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Transporters in Drug Development

Transporters in Drug Development
  • Author : Yuichi Sugiyama,Bente Steffansen
  • Publisher :Unknown
  • Release Date :2013-09-16
  • Total pages :317
  • ISBN : 9781461482291
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Summary : Transporters in Drug Development examines how membrane transporters can be dealt with in academic–industrial drug discovery and pharmaceutical development as well as from a regulatory perspective. The book describes methods and examples of in vitro characterization of single transporters in the intestines, liver and kidneys as well as characterization of substrate overlap between various transporters. Furthermore, probes and biomarkers are suggested for studies of the transporters’ impact on the pharmacokinetics of drug substrates/candidates interacting on transporters. The challenges of translating in vitro observed interaction of transporters into in vivo relevance are explored, and the book highlights perspectives of applying targeted proteomics and mechanistic modeling in this process.

Transporters in Drug Discovery and Development

Transporters in Drug Discovery and Development
  • Author : Yurong Lai
  • Publisher :Unknown
  • Release Date :2014-08-22
  • Total pages :780
  • ISBN : 9781908818287
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Summary : Written by a leading researcher in the field, Transporters in Drug Discovery and Development provides a comprehensive and practical guide to drug transporter families that are the most important for drug discovery and development. It covers: an overview of transporter families and organ distribution; clinical relevant drug-drug interaction; clinical relevant polymorphism; drug transporter related pharmacokinetic, pharmacodynamics and toxicity; in vitro/in vivo probes of drug transport studies; the practical methodologies of industrial transporter screening and translational aspect in drug discovery and developments. A comprehensive overview of drug transporter families and their clinical relevance in drug discovery and development Balanced coverage of molecular biology aspects and functional outcomes State of art knowledge related to transporter-mediated DDI and the clinical relevance in pharmacokinetics, dynamics, and toxicity

Transporters in Drug Discovery and Development

Transporters in Drug Discovery and Development
  • Author : Yurong Lai
  • Publisher :Unknown
  • Release Date :2014-08-22
  • Total pages :780
  • ISBN : 9781908818287
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Summary : Written by a leading researcher in the field, Transporters in Drug Discovery and Development provides a comprehensive and practical guide to drug transporter families that are the most important for drug discovery and development. It covers: an overview of transporter families and organ distribution; clinical relevant drug-drug interaction; clinical relevant polymorphism; drug transporter related pharmacokinetic, pharmacodynamics and toxicity; in vitro/in vivo probes of drug transport studies; the practical methodologies of industrial transporter screening and translational aspect in drug discovery and developments. A comprehensive overview of drug transporter families and their clinical relevance in drug discovery and development Balanced coverage of molecular biology aspects and functional outcomes State of art knowledge related to transporter-mediated DDI and the clinical relevance in pharmacokinetics, dynamics, and toxicity

Drug Transporters

Drug Transporters
  • Author : Guofeng You,Marilyn E. Morris
  • Publisher :Unknown
  • Release Date :2014-07-07
  • Total pages :528
  • ISBN : 9781118704981
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Summary : This new edition overviews drug transporters and presents the principles of drug transport and associated techniques, featuring new chapters on multidrug and toxin extrusion proteins, placental transport, in silico approaches in drug discovery, and regulatory guidance for drug transport studies in drug development. • Describes drug transporter families, mechanisms, and clinical implications along with experimental methods for studying and characterizing drug transporters • Includes new chapters on multidrug and toxin extrusion proteins, placental transport and in silico approaches in drug discovery • Has a new chapter covering regulatory guidance for the evaluation of drug transport in drug development with global criteria used for drug transporters in clinical trials • Arranges material to go from fundamental mechanisms to clinical outcomes, making the book useful for novice and expert readers

Membrane Transporters in Drug Discovery and Development

Membrane Transporters in Drug Discovery and Development
  • Author : Qing Yan
  • Publisher :Unknown
  • Release Date :2016-08-23
  • Total pages :365
  • ISBN : 1493957333
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Summary : Studies of membrane transporters have had a great impact on our understanding of human diseases and the design of effective drugs. In Membrane Transporters in Drug Discovery and Development: Methods and Protocols, expert researchers provide practical methodologies of the ongoing research on membrane transporters, considering applications of transporter technologies in drug discovery and development. Chapters include new and useful fields and methodologies, including pharmacogenomics, nutrigenomics, systems biology, bioinformatics, nuclear magnetic resonance (NMR), imaging, and quantitative real-time-PCR. Transporter studies in drug discovery and development for various diseases are discussed, including neuropsychiatric disorders, cardiovascular diseases, ophthalmic diseases, cancer, and diabetes. Composed in the highly successful Methods in Molecular BiologyTM series format, each chapter contains a brief introduction, step-by-step methods, a list of necessary materials, and a Notes section which shares tips on troubleshooting and avoiding known pitfalls. Wide-ranging and current, Membrane Transporters in Drug Discovery and Development: Methods and Protocols delivers a collection of practical protocols that can be used immediately in the lab, along with critical surveys of key topics by leading researchers in the field.

