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Caspase, a family of cysteine proteases, serve as effectors in apoptosis. The ced3 gene in C.elegans was first identified to be involved in apoptosis. This gene encodes the ced-3 caspase that is similar to the interleukin-1-beta converting enzyme or ICE in mammals. In addition to apoptosis, caspases also function in the inflammatory response. Inflammatory caspases are essential in activating pro-inflammatory cytokines that recruit immune cells and block the replication of pathogens inside cells.
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Nanosensors to Detect Protease Activity In Vivo for Noninvasive Diagnostics
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Aspartic proteases in drug discovery.

Jörg Eder1, Ulrich Hommel, Frederic Cumin

  • 1Novartis Institutes for BioMedical Research, Expertise Platform Proteases, CH-4002 Basel, Switzerland.

Current Pharmaceutical Design
|February 23, 2007
PubMed
Summary

Aspartic proteases are key targets for new drugs, with research focusing on human enzymes like renin and BACE1. Structural insights are driving the development of novel inhibitors for various diseases.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Aspartic proteases, a small human protease class (15 members), are crucial in physiological and pathological processes.
  • Current marketed inhibitors target viral HIV protease; human aspartic protease inhibitors are in development.
  • Seven human aspartic protease crystal structures are solved, aiding inhibitor design.

Purpose of the Study:

  • To review current human aspartic protease drug targets.
  • To summarize drug discovery efforts for aspartic protease inhibitors.
  • To highlight recent advancements in developing a new generation of inhibitors.

Main Methods:

  • Literature review of current aspartic protease drug targets.
  • Summary of drug discovery efforts and inhibitor development.
  • Analysis of structural and kinetic data for inhibitor design.

Main Results:

  • Several aspartic proteases (renin, BACE1, gamma-secretase) have inhibitors in clinical/preclinical development.
  • Structural and mechanistic understanding facilitates novel inhibitor discovery.
  • Ongoing research explores other aspartic proteases as potential drug targets.

Conclusions:

  • Aspartic proteases represent significant therapeutic targets.
  • Advances in structural biology and kinetics are crucial for developing new inhibitors.
  • The field is progressing towards a new generation of aspartic protease-targeting drugs.