Abstract
This article presents a simplified view of integrins with emphasis on the α4 (α4β1/VLA-4) integrin. Integrins are heterodimeric proteins expressed on the cell surface of leukocytes that participate in a wide variety of functions, such as survival, growth, differentiation, migration, inflammatory responses, tumour invasion, among others. When the extracellular matrix is degraded or deformed, cells are forced to undergo responsive changes that influence remodelling during physiological and pathological events. Integrins recognize these changes and trigger a series of cellular responses, forming a physical connection between the interior and the outside of the cell. The communication of integrins through the plasma membrane occurs in both directions, from the extracellular to the intracellular (outside-in) and from the intracellular to the extracellular (inside-out). Integrins are valid targets for antibodies and small-molecule antagonists. One example is the monoclonal antibody natalizumab, marketed under the name of TYSABRI®, used in the treatment of recurrent multiple sclerosis, which inhibits the adhesion of α4 integrin to its counter-receptor. α4β1 Integrin antagonists are summarized here, and their utility as therapeutics are also discussed.
Keywords: Integrin, target, adhesion molecule, CD49d, VLA-4, α4, α4β1 integrin antagonists, extracellular matrix.
Current Medicinal Chemistry
Title:An Overview of the α4β1 Integrin and the Potential Therapeutic Role of its Antagonists
Volume: 28 Issue: 29
Author(s): Elenilze F.B. Ferreira , Luciane B. Silva , Josiane V. Cruz, Pedro H.F. Araújo, Njogu M. Kimani, Franco H.A. Leite , Joaquín M. Campos *Cleydson B.R. Santos
Affiliation:
- Department of Pharmaceutical and Organic Chemistry, Faculty of Pharmacy, Campus of Cartuja, University of Granada, 18071 Granada,Spain
Keywords: Integrin, target, adhesion molecule, CD49d, VLA-4, α4, α4β1 integrin antagonists, extracellular matrix.
Abstract: This article presents a simplified view of integrins with emphasis on the α4 (α4β1/VLA-4) integrin. Integrins are heterodimeric proteins expressed on the cell surface of leukocytes that participate in a wide variety of functions, such as survival, growth, differentiation, migration, inflammatory responses, tumour invasion, among others. When the extracellular matrix is degraded or deformed, cells are forced to undergo responsive changes that influence remodelling during physiological and pathological events. Integrins recognize these changes and trigger a series of cellular responses, forming a physical connection between the interior and the outside of the cell. The communication of integrins through the plasma membrane occurs in both directions, from the extracellular to the intracellular (outside-in) and from the intracellular to the extracellular (inside-out). Integrins are valid targets for antibodies and small-molecule antagonists. One example is the monoclonal antibody natalizumab, marketed under the name of TYSABRI®, used in the treatment of recurrent multiple sclerosis, which inhibits the adhesion of α4 integrin to its counter-receptor. α4β1 Integrin antagonists are summarized here, and their utility as therapeutics are also discussed.
Export Options
About this article
Cite this article as:
Ferreira F.B. Elenilze, Silva B. Luciane , Cruz V. Josiane , Araújo H.F. Pedro , Kimani M. Njogu , Leite H.A. Franco , Campos M. Joaquín *, Santos B.R. Cleydson , An Overview of the α4β1 Integrin and the Potential Therapeutic Role of its Antagonists, Current Medicinal Chemistry 2021; 28 (29) . https://dx.doi.org/10.2174/0929867328666210217153609
DOI https://dx.doi.org/10.2174/0929867328666210217153609 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...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
- Announcements
Related Articles
-
Immunotherapeutic and Immunoregulatory Drugs in Haematologic Malignancies
Current Topics in Medicinal Chemistry Targeting Transcription Factor Binding to DNA by Competing with DNA Binders as an Approach for Controlling Gene Expression
Current Topics in Medicinal Chemistry Coumarins as Antioxidants
Current Medicinal Chemistry Stable Expression of the Sodium/Iodide Symporter (NIS) for anti-Cancer Gene Therapy of Glioma Cells Using a Third Generation Self-Inactivating Lentiviral Vector System in Combination with 211At
Current Radiopharmaceuticals Promising Activity of Mammalian Target of Rapamycin Inhibitors in Hematologic Malignancies Therapy
Current Signal Transduction Therapy Tumor Stem Cell Niches: A New Functional Framework for the Action of Anticancer Drugs
Recent Patents on Anti-Cancer Drug Discovery Molecular Docking Study, Cytotoxicity, Cell Cycle Arrest and Apoptotic Induction of Novel Chalcones Incorporating Thiadiazolyl Isoquinoline in Cervical Cancer
Anti-Cancer Agents in Medicinal Chemistry A Role for the Inflammatory Mediators Cox-2 and Metalloproteinases in Cancer Stemness
Anti-Cancer Agents in Medicinal Chemistry Cancer Stem Cells: The ‘Achilles Heel’ of Chemo-Resistant Tumors
Recent Patents on Anti-Cancer Drug Discovery Cancer Stem Cells – Are Surface Markers Alone Sufficient?
Current Stem Cell Research & Therapy The Current Chemical Utility of Marine and Terrestrial Filamentous Fungi in Side-Chain Chemistry
Current Organic Chemistry Targeting Sphingosine-1-Phosphate in Hematologic Malignancies
Anti-Cancer Agents in Medicinal Chemistry Apoptosis and Autophagy Induction As Mechanism of Cancer Prevention by Naturally Occurring Dietary Agents
Current Drug Targets ANN-QSAR Model for Virtual Screening of Androstenedione C-Skeleton Containing Phytomolecules and Analogues for Cytotoxic Activity Against Human Breast Cancer Cell Line MCF-7
Combinatorial Chemistry & High Throughput Screening Nutrition Support of Patients Undergoing Hematopoietic Stem Cell Transplantation (HSCT)
Current Nutrition & Food Science The Role of Retinoids in the Adult Nervous System and their Therapeutic Potential
Mini-Reviews in Medicinal Chemistry NF-κB Blockers Gifted by Mother Nature: Prospectives in Cancer Cell Chemosensitization
Current Pharmaceutical Design How is Gene Transfection Able to Improve Current Chemotherapy? The Role of Combined Therapy in Cancer Treatment
Current Medicinal Chemistry Retinoid Receptors in Inflammatory Responses: A Potential Target for Pharmacology
Current Drug Targets - Inflammation & Allergy Triggering PIK3CA Mutations in PI3K/Akt/mTOR Axis: Exploration of Newer Inhibitors and Rational Preventive Strategies
Current Pharmaceutical Design