Claudiu T. Supuran – författare

Carbonic Anhydrases provides an interdisciplinary review of the burgeoning carbonic anhydrase (CA) research area, spanning from CAs classification (biochemical and structural features) to drug design and pharmacology of CA inhibitors and activators, finally touching on the biotechnological applications of these metalloenzymes. The book adopts a clear step-by-step approach and introduction to this intricate and highly interdisciplinary field. A diverse range of chapters from international experts speak to CA classification and distribution, the mechanisms of action and drug design of inhibitors and activators, the druggability of the various isoforms in the treatment of a multitude of diseases, and threats to human health.

Carbonic Anhydrases provides biology, biochemistry, and medicinal chemistry students and researchers a thorough discussion and update on the evergreen and expanding research area of CAs.

Offers a full overview of CAs' biochemical and structural features, as well as drug design and pharmacology of inhibitors and activators Provides a thorough update on the newly identified isoforms, modulating chemotypes, and innovative biomedical applications Describes the current biotechnological applications of CAs, including processes for CO2 capture Features chapter contributions from international leaders in CA biology, medicinal chemistry, and pharmacology

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

Metalloenzymes: From Bench to Bedside offers a thorough overview of metalloenzymes, spanning biochemical and structural features, pharmacology, and biotechnological applications. After a brief overview, international experts in the field discuss a wide range of magnesium, calcium, zinc, manganese, nickel, iron, copper, cadmium, molybdenum, and tungsten enzymes, along with catalytic roles within their active sites. With a uniform approach throughout, each chapter includes the structure and function of the enzyme, physiologic and pathologic roles, inhibitors and activators of the enzyme (and their design), and clinical agents or compounds applied in medicine and drug discovery. This book enables scientists across academia and industry to adopt ongoing metalloenzyme research, and continuous discovery of novel metalloenzymes, in new life science studies and clinical applications.

Examines a range of metalloenzymes, from biochemistry to pharmacology and drug design Each chapter examines enzyme structure and function, physiologic and pathologic roles, inhibitors and activators, and clinical application Features chapter contributions from international experts in the field

Vertebrate Carbonic Anhydrases, Volume 59 in The Enzymes series, explores recent advances in the study of carbonic anhydrases (CAs) in vertebrate systems. This volume presents a comprehensive collection of chapters examining the diversity, structure, function, and physiological roles of vertebrate CA isoforms across multiple tissues and cellular compartments. Chapters include discussions on the phylogenetic relationships of vertebrate carbonic anhydrases and detailed examinations of several important isoforms, including carbonic anhydrases I, II, and III, as well as membrane-associated enzymes such as CA IV and XV. Additional contributions explore mitochondrial carbonic anhydrases (CA VA and VB), secreted isoforms such as CA VI, and more.The volume also examines acatalytic carbonic anhydrases and tumor-associated isoforms, providing insights into their structural characteristics and biological significance. A concluding chapter addresses current challenges and opportunities in the development of selective inhibitors and activators targeting vertebrate carbonic anhydrase isoforms, highlighting their potential therapeutic applications.

Provides comprehensive reviews on vertebrate carbonic anhydrase isoforms and their biological rolesIncludes contributions from leading experts in enzymology, biochemistry, and molecular biologyCovers structural, functional, and evolutionary aspects of multiple carbonic anhydrase familiesExplores mitochondrial, cytosolic, membrane-associated, and secreted carbonic anhydrase isoformsDiscusses emerging opportunities for developing selective carbonic anhydrase inhibitors and activators for therapeutic applications

Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context.With contributions from the leaders of today's research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

This book reviews new promising drug targets for Neglected Tropical Diseases (NTDs), with a special focus on antiprotozoal drugs against trpyanosomatids Trypanosoma cruzi and Leishmania spp.

This book reviews new promising drug targets for Neglected Tropical Diseases (NTDs), with a special focus on antiprotozoal drugs against trpyanosomatids Trypanosoma cruzi and Leishmania spp. The book offers a comprehensive overview of the most recent studied targets, and it outlines classical and new treatments and delivery strategies. Expert contributors describe new methods of analysis and bio-prospecting for new compounds, and provide a critical perspective of the translational process used in the research and development of new drug candidates.The book will appeal not only to researchers, students and professionals interested in drug development to protozoan diseases, but also to medicinal chemists in general.

