Abstract
Since the activation of coagulation system and platelets triggers the thrombosis, the agents possessing anticoagulation or anti-platelet function have been used for the antithrombotic procession actions. However, in the physiological condition, the fibrinolytic system serves as antithrombotic, which removes the thrombus from the circulation. The fibrinolytic system plays an important role in the dissolution of fibrin, which is the main component of thrombus. So that, the balance between the coagulation and fibrinolytic system regulates the formation of thrombus. Now, the new agents that activate the fibrinolytic system have been clinically applied for the thrombolytic therapy. The main factor in fibrinolytic system is the plasmin, which is activated from the plasminogen by the plasminogen activator (PA). The plasminogen activator is mainly used for the thrombolytic therapy. There are two types of PA. One is the non fibrin-specific PA such as streptokinase (SK) and two-chain urokinase-type PA (tcu-PA, urokinase), and another is the fibrin-specific PA such as tissue- type PA (t-PA) and single-chain urokinase-type PA (scu-PA). Recently, some derivatives of t-PA have been developed to obtain the longer half-life than native t-PA and allowed to administrate as the single-bolus. Further, the new fibrin- specific PA such as staphylokinase and bat-PA has been developed. Many attempts have been made to develop the agents that would induce the release of t-PA from endothelial cells. In this review, the development of new fibrinolytic agents is summarized.
Keywords: scu-PA, t-PA, u-PA, Fibrinolysis, mutant t-PA, staphylokinase, bat-PA, endothelial cells
Current Pharmaceutical Design
Title: Development of New Fibrinolytic Agents
Volume: 12 Issue: 7
Author(s): Shigeru Ueshima and Osamu Matsuo
Affiliation:
Keywords: scu-PA, t-PA, u-PA, Fibrinolysis, mutant t-PA, staphylokinase, bat-PA, endothelial cells
Abstract: Since the activation of coagulation system and platelets triggers the thrombosis, the agents possessing anticoagulation or anti-platelet function have been used for the antithrombotic procession actions. However, in the physiological condition, the fibrinolytic system serves as antithrombotic, which removes the thrombus from the circulation. The fibrinolytic system plays an important role in the dissolution of fibrin, which is the main component of thrombus. So that, the balance between the coagulation and fibrinolytic system regulates the formation of thrombus. Now, the new agents that activate the fibrinolytic system have been clinically applied for the thrombolytic therapy. The main factor in fibrinolytic system is the plasmin, which is activated from the plasminogen by the plasminogen activator (PA). The plasminogen activator is mainly used for the thrombolytic therapy. There are two types of PA. One is the non fibrin-specific PA such as streptokinase (SK) and two-chain urokinase-type PA (tcu-PA, urokinase), and another is the fibrin-specific PA such as tissue- type PA (t-PA) and single-chain urokinase-type PA (scu-PA). Recently, some derivatives of t-PA have been developed to obtain the longer half-life than native t-PA and allowed to administrate as the single-bolus. Further, the new fibrin- specific PA such as staphylokinase and bat-PA has been developed. Many attempts have been made to develop the agents that would induce the release of t-PA from endothelial cells. In this review, the development of new fibrinolytic agents is summarized.
Export Options
About this article
Cite this article as:
Ueshima Shigeru and Matsuo Osamu, Development of New Fibrinolytic Agents, Current Pharmaceutical Design 2006; 12 (7) . https://dx.doi.org/10.2174/138161206776056065
DOI https://dx.doi.org/10.2174/138161206776056065 |
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
-
Angiopoietin-1 and C16 Peptide Attenuate Vascular and Inflammatory Responses in Experimental Allergic Encephalomyelitis
CNS & Neurological Disorders - Drug Targets Novel Pyrazolo[4, 3-c]Quinolin-3-One Derivatives as PDE5A Inhibitors
Current Topics in Medicinal Chemistry The Hydroxamic Acids as Potential Anticancer and Neuroprotective Agents
Current Medicinal Chemistry Sympathetic Nervous System in Patients with Sleep Related Breathing Disorders
Current Hypertension Reviews Parvalbumin as a Pleomorphic Protein
Current Protein & Peptide Science iMethylK-PseAAC: Improving Accuracy of Lysine Methylation Sites Identification by Incorporating Statistical Moments and Position Relative Features into General PseAAC via Chou’s 5-steps Rule
Current Genomics SHP-2 Regulates Growth Factor Dependent Vascular Signalling and Function
Mini-Reviews in Medicinal Chemistry Pleiotropic Effects of 3-Hydroxy-3-methylglutaryl-coenzyme A Reductase Inhibitors: Candidate Mechanisms for Anti-Lipid Deposition in Blood Vessels
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Myocardial Infarction in Systemic Lupus Erythematosus – the Sex-Specific Risk Profile
Current Pharmaceutical Design The Role of Oxidative Stress in Smoking-Related Diseases
Mini-Reviews in Organic Chemistry Diabetes and Complications: Cellular Signaling Pathways, Current Understanding and Targeted Therapies
Current Drug Targets Pulmonary Hypertension in COPD: Pathophysiology and Therapeutic Targets
Current Drug Targets Synthesis and Enzymological Characterization of Some 2-(Substitutedphenylamino) quinazolin-4(3H)-one Derivatives as Potent α-Glucosidase Inhibitors In Vitro
Letters in Drug Design & Discovery miRNAs in Cancer Prevention and Treatment and as Molecular Targets for Natural Product Anticancer Agents
Current Cancer Drug Targets New Challenges for ACE-Inhibitors in Vascular Diseases
Drug Design Reviews - Online (Discontinued) Dynamic Role of Microparticles in Type 2 Diabetes Mellitus
Current Diabetes Reviews Antioxidative Properties of Flavonoids
Current Organic Chemistry Lysophosphatidic Acid and Ischemic Stroke
Vascular Disease Prevention (Discontinued) Recent Progress of Medicinal Chemistry Research on Peroxisome Proliferator-Activated Receptor (PPAR) Ligands for the Treatment of Metabolic Syndrome
Current Bioactive Compounds Ultrasound Features of Polycystic Ovaries and Syndrome X: A Pilot Study
Vascular Disease Prevention (Discontinued)