Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Compounds mimicking the Michaelis-Menten transition state of the phosphatidylinositol 4-kinase.

Bioorganic & medicinal chemistry·2026

Same author

Early Kinetic Characterization of SARS-CoV-2 Main Protease Inhibitors: A Review and Guidance for Biochemical Assessments.

Biochemistry·2026

Same author

Discovery of Histone Deacetylase 8-Specific Proteolysis-Targeting Chimeras with Anticancer Activity against Hematological Malignancies.

Journal of medicinal chemistry·2026

Same author

Sequential Optimization Approach Toward an Azapeptide-Based SARS-CoV-2 Main Protease Inhibitor.

Archiv der Pharmazie·2025

Same author

Crosstalk between NLRP3 Signaling and Histone Deacetylases in Inflammasome-Driven Diseases.

Journal of medicinal chemistry·2025

Same author

A Facile Protocol for C(sp<sup>2</sup>)-C(sp<sup>3</sup>) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands.

ChemMedChem·2025

Same journal

A Melatonin-Catechol Hybrid Molecule Prolongs Lifespan via Regulating ROS and Reprogramming Mitochondrial Metabolism.

Journal of medicinal chemistry·2026

Same journal

Discovery of SD-2301 as a Highly Potent and Selective PROTAC STAT3 Degrader Capable of Achieving Complete Tumor Regression with Single Administration.

Journal of medicinal chemistry·2026

Same journal

GID4-Recruiting PROTACs for BRD4 Degradation Overcome Resistance Driven by CRBN and VHL Deficiency.

Journal of medicinal chemistry·2026

Same journal

Alpha-Particle Therapy with an Actinium-225 Labeled Bivalent Inhibitor of Prostate-Specific Membrane Antigen is Therapeutically Efficacious in a Mouse Model of Prostate Cancer.

Journal of medicinal chemistry·2026

Same journal

Development of Telmisartan Platinum(IV) Complexes for Antimetastatic Therapy: Targeting EMT and Tumor Immunity through Suppressing AT1R.

Journal of medicinal chemistry·2026

Same journal

Library Docking for Cannabinoid-2 Receptor Ligands.

Journal of medicinal chemistry·2026

See all related articles

Search research articles

Related Experiment Video

Updated: Oct 21, 2025

In Vivo Imaging of Transduction Efficiencies of Cardiac Targeting Peptide

In Vivo Imaging of Transduction Efficiencies of Cardiac Targeting Peptide

Published on: June 11, 2020

An Activity-Based Probe for Cathepsin K Imaging with Excellent Potency and Selectivity.

Carina Lemke¹, Jakub Benýšek^2,3, Dominik Brajtenbach¹

¹Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, An der Immenburg 4, Bonn 53121, Germany.

Journal of Medicinal Chemistry

|September 2, 2021

Summary

This summary is machine-generated.

Researchers developed novel fluorescent probes to target and detect cathepsin K, a key enzyme in bone diseases. These probes enable sensitive visualization and imaging, aiding in understanding bone turnover and related pathologies.

More Related Videos

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent

Published on: September 3, 2013

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Published on: November 23, 2016

Related Experiment Videos

Last Updated: Oct 21, 2025

In Vivo Imaging of Transduction Efficiencies of Cardiac Targeting Peptide

In Vivo Imaging of Transduction Efficiencies of Cardiac Targeting Peptide

Published on: June 11, 2020

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent

MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent

Published on: September 3, 2013

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase

Published on: November 23, 2016

Area of Science:

Biochemistry
Molecular Biology
Medicinal Chemistry

Background:

Cathepsin K is a cysteine protease crucial for bone matrix degradation and implicated in bone diseases.
Targeting cathepsin K offers a therapeutic strategy for conditions characterized by high bone turnover.

Purpose of the Study:

To design and synthesize novel fluorescent activity-based probes (ABPs) for cathepsin K.
To characterize the binding and inhibitory properties of these probes.
To evaluate their utility in detecting and visualizing cathepsin K in biological systems.

Main Methods:

Design and synthesis of fluorescent ABPs and their precursors.
Biochemical assays to determine probe potency (k_inac/K_i) and selectivity.
X-ray crystallography to elucidate the binding mode of probes with cathepsin K.
Cell-based assays including live cell imaging of human osteosarcoma cells.

Main Results:

ABP 25 demonstrated high potency and selectivity for human cathepsin K.
Crystal structures revealed the binding interactions of ABP 25 and precursor 21 with cathepsin K.
Probe 25 enabled sensitive detection and selective visualization of cathepsin K in complex proteomes.
Live cell imaging confirmed the probe's applicability in a pathophysiological context.

Conclusions:

Novel acrylamide-based Michael acceptor probes were developed for cathepsin K.
ABP 25 is a potent and selective inhibitor and imaging agent for cathepsin K.
These probes show promise for diagnostic and research applications in bone-related diseases.