Design
  • Dynamic Light Scattering
  • Humans
  • Microscopy
  • Molecular Conformation
  • Molecular Dynamics Simulation
  • Peptide Library
  • Peptides / chemistry*
  • Polyethylene Glycols / chemistry*
  • Protein Aggregates / drug effects
  • Protein Binding
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology
  • Small Molecule Libraries / therapeutic use
  • Solubility
  • Spectrum Analysis, Raman
  • tau Proteins / chemistry
  • tau Proteins / metabolism

Substances

  • Peptide Library
  • Peptides
  • Protein Aggregates
  • Small Molecule Libraries
  • tau Proteins
  • Polyethylene Glycols