Use of a fluorescent polarization based high throughput assay to identify new calmodulin ligands

Biochim Biophys Acta. 2006 Nov;1763(11):1250-5. doi: 10.1016/j.bbamcr.2006.09.027. Epub 2006 Sep 26.

Abstract

In order to develop a fluorescence polarization (FP) assay for calcium binding proteins, a fluorescent peptides based library of 1328 compounds has been synthesized. The use of this library has been validated by setting up a FP-high-throughput screening (FP-HTS) assay for calmodulin using the synthetic gene product (synCaM). With this assay, a set of 880 FDA approved compounds was screened. Besides the promazine class, we discovered two new classes of compounds that interact with calmodulin in a calcium dependent manner. One class has compounds with anti-histaminic/spasmolytic activities, and the other one are detergents with antibacterial activities.

Publication types

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

MeSH terms

  • Calcium-Binding Proteins / chemistry*
  • Calcium-Binding Proteins / genetics
  • Calmodulin / chemistry*
  • Calmodulin / genetics
  • Drug Evaluation, Preclinical / methods*
  • Fluorescence Polarization / methods*
  • Ligands
  • Peptide Library*
  • Peptides / chemical synthesis
  • Peptides / chemistry

Substances

  • Calcium-Binding Proteins
  • Calmodulin
  • Ligands
  • Peptide Library
  • Peptides