Related Experiment Video

Updated: May 7, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Inhibitors of cathepsin G: a patent review (2005 to present)

Paulina Kosikowska1, Adam Lesner

  • 1University of Gdansk, Department of Bioorganic Chemistry , Wita Stwosza 63, 80-952 Gdansk , Poland +48585235095 ; +48585235472 ; alesner@chem.univ.gda.pl.

Expert Opinion on Therapeutic Patents
|October 2, 2013
PubMed

Insights

Cathepsin G (CatG) inhibitors show therapeutic promise, particularly natural compounds like boswellic acids. Further research is needed to develop stable, clinically effective CatG-targeting drugs.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Cathepsin G (CatG) is a neutrophil proteinase with dual specificity, implicated in inflammatory diseases like COPD and rheumatoid arthritis.
  • Its enzymatic activity is difficult to control, making it a therapeutic target, though no drugs are currently marketed.
  • CatG's role in disease pathophysiology drives interest in developing specific inhibitors.

Purpose of the Study:

  • To analyze the therapeutic potential of Cathepsin G inhibitors.
  • To review patent applications and academic literature on CatG inhibitors from 1991-2012.
  • To identify promising inhibitor classes and future research directions.

Main Methods:

  • Comprehensive review of patent applications and academic publications.
  • Analysis of disclosed CatG inhibitors within a specific time frame (1991-2012).
  • Inclusion of select inhibitors from academic articles outside patent disclosures.

Main Results:

  • Several CatG inhibitor classes show promise, including beta-ketophosphonic acids, aminoalkylphosphonic esters, and boswellic acids (BAs).
  • Analogues of natural compounds, specifically peptidic and BA derivatives, appear most promising.
  • No clinical disposition data is available for any identified CatG inhibitors.

Conclusions:

  • Boswellic acid derivatives and other natural product analogues represent promising avenues for CatG inhibitor development.
  • Significant work remains in designing stable, pharmacologically active compounds for specific in vivo CatG regulation.
  • The lack of clinical data highlights the need for further research into the clinical efficacy and safety of CatG inhibitors.
Abstract

More Related Videos

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries08:49

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

Screening for Thermotoga maritima Membrane-Bound Pyrophosphatase Inhibitors09:11

Screening for Thermotoga maritima Membrane-Bound Pyrophosphatase Inhibitors

Published on: November 23, 2019

Related Concept Videos

GTPases and their Regulation02:14

GTPases and their Regulation

Guanine nucleotide-binding proteins (G-proteins), also known as GTPases, are a superfamily of proteins that regulate many cellular processes, such as cell signaling, vesicular transport, and the regulation of cell shape and motility. Mutation or dysfunction of these proteins can lead to disease. There are around 40,000 known G-proteins that can broadly be classified into two groups ‒  small G-proteins consisting of a single domain and large multi-domain G-proteins.
Large G-proteins, also known...
Enzyme Inhibition01:30

Enzyme Inhibition

Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.
Patch Clamp01:18

Patch Clamp

Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
In this method, a glass micropipette containing electrolyte solution is tightly sealed against a small portion of the cell membrane. As a result, a patch of the cell...
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
ATP Synthase: Mechanism01:48

ATP Synthase: Mechanism

In animals, the mitochondrial F1F0 ATP synthase is the key protein that synthesizes ATP molecules through a complex catalytic mechanism. While the nuclear genome encodes the majority of ATP synthase subunits, the mitochondrial genome encodes some of the enzyme's most critical components. The formation of this multi-subunit enzyme is a complex multi-step process regulated at the level of transcription, translation, and assembly. Defects in one or more of these steps can result in decreased ATP...
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...