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Proteases as drug targets.

Andy J Docherty1, Tom Crabbe, James P O'Connell

  • 1adocherty@celltech.co.uk

Biochemical Society Symposium
|November 1, 2003
PubMed
Summary
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Proteases are viable drug targets, but matrix metalloproteinase inhibitors have faced setbacks. Future drug discovery should focus on disease pathways and orally available therapeutics for better success.

Area of Science:

  • Drug discovery and development
  • Medicinal chemistry
  • Biochemistry

Background:

  • Proteases are validated drug targets, exemplified by HIV protease inhibitors for AIDS.
  • Matrix metalloproteinase (MMP) inhibitors have shown limited success in clinical trials for cancer and rheumatoid arthritis.
  • Recent therapeutic successes in rheumatoid arthritis highlight the importance of target positioning within pathophysiological pathways.

Purpose of the Study:

  • To evaluate the tractability of proteases as drug targets from a chemical perspective, considering past challenges.
  • To explore the potential of novel proteolytic enzymes identified through genome research as improved drug targets.
  • To assess the impact of biologics, such as antibodies, on protease-targeted drug discovery strategies.

Main Methods:

Related Experiment Videos

  • Review of existing literature on protease inhibitors and clinical trial outcomes.
  • Analysis of pathophysiological pathways relevant to diseases like rheumatoid arthritis.
  • Consideration of emerging trends in drug discovery, including genomics and biologics.

Main Results:

  • While some proteases are effective drug targets, MMP inhibitors have encountered significant hurdles.
  • Identifying proteolytic enzymes causally linked to disease could lead to more effective therapies.
  • The landscape of drug discovery is evolving with the rise of biologics.

Conclusions:

  • Proteases remain promising drug targets, but strategic selection and chemical approaches are crucial for success.
  • A deeper understanding of disease mechanisms and target-specific pathways is essential for developing novel therapeutics.
  • Biologics may reshape the approach to targeting proteases and discovering inhibitors.