Abstract
Lamprey gonadotropin-releasing hormone-III (lGnRH-III; Glp-His-Trp-Ser-His-Asp-Trp-Lys-Pro-Gly-NH2), a native isoform of human GnRH (GnRH-I), was initially isolated from the brain of the sea lamprey (Petromyzon marinus). It is a weak GnRH agonist, which exerts a direct antiproliferative effect on cancer cells and has an insignificant LH and FSH releasing potency in mammals. These features reveal the advantages of lGnRH-III and its derivatives for use in cancer therapy. Here we give an overview of various strategies to increase the antitumor activity of lGnRH-III, such as amino acid replacement, cyclization, dimerization and conjugation to polymers or to chemotherapeutic agents. In vitro and in vivo antitumor activity of lGnRH-III based compounds was demonstrated both on hormone dependent and independent tumors.
Keywords: Lamprey gonadotropin-releasing hormone-III (lGnRH-III), anticancer activity, targeted cancer chemotherapy, anthracyclines, peptide dimers, drug - peptide conjugates, antiproliferative effect, chemotherapeutic agent, tumor, steroid
Protein & Peptide Letters
Title:lGnRH-III - a Promising Candidate for Anticancer Drug Development
Volume: 20 Issue: 4
Author(s): Marilena Manea and Gabor Mezo
Affiliation:
Keywords: Lamprey gonadotropin-releasing hormone-III (lGnRH-III), anticancer activity, targeted cancer chemotherapy, anthracyclines, peptide dimers, drug - peptide conjugates, antiproliferative effect, chemotherapeutic agent, tumor, steroid
Abstract: Lamprey gonadotropin-releasing hormone-III (lGnRH-III; Glp-His-Trp-Ser-His-Asp-Trp-Lys-Pro-Gly-NH2), a native isoform of human GnRH (GnRH-I), was initially isolated from the brain of the sea lamprey (Petromyzon marinus). It is a weak GnRH agonist, which exerts a direct antiproliferative effect on cancer cells and has an insignificant LH and FSH releasing potency in mammals. These features reveal the advantages of lGnRH-III and its derivatives for use in cancer therapy. Here we give an overview of various strategies to increase the antitumor activity of lGnRH-III, such as amino acid replacement, cyclization, dimerization and conjugation to polymers or to chemotherapeutic agents. In vitro and in vivo antitumor activity of lGnRH-III based compounds was demonstrated both on hormone dependent and independent tumors.
Export Options
About this article
Cite this article as:
Manea Marilena and Mezo Gabor, lGnRH-III - a Promising Candidate for Anticancer Drug Development, Protein & Peptide Letters 2013; 20 (4) . https://dx.doi.org/10.2174/0929866511320040008
DOI https://dx.doi.org/10.2174/0929866511320040008 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
- 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
-
Inhibition of Dipeptidyl Peptidase-4 (DPP-4) - A Novel Approach to Treat Type 2 Diabetes
Current Enzyme Inhibition Wasp Venom Toxins as a Potential Therapeutic Agent
Protein & Peptide Letters Relaxin Receptors - New Drug Targets for Multiple Disease States
Current Drug Targets Synthesis, Anti-inflammatory and Molecular Docking Study of Schiff Bases Containing Methanesulphonyl Pharmacophore
Letters in Drug Design & Discovery Quinones Derived from Plant Secondary Metabolites as Anti-cancer Agents
Anti-Cancer Agents in Medicinal Chemistry Meet Our Editorial Board Member:
Current Medicinal Chemistry Carbon Nanotubes in the Treatment of Skin Cancers: Safety and Toxic ological Aspects
Pharmaceutical Nanotechnology The Role of Mitochondria in Cancer Induction, Progression and Changes in Metabolism
Mini-Reviews in Medicinal Chemistry Light-at-Night-Induced Circadian Disruption, Cancer and Aging
Current Aging Science Signaling Through Rho GTPase Pathway as Viable Drug Target
Current Medicinal Chemistry Recent Patents on Light Based Therapies: Photodynamic Therapy, Photothermal Therapy and Photoimmunotherapy
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Sperm Quality in Mouse After Exposure to Low Doses of TCDD
Current Topics in Medicinal Chemistry Bortezomib in the Treatment of Cancer
Recent Patents on Anti-Cancer Drug Discovery Production and Application of Copper Radiopharmaceuticals
Current Radiopharmaceuticals Inflammation, Serotonin and Major Depression
Current Drug Targets Synthesis and Screening of Pro-apoptotic and Angio-inhibitory Activity of Novel Benzisoxazole Derivatives both In Vitro and In Vivo
Anti-Cancer Agents in Medicinal Chemistry Non-Viral Delivery of RNA Interference Targeting Cancer Cells in Cancer Gene Therapy
Current Gene Therapy Meet Our Editorial Board Member
Current Drug Targets CD26/Dipeptidyl Peptidase IV as a Novel Therapeutic Target for Cancer and Immune Disorders
Mini-Reviews in Medicinal Chemistry miR-15b and miR-21 as Circulating Biomarkers for Diagnosis of Glioma
Current Genomics