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Analytical chemistry --- Organic chemistry --- General biochemistry --- Oncology. Neoplasms --- Clinical chemistry --- klinische chemie --- medische chemie --- organische chemie --- analytische chemie --- biochemie --- oncologie
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This volume looks at the latest methods used to study and modulate the biological function and mechanisms of SH2 domains. The chapters in this book are organized into five parts. Part One presents methodology aimed at determining the structures and dynamics of SH2 domains and their complexes with phosphopeptides. Part Two discusses techniques to understand and predict interactions of SH2 domains by measuring or calculating their affinity to phosphopeptides. Part Three focuses on inhibitors of SH2 domains that lead the way for chemical tool development and drug discovery. Part Four describes how to evolve and engineer SH2 domains with specific binding properties, and Part Five explores how to measure the regulation of protein tyrosine phosphatase activity through allosteric binding of peptides to SH2 domains and condensation. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and comprehensive, SH2 Domains: Functional Modules and Evolving Tools in Biology is a valuable resource for researchers, working in the biophysical and biochemical field, who want to learn more about this exciting and versatile class of regulatory and signaling domains. .
Cytology. --- Biomolecules. --- Physical biochemistry. --- Macromolecules. --- Proteins. --- Cell Biology. --- Structural Biology.
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reviews. The SAR data are discussed in light of the structural information available for each agent. The second chapter focuses on the total synthesis of the marine sponge-derived polyketide discodermolide. A comprehensive survey of the synthetic chemistry efforts of several groups over a 14-year period is provided together with a comparison of the different approaches. The third chapter describes a comprehensive study of the mechanisms of activity of microtubules stabilizing drugs. Thermodynamic, kinetic, structural and functional data on microtubules stabilizing drugs are discussed in an interdisciplinary manner to generate a “time-resolved” picture of the interaction of the drugs with different tubulin forms. The fourth and fifth chapters review the efforts and achievements made in the characterization of the structure of the complexes of tubulin with microtubules stabilizing agents by NMR (Chapter 4) and EM (Chapter 5). Especially evident is the discrepancy of the results obtained for epothilones, where the two techniques deliver radically different structures of the bound drug. Both NMR and EM models are, however, able to explain a consistent set of SAR data. The authors of the two chapters discuss critically the advantages and limitations of each methodology.
Tubulins --- Stabilizing agents --- Microtubules --- Chemistry --- Tubulin --- Nerve Tissue Proteins --- Microtubule Proteins --- Natural Science Disciplines --- Cytoskeleton --- Proteins --- Cytoplasmic Structures --- Disciplines and Occupations --- Cytoskeletal Proteins --- Biopolymers --- Amino Acids, Peptides, and Proteins --- Cytoplasm --- Polymers --- Macromolecular Substances --- Chemicals and Drugs --- Intracellular Space --- Cellular Structures --- Cells --- Anatomy --- Animal Biochemistry --- Pharmacy, Therapeutics, & Pharmacology --- Chemical Engineering --- Chemical & Materials Engineering --- Health & Biological Sciences --- Human Anatomy & Physiology --- Engineering & Applied Sciences --- Microtubules. --- Stabilizing agents. --- Tubulins. --- Agents, Stabilizing --- Stabilizers (Chemistry) --- Cytotubules --- Microtubule proteins --- Chemistry. --- Cancer research. --- Analytical chemistry. --- Organic chemistry. --- Medicinal chemistry. --- Biochemistry. --- Medicinal Chemistry. --- Biochemistry, general. --- Cancer Research. --- Organic Chemistry. --- Analytical Chemistry. --- Chemicals --- Cell organelles --- Oncology. --- Chemistry, Organic. --- Analytical biochemistry. --- Analytic biochemistry --- Biochemistry --- Chemistry, Analytic --- Organic chemistry --- Tumors --- Biological chemistry --- Chemical composition of organisms --- Organisms --- Physiological chemistry --- Biology --- Medical sciences --- Composition --- Bioanalytic chemistry --- Bioanalytical chemistry --- Analytical chemistry --- Analysis, Chemical --- Analytic chemistry --- Chemical analysis --- Cancer research --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Drugs --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry
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reviews. The SAR data are discussed in light of the structural information available for each agent. The second chapter focuses on the total synthesis of the marine sponge-derived polyketide discodermolide. A comprehensive survey of the synthetic chemistry efforts of several groups over a 14-year period is provided together with a compa- son of the different approaches. The third chapter describes a comprehensive study of the mechanisms of activity of microtubules stabilizing drugs. Thermodynamic, kinetic, structural and fu- tional data on microtubules stabilizing drugs are discussed in an interdisciplinary manner to generate a time-resolved picture of the interaction of the drugs with different tubulin forms. The fourth and fifth chapters review the efforts and achievements made in the characterization of the structure of the complexes of tubulin with microtubules stabilizing agents by NMR (Chapter 4) and EM (Chapter 5). Especially evident is the discrepancy of the results obtained for epothilones, where the two techniques deliver radically different structures of the bound drug. Both NMR and EM models are, however, able to explain a consistent set of SAR data. The authors of the two chapters discuss critically the advantages and limitations of each methodology.
Tubulins --- Stabilizing agents --- Microtubules
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