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Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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A Fluorescence-based Lymphocyte Assay Suitable for High-throughput Screening of Small Molecules
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Solid-phase biological assays for drug discovery.

Erica M Forsberg1, Clémence Sicard, John D Brennan

  • 1Biointerfaces Institute, McMaster University, Hamilton, Ontario L8S 4L8, Canada;

Annual Review of Analytical Chemistry (Palo Alto, Calif.)
|July 9, 2014
PubMed
Summary
This summary is machine-generated.

Solid-phase biological assays (SPBAs) have grown significantly in drug discovery over 30 years. This review covers SPBA methods, targets, and applications for identifying drug leads, especially for labile biomolecules.

Keywords:
bioaffinity chromatographykinasesmembrane proteinsprotein microarrays

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Assay Development

Background:

  • Solid-phase biological assays (SPBAs) have seen substantial growth in drug discovery over the last three decades.
  • These assays are employed for both soluble and membrane-bound biological targets.
  • The review focuses on labile biomolecular targets like kinases and membrane receptors.

Purpose of the Study:

  • To provide background on drug targets and immobilization protocols in SPBAs.
  • To highlight recent advancements in protein microarrays and bioaffinity columns for small molecule screening.
  • To discuss the application of SPBAs in identifying drug leads, including mixture screening.

Main Methods:

  • Review of immobilization protocols for solid-phase assays.
  • Discussion of protein microarray and bioaffinity column production methods.
  • Analysis of SPBA applications in small molecule screening and mixture analysis.

Main Results:

  • SPBAs are versatile tools for drug discovery, adaptable to various targets.
  • Recent innovations facilitate the creation of devices crucial for high-throughput screening.
  • Mixture screening using SPBAs is a key application for lead identification.

Conclusions:

  • SPBAs offer specific advantages for drug discovery, particularly in screening labile targets.
  • Understanding the advantages and disadvantages of different SPBA formats is crucial for assay design.
  • The continued development of SPBAs promises to enhance the efficiency of identifying novel drug candidates.