Abstract
Aminopeptidase N (APN/CD13) of the M1 family is a broad specificity enzyme that is intimately involved in tumor angiogenesis and metastasis. Asparagine–glycine–arginine (NGR) is a tumor-homing tripeptide, which can selectively combine with APN/CD13 that is overexpressed on the surface of some tumor cells. Various anti-tumor drugs can be conjugated to NGR to improve selectivity, efficacy, and to decrease drug toxicity. In this study, a tripeptide NGR(NO2) was synthesized and conjugated with 5-fluorouracil. The anti-tumor activities of this new prodrug were evaluated in vivo. More significant anti-tumor effects were observed over the parent 5-fluorouracil.
Keywords: Aminopeptidase N, NGR, 5-fluorouracil, antitumor, angiogenesis, metastasis, tumor cells, tumor-homing tripeptide, 5-fluorouracil
Protein & Peptide Letters
Title:Design, Synthesis, and Activity Evaluation of a New 5-fluorouracil Prodrug Containing an Asn-Gly-Arg(NO2)COOCH3 Tripeptide
Volume: 19 Issue: 10
Author(s): Yepeng Luan, Fanbo Jing, Jian Zhang, Mingming Zou, Xuejian Wang, Yuping Jia, Ning Liu, Jiajia Mou and Wenfang Xu
Affiliation:
Keywords: Aminopeptidase N, NGR, 5-fluorouracil, antitumor, angiogenesis, metastasis, tumor cells, tumor-homing tripeptide, 5-fluorouracil
Abstract: Aminopeptidase N (APN/CD13) of the M1 family is a broad specificity enzyme that is intimately involved in tumor angiogenesis and metastasis. Asparagine–glycine–arginine (NGR) is a tumor-homing tripeptide, which can selectively combine with APN/CD13 that is overexpressed on the surface of some tumor cells. Various anti-tumor drugs can be conjugated to NGR to improve selectivity, efficacy, and to decrease drug toxicity. In this study, a tripeptide NGR(NO2) was synthesized and conjugated with 5-fluorouracil. The anti-tumor activities of this new prodrug were evaluated in vivo. More significant anti-tumor effects were observed over the parent 5-fluorouracil.
Export Options
About this article
Cite this article as:
Luan Yepeng, Jing Fanbo, Zhang Jian, Zou Mingming, Wang Xuejian, Jia Yuping, Liu Ning, Mou Jiajia and Xu Wenfang, Design, Synthesis, and Activity Evaluation of a New 5-fluorouracil Prodrug Containing an Asn-Gly-Arg(NO2)COOCH3 Tripeptide, Protein & Peptide Letters 2012; 19 (10) . https://dx.doi.org/10.2174/092986612802762615
DOI https://dx.doi.org/10.2174/092986612802762615 |
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
-
Diverse Models for the Prediction of Dual mTOR and PI3Kα Inhibitory Activities of Substituted 4-morpholinopyrrolopyrimidines
Letters in Drug Design & Discovery Exercise and Cognitive-Behavioural Treatment in Fibromyalgia Syndrome
Current Pharmaceutical Design Glycine Site Modulators and Glycine Transporter-1 Inhibitors as Novel Therapeutic Targets for the Treatment of Schizophrenia
Current Neuropharmacology Critical Illness in the Obese Patient
Current Respiratory Medicine Reviews Viral Entry Inhibitors Targeting Six-Helical Bundle Core against Highly Pathogenic Enveloped Viruses with Class I Fusion Proteins
Current Medicinal Chemistry On the Psychotropic Effects of Carbon Dioxide
Current Pharmaceutical Design Protein Homeostasis as a Therapeutic Target for Diseases of Protein Conformation
Current Topics in Medicinal Chemistry Antibacterial Activity of Lipophilic Fluoroquinolone Derivatives
Medicinal Chemistry Enantioselective Organocatalytic Reactions with Isatin
Current Organic Chemistry Human- and Virus-Encoded microRNAs as Potential Targets of Antiviral Therapy
Mini-Reviews in Medicinal Chemistry Graphical Abstracts
Current Organic Chemistry Multi-Targeted Molecular Docking and Drug-Likeness Evaluation of some Nitrogen Heterocyclic Compounds Targeting Proteins Involved in the Development of COVID-19
Medicinal Chemistry Double-Faced Role of Human Mesenchymal Stem Cells and their Role/Challenges in Cancer Therapy
Current Stem Cell Research & Therapy Preface
Mini-Reviews in Medicinal Chemistry Diagnostic Performance of Radiology Residents in Thoracic CT Imaging in Emergency Radiology During The COVID-19 Pandemic
Current Medical Imaging Patent Selections
Recent Patents on Anti-Infective Drug Discovery Independent Component Analysis Applied to Pharmacological Magnetic Resonance Imaging (phMRI): New Insights Into the Functional Networks Underlying Panic Attacks as Induced by CCK-4
Current Pharmaceutical Design Biomarkers for Risk Assessment and Prevention of Breast Cancer
Current Cancer Drug Targets Selective Chemokine Receptor-Targeted Depletion of Pathological Cells as A Therapeutic Strategy for Inflammatory, Allergic and Autoimmune Diseases
Recent Patents on Inflammation & Allergy Drug Discovery In Silico Studies in ADME/Tox: Caveat Emptor
Current Computer-Aided Drug Design