Abstract
Lys49-phospholipase A2 homologues constitute a large family of toxins present in the venoms of viperid snake species, which despite lacking catalytic activity, cause significant skeletal muscle necrosis. The main structural determinants of this toxic effect have been experimentally mapped to a region near their C-terminus (115-129), which combines cationic and hydrophobic/aromatic amino acid residues. Short (13-mer) synthetic peptides representing this C-terminal region can mimick several of the effects of Lys49 PLA2 homologues. In addition to their ability to damage muscle cells, these peptides display antibacterial, antiendotoxic, antifungal, antiparasite, and antitumor activities, as well as VEGF-receptor 2 (KDR)-binding and heparin-binding properties. Modifications of their sequences have shown possibilities to enhance their effects upon prokaryotic cells, while decreasing toxicity for eukaryotic cells. This review presents an updated summary on the biomimetic actions exerted by such peptides, and highlights their potential value as molecular tools or as drug leads in diverse biomedical areas.
Keywords: Synthetic peptides, phospholipase A2, snake venom, biomimetic, antimicrobial, antitumor, VEGF, heparin
Current Pharmaceutical Design
Title: Synthetic Peptides Derived from the C-Terminal Region of Lys49 Phospholipase A2 Homologues from Viperidae Snake Venoms: Biomimetic Activities and Potential Applications
Volume: 16 Issue: 28
Author(s): Bruno Lomonte, Yamileth Angulo and Edgardo Moreno
Affiliation:
Keywords: Synthetic peptides, phospholipase A2, snake venom, biomimetic, antimicrobial, antitumor, VEGF, heparin
Abstract: Lys49-phospholipase A2 homologues constitute a large family of toxins present in the venoms of viperid snake species, which despite lacking catalytic activity, cause significant skeletal muscle necrosis. The main structural determinants of this toxic effect have been experimentally mapped to a region near their C-terminus (115-129), which combines cationic and hydrophobic/aromatic amino acid residues. Short (13-mer) synthetic peptides representing this C-terminal region can mimick several of the effects of Lys49 PLA2 homologues. In addition to their ability to damage muscle cells, these peptides display antibacterial, antiendotoxic, antifungal, antiparasite, and antitumor activities, as well as VEGF-receptor 2 (KDR)-binding and heparin-binding properties. Modifications of their sequences have shown possibilities to enhance their effects upon prokaryotic cells, while decreasing toxicity for eukaryotic cells. This review presents an updated summary on the biomimetic actions exerted by such peptides, and highlights their potential value as molecular tools or as drug leads in diverse biomedical areas.
Export Options
About this article
Cite this article as:
Lomonte Bruno, Angulo Yamileth and Moreno Edgardo, Synthetic Peptides Derived from the C-Terminal Region of Lys49 Phospholipase A2 Homologues from Viperidae Snake Venoms: Biomimetic Activities and Potential Applications, Current Pharmaceutical Design 2010; 16 (28) . https://dx.doi.org/10.2174/138161210793292456
DOI https://dx.doi.org/10.2174/138161210793292456 |
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
-
Recent Advances in the Research and Development of B-Raf Inhibitors
Current Medicinal Chemistry Synthesis of Phenol-derivatives and Biological Screening for Anticancer Activity
Anti-Cancer Agents in Medicinal Chemistry Chemomodulating Effects of Flavonoids in Human Leukemia Cells
Anti-Cancer Agents in Medicinal Chemistry The Use of Interferons in Respiratory Diseases
Current Respiratory Medicine Reviews Modeling and Proposed Molecular Mechanism of Hydroxyurea Through Docking and Molecular Dynamic Simulation to Curtail the Action of Ribonucleotide Reductase
Recent Patents on Anti-Cancer Drug Discovery Clinical Applications and Biosafety of Human Adult Mesenchymal Stem Cells
Current Pharmaceutical Design Editorial (Hot Topic: Computer-Aided Drug Design, Synthesis and Evaluation of New Anti-Cancer Drugs)
Current Topics in Medicinal Chemistry Anti-Angiogenic Therapies for Children with Cancer
Current Cancer Drug Targets Gene Silencing in the Development of Personalized Cancer Treatment: The Targets, the Agents and the Delivery Systems
Current Gene Therapy The Effect of Krill Oil and n-3 Polyunsaturated Fatty Acids on Human Osteosarcoma Cell Proliferation and Migration
Current Drug Targets Back Pain in Children and Adolescents: Etiology, Clinical Approach and Treatment
Current Pediatric Reviews Circulating microRNAs as Potential Diagnostic, Prognostic and Therapeutic Targets in Pancreatic Cancer
Current Pharmaceutical Design Lipid-Based Nanoparticulate Systems for the Delivery of Anti-Cancer Drug Cocktails: Implications on Pharmacokinetics and Drug Toxicities
Current Drug Metabolism Protein Aggregation and Defective RNA Metabolism as Mechanisms for Motor Neuron Damage
CNS & Neurological Disorders - Drug Targets Radiation and Gene Therapy: Rays of Hope for the New Millennium?
Current Gene Therapy Modulation of Gene Transcription by Natural Products - A Viable Anticancer Strategy
Current Pharmaceutical Design Current Advances in the Synthesis and Antitumoral Activity of SIRT1-2 Inhibitors by Modulation of p53 and Pro-Apoptotic Proteins
Current Medicinal Chemistry Structural Characterization of Recombinant Therapeutic Proteins by Circular Dichroism
Current Pharmaceutical Biotechnology Safety of Nanoparticles in Medicine
Current Drug Targets Structure of the Epidermal Growth Factor Receptor Gene and Intron Recombination in Human Gliomas
Current Genomics