This book overviews purinergic receptors that are playing key roles in human and pathophysiological processes. The book elaborates on how selective P1 and P2 modulators have been developed as therapeutics for a variety of diseases. It also provides an overview of current perspectives in the design of purinergic receptor modulators and future challenges such as the availability of selective ligands for all receptor subtypes.Divided into 12 chapters, this comprehensive volume also offers a multidisciplinary perspective on the historical evolution, starting with a chapter devoted to the roots and early discoveries of adenosine and its receptors, followed by a twenty-year retrospective on the synthesis, properties, and functional potential of adenosine receptor ligands, probes, and functional conjugates. In the next chapters, experts in the field delve into topics such as the therapeutic potential of adenosine receptor ligands in wound healing and fibrosis, the therapeutic benefits of A2A receptor antagonists, the A2B adenosine receptor as a target for brain ischemia or demyelination, the development and latest advancements in clinical trials of A3 adenosine receptor ligands. Other chapters describe bifunctional tools to study adenosine receptors, allosteric modulators of adenosine receptors, and new computational approaches to inspect adenosine receptor-ligand recognition processes. Furthermore, the book discusses the role of P2X4 receptors in immunity and inflammation. The final chapters illustrate CD73 inhibitors as antitumor agents, and bacterial ectonucleotidases as underexplored antibacterial drug targets. This book is a valuable resource for scholars working in the field of medicinal chemistry, as well as researchers in the industry, providing readers with a comprehensive understanding of adenosine receptor biology and its therapeutic potential.

This book overviews purinergic receptors that are playing key roles in human and pathophysiological processes. The book elaborates on how selective P1 and P2 modulators have been developed as therapeutics for a variety of diseases. It also provides an overview of current perspectives in the design of purinergic receptor modulators and future challenges such as the availability of selective ligands for all receptor subtypes.Divided into 12 chapters, this comprehensive volume also offers a multidisciplinary perspective on the historical evolution, starting with a chapter devoted to the roots and early discoveries of adenosine and its receptors, followed by a twenty-year retrospective on the synthesis, properties, and functional potential of adenosine receptor ligands, probes, and functional conjugates. In the next chapters, experts in the field delve into topics such as the therapeutic potential of adenosine receptor ligands in wound healing and fibrosis, the therapeutic benefits of A2A receptor antagonists, the A2B adenosine receptor as a target for brain ischemia or demyelination, the development and latest advancements in clinical trials of A3 adenosine receptor ligands. Other chapters describe bifunctional tools to study adenosine receptors, allosteric modulators of adenosine receptors, and new computational approaches to inspect adenosine receptor-ligand recognition processes. Furthermore, the book discusses the role of P2X4 receptors in immunity and inflammation. The final chapters illustrate CD73 inhibitors as antitumor agents, and bacterial ectonucleotidases as underexplored antibacterial drug targets. This book is a valuable resource for scholars working in the field of medicinal chemistry, as well as researchers in the industry, providing readers with a comprehensive understanding of adenosine receptor biology and its therapeutic potential.

This title is an exploration of the enzyme carbonic anhydrase (CA) and its inhibitors (CAIs), focusing on its biochemical properties, mechanisms, and wide-ranging applications.The book begins with an introduction to carbonic anhydrase, providing basic knowledge of its structure, function, and importance in various physiological processes. This sets the stage for understanding the enzyme’s role in catalysis and the principles underlying its inhibition. Subsequent chapters focus on the intricate process of drug design, highlighting the strategies used to develop effective CAIs, discussing the principles of drug design, computational approaches, and structure-based drug design, and presenting the technological advances that have revolutionised the field. These chapters provide readers with insight into the scientific methodologies and innovative techniques used to create potent inhibitors, emphasising the importance of precision and specificity in drug development.The therapeutic applications of CAIs are discussed in the following section, which includes their use in the treatment of glaucoma and other eye conditions, their potential in cancer therapy, and their applications in the treatment of neurological disorders, illustrating the versatility and efficacy of these inhibitors in various medical contexts. Beyond medical applications, the book also addresses the industrial and environmental uses of CAIs. The last part of the book explores how CAIs can be used in processes such as carbon capture and sequestration, highlighting their importance in addressing global environmental challenges.Finally, the book focuses on future directions for biotechnological and pharmacological applications, providing an overview of ongoing research and emerging trends. This book is an essential resource for researchers, clinicians, and students, offering an in-depth understanding of carbonic anhydrase inhibitors and their multiple applications.

Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.