Abstract
We aim from this review to stimulate further research in this area by providing a description of the different types of inhibitors containing heparin mimetic molecules that have recently been reported and data on their biological activity. Molecules that mimic heparin and bind to heparin-binding growth factors are important building blocks for synthetic biomaterials. Different types of synthetic mimics of the biological properties of heparin have been prepared including high molecular weight compounds or small molecule mimics. Peptide-based mimics of heparin functionality are limited and because of their low degree of sulfation, they are natural targets as heparin mimics. Aromatic sulfonamide derivatives exhibit a range of bioactivities and a novel angiogenesis inhibitor (E 7820) is used as a TF model for screening assay. The anticoagulant activity of the known heparin pentasaccharide sequence prompted synthetic efforts aimed at the procurement of this structure as well as a host of related sequences. Chemical modification of the natural or synthetic heparin increased factor activation of AT III Xa affinity. A variety of non-peptide non-saccharides inhibitors as antiangiogenesis therapies directed against the VEGFR kinase are a promising and well-validated therapeutic approach under active evaluation of their safety and efficacy in multiple clinical trials. These low molecular weight modulators could be useful tools for biologists and may have potential as drugs or as leads for drug development.
Keywords: FGF family, heparin, angiogenesis, tumor, peptides, glycosides, polymers, inhibitors
Mini-Reviews in Medicinal Chemistry
Title: Chemistry and Biology of Heparin Mimetics that Bind to Fibroblast Growth Factors
Volume: 7 Issue: 12
Author(s): Hammed H.A.M. Hassan
Affiliation:
Keywords: FGF family, heparin, angiogenesis, tumor, peptides, glycosides, polymers, inhibitors
Abstract: We aim from this review to stimulate further research in this area by providing a description of the different types of inhibitors containing heparin mimetic molecules that have recently been reported and data on their biological activity. Molecules that mimic heparin and bind to heparin-binding growth factors are important building blocks for synthetic biomaterials. Different types of synthetic mimics of the biological properties of heparin have been prepared including high molecular weight compounds or small molecule mimics. Peptide-based mimics of heparin functionality are limited and because of their low degree of sulfation, they are natural targets as heparin mimics. Aromatic sulfonamide derivatives exhibit a range of bioactivities and a novel angiogenesis inhibitor (E 7820) is used as a TF model for screening assay. The anticoagulant activity of the known heparin pentasaccharide sequence prompted synthetic efforts aimed at the procurement of this structure as well as a host of related sequences. Chemical modification of the natural or synthetic heparin increased factor activation of AT III Xa affinity. A variety of non-peptide non-saccharides inhibitors as antiangiogenesis therapies directed against the VEGFR kinase are a promising and well-validated therapeutic approach under active evaluation of their safety and efficacy in multiple clinical trials. These low molecular weight modulators could be useful tools for biologists and may have potential as drugs or as leads for drug development.
Export Options
About this article
Cite this article as:
Hassan H.A.M. Hammed, Chemistry and Biology of Heparin Mimetics that Bind to Fibroblast Growth Factors, Mini-Reviews in Medicinal Chemistry 2007; 7 (12) . https://dx.doi.org/10.2174/138955707782795665
DOI https://dx.doi.org/10.2174/138955707782795665 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Insight γ-Secretase: Structure, Function, and Role in Alzheimer’s Disease
Current Drug Targets Chemopreventive Properties of Peptide Lunasin: A Review
Protein & Peptide Letters Synthesis and Preliminary Evaluation of n.c.a. Iodoquine: A Novel Radiotracer with High Uptake in Cells with High ALDH1 Expression
Current Radiopharmaceuticals Targeting the RAS Signaling Pathway in Malignant Hematologic Diseases
Current Drug Targets Chemotherapy and Cardiotoxicity in Hematologic Malignancies
Current Cancer Drug Targets Amberlyst-15® in PEG-400: Green Synthesis of 3-Benzoyl-5-Hydroxy Benzofuran and Naphtho[1,2-b]furan Derivatives at Room Temperature
Letters in Organic Chemistry Stabilization of Eukaryotic Topoisomerase II-DNA Cleavage Complexes
Current Topics in Medicinal Chemistry Advances in the Systemic Treatment of Neuroendocrine Tumors in the Era of Molecular Therapy
Anti-Cancer Agents in Medicinal Chemistry Patent Selections
Recent Patents on Cardiovascular Drug Discovery Overexpression of p62 Induces Autophagy and Promotes Proliferation, Migration and Invasion of Nasopharyngeal Carcinoma Cells through Promoting ERK Signaling Pathway
Current Cancer Drug Targets The Identification of a Novel Unsymmetrical Azine as an Apoptosis Inducer in Colorectal Cancer
Anti-Cancer Agents in Medicinal Chemistry Antiestrogenic Therapies in Solid Cancers and Multiple Myeloma
Current Molecular Medicine LncRNA in Tumorigenesis Microenvironment
Current Bioinformatics Suppression of NF-κB Signaling and P-glycoprotein Function by Gambogic Acid Synergistically Potentiates Adriamycin -induced Apoptosis in Lung Cancer
Current Cancer Drug Targets Inhibition of Glycolysis and Glutaminolysis: An Emerging Drug Discovery Approach to Combat Cancer
Current Topics in Medicinal Chemistry Antiproliferative Effects of Nerium oleander Leaves and Their Cardiac Glycosides Odoroside A and Oleandrin on MCF-7 Cancer Cells
Current Traditional Medicine Sphingolipid Metabolism and Leukemia: A Potential for Novel Therapeutic Approaches
Anti-Cancer Agents in Medicinal Chemistry STAT3: A Molecular Target for Cancer Whose Time Has Come
Current Signal Transduction Therapy Salinomycin Modulates the Expression of mRNAs and miRNAs Related to Stemness in Endometrial Cancer
Current Pharmaceutical Biotechnology Development of Lymphatic Vessels: Tumour Lymphangiogenesis and Lymphatic Invasion
Current Medicinal Chemistry