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Related Experiment Videos

Fragment based drug discovery using fluorescence correlation: spectroscopy techniques: challenges and solutions.

T Hesterkamp1, J Barker, A Davenport

  • 1Evotec, Schnackenburgallee 114, D-22525 Hamburg, Germany. Thomas.Hesterkamp@evotec.com

Current Topics in Medicinal Chemistry
|November 6, 2007
PubMed
Summary
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High-concentration screening of fragment molecules using advanced fluorescence methods identifies novel drug leads. This approach combines quality fragment libraries with sensitive assays for reproducible results in medicinal chemistry.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Structural Biology

Background:

  • Identifying novel starting points for drug discovery is crucial for medicinal chemistry programs.
  • High-concentration screening of fragment libraries in biochemical assays is an effective strategy.
  • Sensitive detection methods are essential for identifying weakly active fragment molecules.

Purpose of the Study:

  • To demonstrate the successful application of high-concentration fragment screening using advanced detection techniques.
  • To validate the reproducibility and sensitivity of single-molecule Fluorescence Correlation Spectroscopy (FCS+plus).
  • To determine the binding modes of identified active fragments to target proteins.

Main Methods:

  • High-concentration screening of fragment libraries using biochemical assays.

Related Experiment Videos

  • Utilizing a portfolio of single-molecule Fluorescence Correlation Spectroscopy (FCS+plus) techniques.
  • X-ray crystallography for determining fragment-protein binding modes.
  • Review of additional biophysical detection methods for fragment binding studies.

    • Main Results:

    • Successful identification of weakly active fragment molecules through high-concentration screening.
    • Demonstrated high reproducibility and sensitivity using FCS+plus techniques.
    • Determined the binding modes of active fragments via X-ray crystallography.

    Conclusions:

    • High-concentration fragment screening is a viable strategy for identifying novel drug leads.
    • Advanced biophysical techniques like FCS+plus enhance the sensitivity and reproducibility of fragment screening.
    • Structural information from X-ray crystallography aids in understanding fragment-protein interactions for drug design.