Abstract
Integrins are a large family of dimeric receptors composed by α and β subunits that, once bound to extracellular matrix (ECM) proteins, regulate a variety of cellular processes such as cell motility, migration, and proliferation. The integrins transduce signals from inside-out and outside-in the cell, thus representing the cellular link to the external environment. For these properties, integrin activation has been involved in pathological processes like tumor growth and metastasis formation. Recent advances in the elucidation of the crystallographic structures of the αvβ3 and αIIβ3 integrins are promoting studies focused to the search of small molecule antagonists that can block the integrin binding to ECM and inhibit the biological effects exerted by these receptors. In this review we will focus on small molecule antagonists of αvβ3 and αvβ5 integrin as tools for cancer therapy while other integrins will only be briefly mentioned. Cilengitide (cyclic peptidic αvβ3 and αvβ5 antagonist) is currently in clinical trials for anti cancer therapy. Combination of integrin αvβ3 antagonists and other traditional therapeutic approaches may represent a future strategy to inhibit tumor growth and metastasis spreading.
Keywords: Integrin antagonists, RGD-peptides, metastasis, anoikis
Call for Papers in Thematic Issues
Biodiversity, Ethnopharmacology, Biotechnology, Bioclimatology and Scientific Education Applied to Toxicology and One Health
Neglected Tropical Diseases (NTDs) are represented by a group of distinct illnesses that affect the most vulnerable segment of the population, negatively impacting the Economy and Public Health. For example, like snakebite, leishmaniasis disproportionately affects vulnerable populations in tropical and subtropical regions. The search for safe drugs against various diseases ...read more
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
Chemistry of Materials and Emerging Techniques: Future of Drug Discovery and Medicinal Product Developments
In drug discovery, established knowledge of functional groups, their chemical behaviors, and structure-activity relationships favor chemists to achieve desired efficacy and safety profiles within the novel designed medicinal products. Here, judicious integration of different tools and techniques of chemistry also plays a fundamental role towards the selection of the processes ...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
Related Journals
Anti-Cancer Agents in Medicinal Chemistry
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Current Bioactive Compounds
Current Cancer Drug Targets
Combinatorial Chemistry & High Throughput Screening
Current Cancer Therapy Reviews
Current Diabetes Reviews
Current Drug Safety
Current Drug Targets
Current Drug Therapy
Related Books
Bioactive Compounds Targeting Neurodegenerative Diseases
Anthraquinones: Bioactive Multifaceted Therapeutic Agents
Therapeutic Plants: Recent Advances in the Use of Herbs as Alternative Medications
Quality Assurance of Ethno-Herbals: Cultivating Confidence in Alternative Medicine
Traditional Medicine in North East Africa: Research on Traditional Healer Preparations and Herbs
Andrographolide and its Analogs: Botanical Sources, Phytochemistry, Pharmacology, and Biotechnology
Metabolites of Medicinal Plants: Insightful Approaches
Herbs for Disease Prevention and Treatment
Anthocyanins: Pharmacology and Nutraceutical Importance
Therapeutic Insights into Herbal Medicine through the Use of Phytomolecules
43
