Abstract
Ten new RGD (Arginine-Glycine-Aspartic acid) peptidomimetics have been synthesized and screened for their affinity to αvβ3 integrin receptor. Arginine and Aspartic acid mimetic subunits were connected through 1,2,3-triazole as central scaffold by click chemistry, affording the final products with good yields. Among them, compounds 3f-j exhibited high affinity to the receptor,with IC50 in the low nanomolar range, comparable to that of the reference compound Cilengitide.
Keywords: RGD peptidomimetics, αvβ3 integrin, Osteoporosis, 1,2,3-Triazole, Click chemistry, RGD, v 3 Integrin Affinity, peptide, aspartic acid, heterocyclic scaffolds, cycloaddition
Letters in Drug Design & Discovery
Title: Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and αvβ3 Integrin Affinity
Volume: 8 Issue: 5
Author(s): Ming Hong Ni, Emiliano Esposito, Massimo Castorina and Alma Dal Pozzo
Affiliation:
Keywords: RGD peptidomimetics, αvβ3 integrin, Osteoporosis, 1,2,3-Triazole, Click chemistry, RGD, v 3 Integrin Affinity, peptide, aspartic acid, heterocyclic scaffolds, cycloaddition
Abstract: Ten new RGD (Arginine-Glycine-Aspartic acid) peptidomimetics have been synthesized and screened for their affinity to αvβ3 integrin receptor. Arginine and Aspartic acid mimetic subunits were connected through 1,2,3-triazole as central scaffold by click chemistry, affording the final products with good yields. Among them, compounds 3f-j exhibited high affinity to the receptor,with IC50 in the low nanomolar range, comparable to that of the reference compound Cilengitide.
Export Options
About this article
Cite this article as:
Hong Ni Ming, Esposito Emiliano, Castorina Massimo and Dal Pozzo Alma, Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and αvβ3 Integrin Affinity, Letters in Drug Design & Discovery 2011; 8 (5) . https://dx.doi.org/10.2174/157018011795514258
DOI https://dx.doi.org/10.2174/157018011795514258 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Advances in Imaging Gene-Directed Enzyme Prodrug Therapy
Current Pharmaceutical Biotechnology Editorial: [Hot Topic: Inflammation and Cancer: New Targets and Novel Therapeutic Approach]
Current Pharmaceutical Design Cellular Iron Homeostasis and Therapeutic Implications of Iron Chelators in Cancer
Current Pharmaceutical Biotechnology Ultra-deformable Liposomes as Flexible Nanovesicular Carrier to Penetrate Versatile Drugs Transdermally
Nanoscience & Nanotechnology-Asia Primary Tumors of the Sacrum: Imaging Findings
Current Medical Imaging Lipid Based Nanoparticles as Inherent Reversing Agents of Multidrug Resistance in Cancer
Current Pharmaceutical Design Poxvirus Cancer Therapy
Recent Patents on Anti-Infective Drug Discovery Cyclin Dependent Kinase 1 Inhibitors: A Review of Recent Progress
Current Medicinal Chemistry A QSAR Analysis of Coumarin Derivatives as TNF-α Inhibitor - A Rational Approach to Anticancer Drug Design
Letters in Drug Design & Discovery Nanotechnology-based Drug Delivery Systems as Potential for Skin Application: A Review
Current Medicinal Chemistry Fumitremorgins and Relatives – From Tremorgenic Compounds to Valuable Anti-Cancer Drugs
Current Medicinal Chemistry Targeting Molecular Imaging of Breast Cancer by Radioimmunodetection Method in Nuclear Medicine
Current Molecular Imaging (Discontinued) Betulinic Acid as a Potent and Complex Antitumor Phytochemical: A Minireview
Anti-Cancer Agents in Medicinal Chemistry Biomimetic Drug Delivery Systems Oriented by Biological Function in Tumor Targeting
Current Drug Targets Nanocarriers Based Anticancer Drugs: Current Scenario and Future Perceptions
Current Drug Targets Clearance of Beta-Amyloid in the Brain
Current Medicinal Chemistry Matrix Metalloproteinases as Potential Targets in the Venous Dilation Associated with Varicose Veins
Current Drug Targets Tumor Necrosis Factor Alpha in Ulcerative Colitis and Diverticular Disease Associated Colitis
Endocrine, Metabolic & Immune Disorders - Drug Targets Neuroprotective Role of Hypothermia in Hypoxic-ischemic Brain Injury: Combined Therapies using Estrogen
Current Neuropharmacology Turning Tumor-Promoting Copper into an Anti-Cancer Weapon via High-Throughput Chemistry
Current Medicinal Chemistry