摘要
Eph-ephrin系统是多种疾病包括癌症,糖尿病,神经退行性疾病和炎症的一个潜在的新靶点。过去十年中,在开发Eph受体小分子拮抗剂方面已作出一些努力。天然和合成的化合物被发现,如(聚)苯酚和甾体衍生物,α1激动剂多沙唑嗪,2,5-二甲基吡咯 - 1-苯甲酸及石胆酸和其他氨基酸的结合物。本文为这些化合物提供可用的数据,并讨论其作为药理学工具或领先优化程序的候选者的潜在有效性。
关键词: Eph,肝配蛋白,药物发现,小分子,蛋白质 - 蛋白质,拮抗剂
图形摘要
Current Drug Targets
Title:Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors
Volume: 16 Issue: 10
Author(s): Massimiliano Tognolini and Alessio Lodola
Affiliation:
关键词: Eph,肝配蛋白,药物发现,小分子,蛋白质 - 蛋白质,拮抗剂
摘要: Eph-ephrin system is emerging as a new potential target in several diseases including cancer, diabetes, neurodegenerative diseases and inflammation. In the last decade, several efforts have been made to develop small molecule antagonists of Eph receptors. Both natural and synthetic compounds were discovered with (poly) phenol and steroidal derivatives on one side and the α1 agonist doxazosin, 2,5-dimethylpyrrol- 1-yl-benzoic acids and amino acid conjugates of lithocholic acid on the other. In the present paper we critically present available data for these compounds and discuss their potential usefulness as pharmacological tools or as candidates for a lead-optimization program.
Export Options
About this article
Cite this article as:
Massimiliano Tognolini and Alessio Lodola , Targeting the Eph-ephrin System with Protein-Protein Interaction (PPI) Inhibitors, Current Drug Targets 2015; 16 (10) . https://dx.doi.org/10.2174/1389450116666150825144457
DOI https://dx.doi.org/10.2174/1389450116666150825144457 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Related Journals
Related Books
- 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
-
In Vitro Evidence for Competitive TSPO Binding of the Imaging Biomarker Candidates Vinpocetine and Two Iodinated DAA1106 Analogues in Post Mortem Autoradiography Experiments on Whole Hemisphere Human Brain Slices
Current Radiopharmaceuticals Tumour Mutation Profiling with High-throughput Multiplexed Genotyping: A Review of its Use for Guiding Targeted Cancer Therapy
Current Cancer Therapy Reviews PLGA Hollow Microbubbles Loaded with Iron Oxide Nanoparticles and Doxorubicin for Dual-mode US/MR Imaging and Drug Delivery
Current Nanoscience Advances in Oncolytic Virus Therapy for Glioma
Recent Patents on CNS Drug Discovery (Discontinued) Endothelial Cell Targeted Molecular Imaging in Tumor Angiogenesis: Strategies and Current Status
Current Pharmaceutical Biotechnology Cancer-Targeting Multifunctionalized Gold Nanoparticles in Imaging and Therapy
Current Medicinal Chemistry Protein Kinase C as a Drug Target Implications for Drug or Diet Prevention and Treatment of Cancer
Current Drug Targets Role of Unani Medicines in Cancer Control and Management
Current Drug Therapy The Molecular Basis of Herpesviruses as Oncolytic Agents
Current Pharmaceutical Biotechnology Targeting SKCa Channels in Cancer: Potential New Therapeutic Approaches
Current Medicinal Chemistry Implications of Nanoscale Based Drug Delivery Systems in Delivery and Targeting Tubulin Binding Agent, Noscapine in Cancer Cells
Current Drug Metabolism Withdrawal Notice: Circulatory Cells as Tumortropic Carrier for Targetability Improvement
Current Drug Delivery Clinical Molecular Imaging with PET Agents Other than 18F-FDG
Current Pharmaceutical Biotechnology Low Concentration of Salinomycin Prevents Regrowth and Partially Depletes Human Glioma Cells Surviving High Concentrations of Alkylating Agents
Clinical Cancer Drugs Role of Aberrant Lipid Metabolism of Cancer Stem Cells in Cancer Progression
Current Cancer Drug Targets Gankyrin Oncoprotein: Structure, Function, and Involvement in Cancer
Current Chemical Biology Gene Therapy: The First Approved Gene-Based Medicines, Molecular Mechanisms and Clinical Indications
Current Molecular Pharmacology Metabolic Targeting of Cancers: From Molecular Mechanisms to Therapeutic Strategies
Current Medicinal Chemistry Vascular Endothelial Growth Factor in Central Nervous System Injuries – A Vascular Growth Factor Getting Nervous?
Current Neurovascular Research Tumour Targeting with Systemically Administered Bacteria
Current Gene Therapy