Drug Transporters

Drug Transporters
  • Author : Martin F. Fromm,Richard B. Kim
  • Publisher :Unknown
  • Release Date :2010-11-19
  • Total pages :454
  • ISBN : 3642145418
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Summary : It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.

Drug Transporters

Drug Transporters
  • Author : Glynis Nicholls,Kuresh Youdim
  • Publisher :Unknown
  • Release Date :2016-08-17
  • Total pages :239
  • ISBN : 9781782628705
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Summary : Understanding and quantifying the effects of membrane transporters within the human body is essential for modulating drug safety and drug efficacy. The first volume comprehensively reviewed current knowledge and techniques in the transporter sciences and their relations to drug metabolism and pharmacokinetics. In this second volume on Drug Transporters, emphasis is placed on emerging sciences and technologies, highlighting potential areas for future advances within the drug transporter field. The topics covered in both volumes ensure that all relevant aspects of transporters are described across the drug development process, from in silico models and preclinical tools through to the potential impact of transporters in the clinic. Contributions are included from expert leaders in the field, at-the-bench industrial scientists, renowned academics and international regulators. Case studies and emerging developments are highlighted, together with the merits and limitations of the available methods and tools, and extensive references to reviews on specific in-depth topics are also included for those wishing to pursue their knowledge further. As such, this text serves as an essential handbook of information for postgraduate students, academics, industrial scientists and regulators who wish to understand the role of transporters in absorption, distribution, metabolism, and excretion processes. In addition, it is also a useful reference tool on the models and calculations necessary to predict their effect on human pharmacokinetics and pharmacodynamics.

Membrane Transporters in Drug Discovery and Development

Membrane Transporters in Drug Discovery and Development
  • Author : Qing Yan
  • Publisher :Unknown
  • Release Date :2010-04-26
  • Total pages :365
  • ISBN : STANFORD:36105211741215
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Summary : This text provides practical methodologies of the ongoing research on membrane transporters, considering applications of transporter technologies in drug discovery and development.

Basic Principles of Drug Discovery and Development

Basic Principles of Drug Discovery and Development
  • Author : Benjamin Blass
  • Publisher :Unknown
  • Release Date :2015-04-24
  • Total pages :580
  • ISBN : 9780124115255
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Summary : Basic Principles of Drug Discovery and Development presents the multifaceted process of identifying a new drug in the modern era, providing comprehensive explanations of enabling technologies such as high throughput screening, structure based drug design, molecular modeling, pharmaceutical profiling, and translational medicine, all areas that have become critical steps in the successful development of marketable therapeutics. The text introduces the fundamental principles of drug discovery and development, also discussing important drug targets by class, in vitro screening methods, medicinal chemistry strategies in drug design, principles in pharmacokinetics and pharmacodynamics, animal models of disease states, clinical trial basics, and selected business aspects of the drug discovery process. It is designed to enable new scientists to rapidly understand the key fundamentals of drug discovery, including pharmacokinetics, toxicology, and intellectual property." Provides a clear explanation of how the pharmaceutical industry works Explains the complete drug discovery process, from obtaining a lead, to testing the bioactivity, to producing the drug, and protecting the intellectual propertyIdeal for anyone interested in learning about the drug discovery process and those contemplating careers in the industry Explains the transition process from academia or other industries

ADME-Enabling Technologies in Drug Design and Development

ADME-Enabling Technologies in Drug Design and Development
  • Author : Donglu Zhang,Sekhar Surapaneni
  • Publisher :Unknown
  • Release Date :2012-04-13
  • Total pages :800
  • ISBN : 9781118180761
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Summary : A comprehensive guide to cutting-edge tools in ADME research The last decade has seen tremendous progress in the developmentof analytical techniques such as mass spectrometry and molecularbiology tools, resulting in important advances in drug discovery,particularly in the area of absorption, distribution, metabolism,and excretion (ADME). ADME-Enabling Technologies in Drug Design and Developmentfocuses on the current state of the art in the field, presenting acomprehensive review of the latest tools for generating ADME datain drug discovery. It examines the broadest possible range ofavailable technologies, giving readers the information they need tochoose the right tool for a given application, a key requisite forobtaining favorable results in a timely fashion for regulatoryfilings. With over thirty contributed chapters by an internationalteam of experts, the book provides: A thorough examination of current tools, covering bothelectronic/mechanical technologies and biologically based ones Coverage of applications for each technology, including keyparameters, optimal conditions for intended results, protocols, andcase studies Detailed discussion of emerging tools and techniques, from stemcells and genetically modified animal models to imagingtechnologies Numerous figures and diagrams throughout the text Scientists and researchers in drug metabolism, pharmacology,medicinal chemistry, pharmaceutics, toxicology, and bioanalyticalscience will find ADME-Enabling Technologies in Drug Design andDevelopment an invaluable guide to the entire drug developmentprocess, from discovery to regulatory issues.

