Related Experiment Video
Updated: Jun 4, 2026
08:49
Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Cathepsin S inhibitors: 2004-2010.
Alice Lee-Dutra1, Danielle K Wiener, Siquan Sun
1Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. alee7@its.jnj.com
Expert Opinion on Therapeutic Patents
|February 24, 2011
Summary
Small molecule inhibitors targeting cathepsin S, a protease involved in antigen presentation, were reviewed. Patent activity decreased, possibly due to increased interest in cathepsin K inhibitors.
Area of Science:
- Biochemistry
- Immunology
- Medicinal Chemistry
Background:
- Cathepsin S is a lysosomal cysteine protease crucial for antigen presentation.
- Inhibition of Cathepsin S can lead to immunosuppression.
- This makes Cathepsin S a potential therapeutic target for autoimmune and inflammatory diseases.
Purpose of the Study:
- To review patent literature on small molecule inhibitors of Cathepsin S.
- To survey different structural classes of inhibitors based on binding strategies.
- To list inhibitors by warhead type and research organization.
Main Methods:
- Focused on patent literature published between 2004 and April 2010.
- Classified inhibitors based on covalent and non-covalent binding strategies.
- Organized findings by warhead type and originating research institution.
Main Results:
- Over 40 patent applications for Cathepsin S inhibitors were identified between 2004 and 2010.
- Inhibitors were categorized into various structural classes.
- A decline in patent filings for Cathepsin S was observed in the later years of the review period.
Conclusions:
- The decrease in Cathepsin S patent applications may indicate a shift in research focus.
- There might be a growing interest in other cathepsins, such as Cathepsin K.
- A Cathepsin K inhibitor is currently in Phase III clinical trials, suggesting a potential therapeutic trend.
More Related Videos
Related Concept Videos
02:57Targeted Cancer Therapies
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
There are several types of targeted therapies against specific...
01:48ATP 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...
01:23Dipeptidyl Peptidase 4 Inhibitors
Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
01:18Patch 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...
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...
02:34Inhibition 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...
01:15Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions
PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure (CHF).