Abstract
Urokinase type plasminogen activator (uPA) activates plasminogen to plasmin and is often associated with diseases where tissue remodeling is essential (e.g. cancer, macular degeneration, atherosclerosis). We discuss some of the mechanisms of uPA action in diseases, and evidence that some of the early uPA inhibitors can modulate the progression of these diseases. Recently, a number of research groups have discovered, with the aid of structure-based design, a new generation of uPA inhibitors. These inhibitors are much more potent and selective than their predecessors. We will review this progress here, and give particular attention to the structural rationale associated with these observed increases in potency and selectivity.
Keywords: urokinase type plasminogen activator, upa inhibitors
Current Pharmaceutical Design
Title: Inhibitors of the Proteolytic Activity of Urokinase Type Plasminogen Activator
Volume: 9 Issue: 19
Author(s): Todd W. Rockway and Vincent L. Giranda
Affiliation:
Keywords: urokinase type plasminogen activator, upa inhibitors
Abstract: Urokinase type plasminogen activator (uPA) activates plasminogen to plasmin and is often associated with diseases where tissue remodeling is essential (e.g. cancer, macular degeneration, atherosclerosis). We discuss some of the mechanisms of uPA action in diseases, and evidence that some of the early uPA inhibitors can modulate the progression of these diseases. Recently, a number of research groups have discovered, with the aid of structure-based design, a new generation of uPA inhibitors. These inhibitors are much more potent and selective than their predecessors. We will review this progress here, and give particular attention to the structural rationale associated with these observed increases in potency and selectivity.
Export Options
About this article
Cite this article as:
Rockway W. Todd and Giranda L. Vincent, Inhibitors of the Proteolytic Activity of Urokinase Type Plasminogen Activator, Current Pharmaceutical Design 2003; 9 (19) . https://dx.doi.org/10.2174/1381612033454649
DOI https://dx.doi.org/10.2174/1381612033454649 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
The Posterior Perforated Substance: A Brain Mystery Wrapped in an Enigma
Current Topics in Medicinal Chemistry Editorial: Overview on microRNAs in Cancer Development and Virus Infection
MicroRNA Preface
Recent Patents on Medical Imaging Update on the Imaging Techniques in the Diagnosis of Diabetic Retinopathy
Current Diabetes Reviews Molecular Hydrogen Application in Stroke: Bench to Bedside
Current Pharmaceutical Design N-Butyl Cyanoacrylate Embolization of a Peripheral Pulmonary Artery Aneurysm in a Patient with Patent Ductus Arteriosus
Current Cardiology Reviews Pitavastatin and 4-Hydroxy-3-Methoxyacetophenone (HMAP) Reduce Cognitive Dysfunction in Vascular Dementia During Experimental Diabetes
Current Neurovascular Research Why Multiples of 21? Why does Selenoprotein P Contain Multiple Selenocysteine Residues?
Current Nutraceuticals Endogenous Events Modulating Myogenic Regulation of Cerebrovascular Function
Current Vascular Pharmacology Implantable Medical Devices and Tissue Engineering: An Overview of Manufacturing Processes and the Use of Polymeric Matrices for Manufacturing and Coating their Surfaces
Current Medicinal Chemistry P2X7 Receptor-Associated Programmed Cell Death in the Pathophysiology of Hemorrhagic Stroke
Current Neuropharmacology Perioperative/Periprocedural Effects of Statin Treatment for Patients Undergoing Vascular Surgery or Endovascular Procedures: An Update
Current Vascular Pharmacology Hyperglycemia-induced Oxidative Stress and its Role in Diabetes Mellitus Related Cardiovascular Diseases
Current Pharmaceutical Design Role of MMPs in Metastatic Dissemination: Implications for Therapeutic Advances
Current Pharmaceutical Biotechnology Transforming Growth Factor β Signaling Perturbation in the Loeys-Dietz Syndrome
Current Medicinal Chemistry Levosimendan Reduces Prostaglandin F2a-dependent Vasoconstriction in Physiological Vessels and After Experimentally Induced Subarachnoid Hemorrhage
Current Neurovascular Research Intracoronary Brachytherapy - Clinical State and Pathophysiological Considerations
Current Pharmaceutical Design A Cerebrovascular Image Segmentation Method Based on Geometrical Feature Point Clustering and Local Threshold
Current Medical Imaging Type 1 Diabetes Mellitus - Risk Factor for Cardiovascular Disease Morbidity and Mortality
Current Diabetes Reviews Efficacy, Duration and Timing of Withdrawal of Prophylactic Treatment with Antiepileptic Drugs in Neurosurgical Conditions
Current Pharmaceutical Design