Drug Discovery and Development - E-Book

Drug Discovery and Development - E-Book
  • Author : Raymond G Hill
  • Publisher :Unknown
  • Release Date :2012-07-20
  • Total pages :368
  • ISBN : 9780702053160
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Summary : The modern pharmacopeia has enormous power to alleviate disease, and owes its existence almost entirely to the work of the pharmaceutical industry. This book provides an introduction to the way the industry goes about the discovery and development of new drugs. The first part gives a brief historical account from its origins in the mediaeval apothecaries’ trade, and discusses the changing understanding of what we mean by disease, and what therapy aims to achieve, as well as summarising case histories of the discovery and development of some important drugs. The second part focuses on the science and technology involved in the discovery process: the stages by which a promising new chemical entity is identified, from the starting point of a medical need and an idea for addressing it. A chapter on biopharmaceuticals, whose discovery and development tend to follow routes somewhat different from synthetic compounds, is included here, as well as accounts of patent issues that arise in the discovery phase, and a chapter on research management in this environment. The third section of the book deals with drug development: the work that has to be undertaken to turn the drug candidate that emerges from the discovery process into a product on the market. The definitive introduction to how a pharmaceutical company goes about its business of discovering and developing drugs. The second edition has a new editor: Professor Raymond Hill ● non-executive director of Addex Pharmaceuticals, Covagen and of Orexo AB ● Visiting Industrial Professor of Pharmacology in the University of Bristol ● Visiting Professor in the School of Medical and Health Sciences at the University of Surrey ● Visiting Professor in Physiology and Pharmacology at the University of Strathclyde ● President and Chair of the Council of the British Pharmacological Society ● member of the Nuffield Council on Bioethics and the Advisory Council on Misuse of Drugs. New to this edition: Completely rewritten chapter on The Role of Medicinal Chemistry in the Drug Discovery Process. New topic - DMPK Optimization Strategy in drug discovery. New chapter on Scaffolds: Small globular proteins as antibody substitutes. Totally updated chapters on Intellectual Property and Marketing 50 new illustrations in full colour Features Accessible, general guide to pharmaceutical research and development. Examines the interfaces between cost and social benefit, quality control and mass production, regulatory bodies, patent management, and all interdisciplinary intersections essential to effective drug development. Written by a strong team of scientists with long experience in the pharmaceutical industry. Solid overview of all the steps from lab bench to market in an easy-to-understand way which will be accessible to non-specialists. From customer reviews of the previous edition: ‘... it will have everything you need to know on this module. Deeply referenced and, thus, deeply reliable. Highly Commended in the medicine category of the BMA 2006 medical book competition Winner of the Royal Society of Medicine Library Prize for Medical Book of the Year

Drug Metabolism in Drug Design and Development

Drug Metabolism in Drug Design and Development
  • Author : Donglu Zhang,Mingshe Zhu,William G. Humphreys
  • Publisher :Unknown
  • Release Date :2007-11-16
  • Total pages :448
  • ISBN : 0470191686
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Summary : The essentials of drug metabolism vital to developing new therapeutic entities Information on the metabolism and disposition of candidate drugs is a critical part of all aspects of the drug discovery and development process. Drug metabolism, as practiced in the pharmaceutical industry today, is a complex, multidisciplinary field that requires knowledge of sophisticated analytical technologies and expertise in mechanistic and kinetic enzymology, organic reaction mechanism, pharmacokinetic analysis, animal physiology, basic chemical toxicology, preclinical pharmacology, and molecular biology. With chapters contributed by experts in their specific areas, this reference covers: * Basic concepts of drug metabolism * The role of drug metabolism in the pharmaceutical industry * Analytical techniques in drug metabolism * Common experimental approaches and protocols Drug Metabolism in Drug Design and Development emphasizes practical considerations such as the data needed, the experiments and analytical methods typically employed, and the interpretation and application of data. Chapters highlight facts, common protocols, detailed experimental designs, applications, and limitations of techniques. This is a comprehensive, hands-on reference for drug metabolism researchers as well as other professionals involved in pre-clinical drug discovery and development.

