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This volume contains a collection of innovative techniques for studying targeted protein degradation. Chapters guide readers through heterobifunctional proteolysis-targeting chimeras (PROTACs) approaches, E3 ligase, E3 ligase-induced ubiquitylation, proteomic approaches, novel degrader molecules, molecular glue, and stabilize binding interaction between a target and E3 ubiquitin ligase. Written in the format of the highly successful Methods in Molecular Biology series, each chapter includes an introduction to the topic, lists necessary materials and reagents, includes tips on troubleshooting and known pitfalls, and step-by-step, readily reproducible protocols. Authoritative and cutting-edge, Targeted Protein Degradation: Methods and Protocols aims to ensure successful results in this emerging field of drug discovery. .
Proteins. --- Pharmaceutical chemistry. --- Pharmaceutics. --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Drugs --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry --- Chemistry --- Proteids --- Biomolecules --- Polypeptides --- Proteomics
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This second edition further develops the principles of applying kinetic principles to drug metabolizing enzymes and transporters. Chapters are divided into six sections detailing fundamental principles of enzyme kinetics, enzyme and transporter structures, highlighting specific oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for drug metabolizing enzymes and transporters, understanding of variability both experimental and interindividual (pharmacogenomic), and expanded case studies that provide real life examples of applying these principles. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, in some cases step-by-step instructions with readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning. Authoritative and fully updated, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications, Second Edition serves as a practical teaching tool for novice and advanced scientists interested in the fundamental concepts.
Pharmaceutical chemistry. --- Enzymology. --- Pharmaceutics. --- Biochemistry --- Enzymes --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Drugs --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry --- Chemistry
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Bioorganic chemistry. --- Proteins. --- Pharmaceutical chemistry. --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Drugs --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry --- Chemistry --- Proteids --- Biomolecules --- Polypeptides --- Proteomics --- Bio-organic chemistry --- Biological organic chemistry --- Biochemistry --- Chemistry, Organic
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This collection explores detailed experimental protocols necessary for setting up a variety of in vitro cytochrome P450 (CYP) assays that are vital in selecting drug candidates in a drug discovery pipeline. Major factors affecting drug metabolism include CYP expression levels, kinetic parameters for individual CYP enzymes, CYP inhibition and induction, time-dependent inhibition (TDI), CYP stability, non-CYP stability, UDP-glucuronosyltransferases (UGT) stability, excretion mechanisms, and drug-drug interactions (DDI), all addressed in this volume. Written for the Methods in Pharmacology and Toxicology series, chapters include helpful background information on the in vitro assay, a list of all the materials, reagents, and equipment necessary to carry out the assay, a step-by-step protocol, notes containing common and unexpected experimental problems in the assay, as well as references containing important supplementary reading. Authoritative and practical, Cytochrome P450: In Vitro Methods and Protocols serves as a key guide for researchers in the area of discovery and development of new medicines. .
Pharmacology. --- Enzymology. --- Pharmaceutical chemistry. --- Pharmaceutics. --- Biochemistry --- Enzymes --- Drug effects --- Medical pharmacology --- Medical sciences --- Chemicals --- Chemotherapy --- Drugs --- Pharmacy --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry --- Chemistry --- Physiological effect
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This detailed book collects modern and established computer-based methods aimed at addressing the drug discovery challenge from disparate perspectives by exploiting information on ligand-protein recognition. Beginning with methods that allow for the exploration of specific areas of chemical space and the designing of virtual libraries, the volume continues with sections on methods based on docking, quantitative models, and molecular dynamics simulations, which are employed for ligand discovery or development, as well as methods exploiting an ensemble of protein structures for the identification of potential protein targets. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and cutting-edge, Protein-Ligand Interactions and Drug Design provides detailed practical procedures of solid computer-aided drug design methodologies employed to rationalize and optimize protein-ligand interactions, for experienced researchers and novices alike.
Pharmaceutical chemistry. --- Chemistry—Data processing. --- Chemistry. --- Chemistry, Physical and theoretical. --- Pharmaceutics. --- Computational Chemistry. --- Theoretical Chemistry. --- Chemistry, Theoretical --- Physical chemistry --- Theoretical chemistry --- Chemistry --- Physical sciences --- Chemistry, Medical and pharmaceutical --- Chemistry, Pharmaceutical --- Drug chemistry --- Drugs --- Medical chemistry --- Medicinal chemistry --- Pharmacochemistry
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