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Related Concept Videos

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Matrix metalloproteases (MMPs) are enzymes involved in the hydrolysis of proteins and glycoproteins of the extracellular matrix. MMPs are essential for the migration and proliferation of cells through the dense matrix network, throughout embryonic development, and throughout morphogenesis. The first MMP activity discovered was a collagenase in a tadpole's tail undergoing metamorphosis. The active collagen deposition and modifications lead to the morphogenesis of tadpoles into the adult body.
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The Proteasome02:18

The Proteasome

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Nanosensors to Detect Protease Activity In Vivo for Noninvasive Diagnostics
10:50

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Published on: July 16, 2018

Extracellular proteases as targets for drug development.

Mare Cudic1, Gregg B Fields

  • 1Department of Biochemistry, University of Texas Health Science Center, 7703 Floyd Curl Drive, San Antonio, TX 78229, USA.

Current Protein & Peptide Science
|August 20, 2009
PubMed
Summary

Extracellular proteases (ECPs) are key drug targets for diseases like cancer and inflammation. New therapies inhibiting ECPs or using them for targeted drug delivery are emerging.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Proteases are crucial targets in drug discovery.
  • Extracellular proteases (ECPs) are differentially expressed in various pathophysiological conditions, including cancer, cardiovascular, inflammatory, pulmonary, and periodontal diseases.
  • This differential expression offers opportunities for targeted therapies and diagnostics.

Purpose of the Study:

  • To review recent advancements in targeted drug development for extracellular proteases.
  • To highlight the potential of ECP inhibitors and targeted delivery systems.

Main Methods:

  • Review of current literature on extracellular proteases.
  • Focus on metalloproteases, serine proteases, and cysteine proteases.
  • Discussion of recent studies in targeted drug development.

Main Results:

  • Numerous ECP inhibitors are in clinical trials.
  • Significant growth in protease inhibition therapies is anticipated.
  • Strategies include direct activity blockade and targeted delivery of agents.

Conclusions:

  • Extracellular proteases represent a promising area for therapeutic intervention.
  • Targeted drug development for ECPs is advancing rapidly.
  • Future therapies will likely leverage ECP inhibition and targeted delivery for various diseases.