Abstract
In comparison to the huge number of peptidic and peptidomimetic inhibitors of cysteine proteases which have been developed during the last twenty years the number of non-peptidic compounds with cysteine protease inhibiting properties is restricted to a few substance classes. In contrast to peptidic and peptidomimetic inhibitors the non-peptidic lead structures have mainly been discovered by computational or enzymatic industrial screenings and not by a rational approach. But, the growing number of resolved X-ray structures of the target enzymes as well as molecular modeling methods have supported the further development of potent inhibitors beginning from these lead structures. In this review we will focus on new non-peptidic cysteine protease inhibitors which have been developed during the last years. Discovery, structure-activity-relationship and inhibition mechanisms will be discussed.
Keywords: cysteine proteases, peptidomimetic cysteine protease inhibitors, papain-like cysteine
Mini-Reviews in Medicinal Chemistry
Title: Non-Peptidic Inhibitors of Cysteine Proteases
Volume: 3 Issue: 4
Author(s): T. Schirmeister and U. Kaeppler
Affiliation:
Keywords: cysteine proteases, peptidomimetic cysteine protease inhibitors, papain-like cysteine
Abstract: In comparison to the huge number of peptidic and peptidomimetic inhibitors of cysteine proteases which have been developed during the last twenty years the number of non-peptidic compounds with cysteine protease inhibiting properties is restricted to a few substance classes. In contrast to peptidic and peptidomimetic inhibitors the non-peptidic lead structures have mainly been discovered by computational or enzymatic industrial screenings and not by a rational approach. But, the growing number of resolved X-ray structures of the target enzymes as well as molecular modeling methods have supported the further development of potent inhibitors beginning from these lead structures. In this review we will focus on new non-peptidic cysteine protease inhibitors which have been developed during the last years. Discovery, structure-activity-relationship and inhibition mechanisms will be discussed.
Export Options
About this article
Cite this article as:
Schirmeister T. and Kaeppler U., Non-Peptidic Inhibitors of Cysteine Proteases, Mini-Reviews in Medicinal Chemistry 2003; 3 (4) . https://dx.doi.org/10.2174/1389557033488079
DOI https://dx.doi.org/10.2174/1389557033488079 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- 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
Related Articles
-
Depression and Quality of Life in Patients with Diabetes: A Systematic Review from the European Depression in Diabetes (EDID) Research Consortium
Current Diabetes Reviews Clinical and Prognostic Implications of Cognitive Dysfunction and Depression in COPD
Current Respiratory Medicine Reviews Pharmacokinetic Changes of Drugs in Rat Model of Acute Renal Failure Induced by Uranyl Nitrate: Correlation Between Drug Metabolism and Hepatic Microsomal Cytochrome P450 Isozymes
Current Clinical Pharmacology Dipeptidyl Peptidase-4 Inhibition: Linking Chemical Properties to Clinical Safety
Current Medicinal Chemistry Vitamin, Mineral, and Drug Absorption Following Bariatric Surgery
Current Drug Metabolism Microvascular Complications of Type 2 Diabetes Mellitus
Current Vascular Pharmacology Cannabinoids and Neuropathic Pain
Mini-Reviews in Medicinal Chemistry Fabrication of Highly Sensitive Chemi-Sensor and Efficient Photocatalyst Based On ZnO Nanostructured Material
Micro and Nanosystems Platelet Ca2+ATPases: Identification and Regulation in Hypertension
Current Hypertension Reviews The Biological and Clinical Activity of Anti-Malarial Drugs In Autoimmune Disorders
Current Rheumatology Reviews Interaction between Thienopyridines and Proton Pump Inhibitors
Cardiovascular & Hematological Disorders-Drug Targets Novel Treatment Strategies for the Nervous System: Circadian Clock Genes, Non-coding RNAs, and Forkhead Transcription Factors
Current Neurovascular Research A New Binding Site Involving the C-terminal Domain to Design Specific Inhibitors of PepX
Protein & Peptide Letters TNF-α and Ghrelin: Opposite Effects on Immune System, Metabolism and Mental Health
Protein & Peptide Letters Effect of Fasting Ramadan in Diabetes Control Status - Application of Extensive Diabetes Education, Serum Creatinine with HbA1c Statistical ANOVA and Regression Models to Prevent Hypoglycemia
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery The Genetic Background of Cholesterol Gallstone Formation: An Inventory of Human Lithogenic Genes
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Atrial Fibrillation: Epidemiology and Peculiarities in the Elderly
Cardiovascular & Hematological Agents in Medicinal Chemistry Combination of Daidzein, Hemin and Bms182874 Halts the Progression of Diabetes-Induced Experimental Nephropathy
Endocrine, Metabolic & Immune Disorders - Drug Targets Role of Molecular Hydrogen in Skin Diseases and its Impact in Beauty
Current Pharmaceutical Design Importance of Pharmacology Knowledge by Dieticians
Current Nutrition & Food Science