Abstract
The cathepsins are a family of lysosomal cysteine proteases that are abundant in living cells and play important roles in intracellular proteolysis. Cathepsins are necessary for cell survival, and disruption of regulation of the activity of these enzymes causes serious diseases including allergy, atherosclerosis, muscular dystrophy, Alzheimers disease and cancer. Therefore, the design of inhibitors for cathepsins is important in development of therapeutic agents. This review will focus on the features of the tertiary structure and substrate-binding specificity of cathepsins B, L, S and K, based on X-ray crystal structures of their complexes with inhibitors. To illustrate an approach to drug design, an example of structure-based design of a cathepsin B-specific inhibitor is described.
Current Topics in Medicinal Chemistry
Title: Development of Cathepsin Inhibitors and Structure-Based Design of Cathepsin B-Specific Inhibitor
Volume: 10 Issue: 7
Author(s): Koji Tomoo
Affiliation:
Abstract: The cathepsins are a family of lysosomal cysteine proteases that are abundant in living cells and play important roles in intracellular proteolysis. Cathepsins are necessary for cell survival, and disruption of regulation of the activity of these enzymes causes serious diseases including allergy, atherosclerosis, muscular dystrophy, Alzheimers disease and cancer. Therefore, the design of inhibitors for cathepsins is important in development of therapeutic agents. This review will focus on the features of the tertiary structure and substrate-binding specificity of cathepsins B, L, S and K, based on X-ray crystal structures of their complexes with inhibitors. To illustrate an approach to drug design, an example of structure-based design of a cathepsin B-specific inhibitor is described.
Export Options
About this article
Cite this article as:
Tomoo Koji, Development of Cathepsin Inhibitors and Structure-Based Design of Cathepsin B-Specific Inhibitor, Current Topics in Medicinal Chemistry 2010; 10 (7) . https://dx.doi.org/10.2174/156802610791113441
DOI https://dx.doi.org/10.2174/156802610791113441 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Adaptogens—History and Future Perspectives
Adaptogens are pharmacologically active compounds or plant extracts that are associated with the ability to enhance the body’s stability against stress. The intake of adaptogens is associated not only with a better ability to adapt to stress and maintain or normalise metabolic functions but also with better mental and physical ...read more
Addressing the Most Common Causes of Death with Niacin/NAD and Inositol Polyphosphates
The most common causes of death in the world are cardiovascular disease (CVD) and cancer. These are perhaps best addressed by reducing lipodystrophy and blockages with niacin and inositol polyphosphates (e.g., IP6+inositol) respectively when addressing CVD. Niacin serves as a vitamin by virtue of its role as a skeletal precursor ...read more
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more

- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Acid-sensing Ion Channels: Implications for Intervertebral Disc
Degeneration
Current Pharmaceutical Biotechnology Monoclonal Antibodies: A Prospective and Retrospective View
Current Medicinal Chemistry Biologics in Systemic Sclerosis
Current Pharmaceutical Biotechnology Selective Inhibitors of Nuclear Factor of Activated T Cells: Potential Therapeutic Drugs for the Treatment of Immunological and Inflammatory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Snake Venom Metalloproteinases: Structure, Mechanism and Induced Diseases
Current Chemical Biology Environmental (Lifestyle) Risk Factors for LADA
Current Diabetes Reviews Neurotransmitters and Chemokines Regulate Tumor Cell Migration: Potential for a New Pharmacological Approach to Inhibit Invasion and Metastasis Development
Current Pharmaceutical Design Role of Interleukin-21 in Inflammation and Allergy
Inflammation & Allergy - Drug Targets (Discontinued) The Emerging Role of COX-2, 15-LOX and PPARγ in Metabolic Diseases and Cancer: An Introduction to Novel Multi-target Directed Ligands (MTDLs)
Current Medicinal Chemistry A Realistic Approach for Anti-Inflammatory, Antinociceptive and Antimutagenic Activities, and Risk Assessment of the Aqueous Extract of <i>Platanus orientalis</i> L. Leaves
Current Molecular Pharmacology Progress in Imaging Agents of Cell Apoptosis
Anti-Cancer Agents in Medicinal Chemistry Immune Therapy of Multiple Sclerosis - Future Strategies
Current Pharmaceutical Design Back Pain in Children and Adolescents: Etiology, Clinical Approach and Treatment
Current Pediatric Reviews A Case of Quinacrine-induced Psychosis: Case Report
Current Drug Safety Arraying Autoantibodies in SLE – Lessons Learned
Current Molecular Medicine Comparative Characterization of Experimental and Calculated Lipophilicity and Anti-Tumour Activity of Isochromanone Derivatives
Current Medicinal Chemistry Geriatric Evaluation of Oncological Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry Addressing the Importance of Stem Cell-Based Therapy: A Perspective in the Treatment of COVID-19
Current Molecular Medicine Endocrine, Metabolic, and Immune Pathogenesis of Postmenopausal Osteoporosis. Is there a Therapeutic Role in Natural Products?
Endocrine, Metabolic & Immune Disorders - Drug Targets Systemic Autoimmune Manifestations: When Should Underlying Thyroid Autoimmunity be Considered?
Current Rheumatology Reviews