pH Interfering Agents as Chemosensitizers In Cancer Therapy, Volume Thirteen provides a detailed overview of the chemosensitizers for the treatment of cancer spanning from biochemical and structural features to pharmacology and drug-design, including technological applications. The book is structured with innovative outlines and a distinction between experimental and clinical results. The continuous discovery and assessment of the role played by old/new synthetic drugs, natural compounds and technological applications has led to the urgent need of classification in terms of biological activity, mechanism of action, clinical outcomes, cancer cell lines sensible to the treatment, and potentialities to better orient research in this field.
Moreover, all the aspects relevant for medicinal chemistry (drug design, structure-activity relationships, permeability data, cytotoxicity, appropriate statistical procedures, and molecular modeling studies) are strictly considered.
- Presents a broad view of the topic according to a medicinal chemistry-based approach beyond syntheses and biological assays, focusing on SAR studies, chemoinformatic, drug targeting and molecular modeling
- Explains the mechanism of action of the chemosensitizers by means of schemes and figures to facilitate comprehension
- Discusses novel targets to explore new possibilities that enhance research in the field
PART I General overview of the topic: An update 1. General introduction about general mechanisms of resistance in cancer (hypoxia, efflux pumps, tumoral microenvironment) and use of chemosensitizers in association with drugs already in the market 2. Clinical studies analysis 3. Combination therapy 4. Oncoimmunology
PART II Chemosensitizing agents with a validated mechanism of action 5. pH regulators of the tumoral microenvironment 6. Proton Pump Inhibitors (PPIs) and other pH buffering agents 7. Selective hCA IX and XII inhibitors 8. Epigenetic modulators 9. Photosensitizing agents 10. Efflux pumps and ABC transporter subfamily inhibitors (e.g., cyclosporin A, verapamil) 11. Metalloproteinase inhibitors (e.g., ADAM17) 12. Kinesin inhibitors 13. Drug repurposing 14. Innovative and putative targets for chemosensitizers 15. Patent survey on chemosensitizers
PART III Chemosensitizing agents from natural sources 16. Natural compounds as chemosensitizers: a lesson from plants 17. Natural compounds: from food to clinic
PART IV Chemosensitizing agents: computational tools and technological approaches 18. Virtual screening and chemoinformatics of new library of chemosensitizers 19. Nanostructures overcoming cancer resistance
Claudiu T. Supuran received his BSc in chemistry from the Polytechnic University of Bucharest, Romania (1987) and PhD in chemistry at the same university in 1991. In 1990 he became assistant and then associate professor of chemistry at the University of Bucharest. He was a visiting scholar at University of Florida, Gainesville, USA, at Grifitth University, Brisbane, Australia and visiting professor at University of La Plata, Argentina. In 1995 he moved at the University of Florence, Italy, where he is currently assistant professor of pharmaceutical chemistry. His main research interests include medicinal chemistry, design of enzyme inhibitors and activators, heterocyclic chemistry, chemistry of sulfonamides, sulfamates and sulfamides, biologically active organo-element derivatives, QSAR studies, X-ray crystallography of metallo-enzymes, metal complexes with biologically active ligands (metal-based drugs), carbonic anhydrases, cyclooxygenases, serine proteases, matrix metalloproteinases, bacterial proteases, and amino acid derivatives among others. He has published more than 700 papers in these fields.
Dr. Carradori is a very prolific researcher with papers dealing with both synthetic and natural products characterized by promising biological activities. Regarding this topic, he has been involved in the study of HAT inhibitors, hCA IX and XII inhibitors, kinesin Eg5 inhibitors and natural compounds active in the field of oncology. Recently, he has been focusing on "drug repurposing disclosing a patent on new roles played by antiparasitic benzimidazoles as anti-cancer agents. He also was Co-Guest Editor of several special issues, co-author of chapters for two books (one edited by Elsevier) and acts as Editorial Board member of several peer-reviewed journals.