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Kinetics and Dynamics
"Kinetics and Dynamics" on molecular modeling of dynamic processes opens with an introductory overview before discussing approaches to reactivity of small systems in the gas phase. Then it examines studies of systems of increasing complexity up to the dynamics of DNA. This title has interdisciplinary character presenting wherever possible an interplay between the theory and the experiment. It provides basic information as well as the details of theory and examples of its application to experimentalists and theoreticians interested in modeling of dynamic processes in chemical and biochemical systems. All contributing authors are renowned experts in their fields and topics covered in this volume represent the forefront of today’s science.
Cancer
This volume reviews advances in cancer chemotherapy research over the last 10 years. Chapters written by leading experts in their field reflect a range of current medicinal chemistry approaches to small molecule drugs. Each chapter covers the drug target and biological rationale, chemotypes, clinical status and future prospects in this rapidly developing area of drug research.
RAS Drug Discovery
KRAS Drug Discovery: Past, Present and Future is a comprehensive overview of the state-of-the-art medicinal chemistry approaches towards targeting the formerly undruggable oncogene, KRAS. It includes Seminal medicinal chemistry case histories of KRASG12C inhibitors such as Sotorosib, the first approved KRASG12C inhibitor for NSCLC, alongside the latest advances towards identification of in vivo tools and development candidates targeting KRAS G12D, KRAS G13C and other mutations. The book also provides the reader with a comprehensive overview of the in vitro assay systems, in vivo pharmacology xenograft models and chemical biology tools available to characterize small molecule inhibitors of KRAS. - Highlights key structure-based drug design (SBDD) innovations to generate potency and selectivity vs. KRAS - Analyzes medicinal chemistry case histories for seminal contributions to the KRAS field - Provides an overview of in vitro and in vivo methods for drugging KRAS
Advances in Medicinal Chemistry
Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment ...
Protein Lipidation
This is the first compilation of protein lipidation enzymes. This volume summarizes recent dramatic developments regarding enzymes responsible for protein lipidation, a process critical for a number of physiological functions, including cell proliferation and morphology. Inhibitors of protein lipidation have recently been shown to be useful as anticancer drugs. Enzymatic mechanisms, mutational analysis, and structural studies are presented. - The enzymatic mechanisms of protein lipidation - Three-dimensional structures of protein farnesytransferase, protein geranylgeranytransferase II, and n-myristoryltransferase
Bioorganic Chemistry of Biological Signal Transduction
The transduction of signals from the extracellular space across the plasma membrane into the interior of cells and ultimately to the nucleus, where in - sponse to such external signals the transcription of the genetic code is inf- enced,belongs to the most fundamental and important events in the regulation of the life cycle of cells. During recent years several signal transduction cascades have been elucidated which regulate,for instance,the growth and the prolife- tion of organisms as diverse as mammals, flies, worms and yeast. The general picture which emerged from these investigations is that nature employs a c- bination of non-covalent ligand/protein and protein/protein interactions toge...
Biochemistry
Biochemistry: The Chemical Reactions of Living Cells is a well-integrated, up-to-date reference for basic chemistry and underlying biological phenomena. Biochemistry is a comprehensive account of the chemical basis of life, describing the amazingly complex structures of the compounds that make up cells, the forces that hold them together, and the chemical reactions that allow for recognition, signaling, and movement. This book contains information on the human body, its genome, and the action of muscles, eyes, and the brain.* Thousands of literature references provide introduction to current research as well as historical background* Contains twice the number of chapters of the first edition* Each chapter contains boxes of information on topics of general interest
Farnesyltransferase Inhibitors in Cancer Therapy
With the explosion of research on genes capable of causing cancer, it has become clear that mutations in the GTPase, Ras, a major regulator of cell division, are found in about 30% of all human cancers, and that farnesylation, a lipid posttranslational modification of Ras, is required for its cancer-causing activity. In Farnesyltransferase Inhibitors in Cancer Therapy, cutting-edge researchers describe their efforts to design, synthesize, and evaluate the biological activities of farnesyltransferase inhibitors (FTIs) and geranylgeranyltransferase inhibitors (GGTIs) that can be used as anticancer drugs and in cardiovascular and parasitic therapy. The authors survey in detail such inhibitors a...
Frontiers in Medicinal Chemistry , Volume (1)
""Frontiers in Medicinal Chemistry" is an Ebook series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. "Frontiers in Medicinal Chemistry" covers all the areas of medicinal chemistry, incl"
Frontiers in Medicinal Chemistry
"Frontiers in Medicinal Chemistry" is an Ebook series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. "Frontiers in Medicinal Chemistry" covers all the areas of medicinal chemistry, including developments in rational drug design, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, chemoinformatics, and structure-activity relationships. Medicinal chemistry as.
