Abstract
The anti-coagulant activated protein C (APC) can exert direct effects on cells, including cytoprotective functions involving apoptosis and inflammation mechanisms. These cytoprotective properties of APC require the presence of protease-activated receptor-1 (PAR-1) and endothelial protein C receptor (EPCR) resulting in inhibition of inflammatory gene expression and down-regulation of p53 and Bax. Several in vitro and animal studies have documented such cytoprotective properties of APC. The first evidence for a cytoprotective role of APC in a clinical setting came from the PROWESS trial in which APC administration reduced mortality rates in severe sepsis patients. However, although APC certainly has the potential to be used in a broader range of clinical settings it is thwarted by the associated risk of bleeding. Further research within this area towards improved therapeutics of specific APC mutants has taken place.
Keywords: APC, anti-coagulation, cytoprotection, animal injury models
Mini-Reviews in Medicinal Chemistry
Title: Activated Protein C: A Promising Drug with Multiple Effects?
Volume: 9 Issue: 5
Author(s): S.T. B.G. Loubele, H. M.H. Spronk and H. ten Cate
Affiliation:
Keywords: APC, anti-coagulation, cytoprotection, animal injury models
Abstract: The anti-coagulant activated protein C (APC) can exert direct effects on cells, including cytoprotective functions involving apoptosis and inflammation mechanisms. These cytoprotective properties of APC require the presence of protease-activated receptor-1 (PAR-1) and endothelial protein C receptor (EPCR) resulting in inhibition of inflammatory gene expression and down-regulation of p53 and Bax. Several in vitro and animal studies have documented such cytoprotective properties of APC. The first evidence for a cytoprotective role of APC in a clinical setting came from the PROWESS trial in which APC administration reduced mortality rates in severe sepsis patients. However, although APC certainly has the potential to be used in a broader range of clinical settings it is thwarted by the associated risk of bleeding. Further research within this area towards improved therapeutics of specific APC mutants has taken place.
Export Options
About this article
Cite this article as:
Loubele B.G. S.T., Spronk M.H. H. and Cate ten H., Activated Protein C: A Promising Drug with Multiple Effects?, Mini-Reviews in Medicinal Chemistry 2009; 9 (5) . https://dx.doi.org/10.2174/138955709788167547
DOI https://dx.doi.org/10.2174/138955709788167547 |
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
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...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
- 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
-
Cardiac Aging and Insulin Resistance: Could Insulin/Insulin-Like Growth Factor (IGF) Signaling be used as a Therapeutic Target?
Current Pharmaceutical Design Therapeutic Angiogenesis in Ischemic Tissues by Growth Factors and Bone Marrow Mononuclear Cells Administration: Biological Foundation and Clinical Prospects
Current Stem Cell Research & Therapy The Activated Endocannabinoid System in Atherosclerosis: Driving Force or Protective Mechanism?
Current Drug Targets MicroRNAs in the Diagnosis and Treatment of Unstable Angina
Current Topics in Medicinal Chemistry Connexins as Precocious Markers and Molecular Targets for Chemical and Pharmacological Agents in Carcinogenesis
Current Medicinal Chemistry Simultaneous Separation, Quantitation, and Determination of the Dissociation Constant of Five Components of Ixeris sonchifolia by Microemulsion Electrokinetic Chromatography
Current Pharmaceutical Analysis Therapeutic Use of Heat Shock Protein 70
Recent Patents on DNA & Gene Sequences Vanilloid Receptor Antagonists: Emerging Class of Novel Anti-Inflammatory Agents for Pain Management
Current Pharmaceutical Design Radiopharmaceuticals for Oncology Drug Development: A Pharmaceutical Industry Perspective
Current Pharmaceutical Design ESVS Guidelines: Section B - Diagnosis and Investigation of Patients with Carotid Stenosis
Current Vascular Pharmacology Dietary Antioxidants as Potential Pharmacological Agents for Ischemic Stroke
Current Medicinal Chemistry Atrial Fibrillation – New Frontiers in Anticoagulation
Cardiovascular & Hematological Disorders-Drug Targets Atheroprotective Properties of Pigment Epithelium-Derived Factor (PEDF) in Cardiometabolic Disorders
Current Pharmaceutical Design Use of Antiplatelet Therapy after Percutaneous Coronary Intervention with Bare-Metal Stents and Different Types of Drug-Eluting Stents
Current Clinical Pharmacology MicroRNA-34a Promotes Cardiomyocyte Apoptosis Post Myocardial Infarction Through Down-regulating Aldehyde Dehydrogenase 2
Current Pharmaceutical Design Peptides as Signaling Inhibitors for Mammalian MAP Kinase Cascades
Current Pharmaceutical Design An Angiotensin II (Ang II) Type 1 Receptor Blocker, Telmisartan Protects Against Neurological Deficits and Prolongs Survival in Spontaneously Hypertensive Rats Stroke-Prone (SHR-SP) Infused with Ang II
Vascular Disease Prevention (Discontinued) Ischemic Colitis: Current Diagnosis and Treatment
Current Drug Targets Neurovascular Complications of Ovarian Hyperstimulation Syndrome (OHSS): From Pathophysiology to Recent Treatment Options
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Cerebroprotective Functions of HO-2
Current Pharmaceutical Design