Membrane Transporters and Channels as Targets for Drugs

Membrane Transporters and Channels as Targets for Drugs
  • Author : Graça Soveral,Cesare Indiveri
  • Publisher :Unknown
  • Release Date :2020-01-03
  • Total pages :229
  • ISBN : 9782889633579
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Summary : Transporters and channels are membrane proteins that mediate the traffic of metabolites, water and ions across biological membranes. Membrane transport proteins are crucial to maintain homeostasis and assure cell survival upon intracellular or environmental stress. A failure of any of these transport systems may have dramatic consequences for cell function. There is increasing evidence that membrane transport proteins play important functions in healthy conditions and that their absence or dysfunction may cause diseases. In recent years much attention has been paid to diseases resulting from defective transporters (“carrier diseases”) and ion channels (“channelopathies”). Very interestingly, altered expression of transporters has been described in several human pathologies. On this basis, many transport proteins are well acknowledged targets for drugs. Many others are involved in drug delivery and disposition and/or are considered potential targets. Others are off-targets for drugs and then, are responsible for side effects. Thus, membrane protein drug discovery is now an emerging field where the search for physiological mechanisms of regulation and for chemical compounds as modulators of transport activity, present new opportunities for drug development and for new therapies. This Research Topic addresses the latest research advances in membrane transport proteins, stimulating future research on these important protein families.

Oral Bioavailability Assessment

Oral Bioavailability Assessment
  • Author : Ayman F. El-Kattan
  • Publisher :Unknown
  • Release Date :2017-06-06
  • Total pages :448
  • ISBN : 9781118916698
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Summary : Specifically geared to personnel in the pharmaceutical and biotechnology industries, this book describes the basics and challenges of oral bioavailability – one of the most significant hurdles in drug discovery and development. • Describes approaches to assess pharmacokinetics and how drug efflux and uptake transporters impact oral bioavailability • Helps readers reduce the failure rate of drug candidates when transitioning from the bench to the clinic during development • Explains how preclinical animal models – used in preclinical testing – and in vitro tools translate to humans, which is an underappreciated and complicated area of drug development • Includes chapters about pharmacokinetic modelling, the Biopharmaceutics Drug Disposition Classification System (BDDCS), and the Extended Clearance Classification System (ECCS) • Has tutorials for applying strategies to medicinal chemistry practices of drug discovery/development

Transporters as Drug Targets

Transporters as Drug Targets
  • Author : Gerhard F. Ecker,Rasmus P. Clausen,Gerd Folkers,Harald H. Sitte,Raimund Mannhold,Helmut Buschmann
  • Publisher :Unknown
  • Release Date :2017-04-10
  • Total pages :354
  • ISBN : 9783527333844
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Summary : As opposed to other books on the topic, this volume is unique in also covering emerging transporter targets. Following a general introduction to the importance of targeting transporter proteins with drugs, the book systematically presents individual transporter classes and explains their pharmacology and physiology. The text covers all transporter families with known or suspected importance as drug targets, including neurotransmitter transporters, ABC transporters, glucose transporters and organic ion transporters. The final part discusses recent advances in structural studies of transport proteins, assay methods for transport activity, and the systems biology of transporters and their regulation. With its focus on drug development issues, this authoritative overview is required reading for researchers in industry and academia targeting transport proteins for the treatment of disease.

Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters

Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters
  • Author : Shuguang Ma,Swapan Chowdhury
  • Publisher :Unknown
  • Release Date :2020-07-09
  • Total pages :708
  • ISBN : 9780128200193
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Summary : Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters, Second Edition, is completely updated to provide an overview of the last decade’s numerous advances in analytical technologies for detection and quantification of drugs, metabolites, and biomarkers. This new edition goes beyond LC-MS and features all-new chapters on how to evaluate drug absorption, distribution, metabolism, and excretion, potential for hepatic and renal toxicity, immunogenicity of biotherapeutics and translational tools for predicting human dosage, safety and efficacy of small molecules and biologics. This book will be an important handbook and desk reference for pharmacologists, toxicologists, clinical scientists, and students interested in the fields of pharmacology, biochemistry, and drug metabolism. Four sections in the book with 24 chapters give readers an overview of state-of-the-art techniques for identifying and quantifying drugs, metabolites and biomarkers, including a chapter on new approaches for quantification of enzymes and transporters in different tissues Focuses on the role of drug metabolism enzymes, transporters in disposition and drug-drug interactions, as well as strategies for evaluating drug metabolism and safety using advanced liver and kidney models. Discussions on immunogenicity risks of biologics and their evaluation methods have been included Includes several chapters on advanced translational sciences to predict human dosage, pharmacokinetics and efficacy for small molecules and biotherapeutics All chapters are written by experts with a wide range of practical experience from the industry and academia

Drug-Drug Interactions in Pharmaceutical Development

Drug-Drug Interactions in Pharmaceutical Development
  • Author : Binghe Wang
  • Publisher :Unknown
  • Release Date :2008-03-05
  • Total pages :264
  • ISBN : 0470187913
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Summary : Drug-Drug Interactions in Pharmaceutical Development comprehensively reviews the relevant science, industrial practice, and regulatory agency positions on drug-drug interactions. It focuses on the evaluation of potential drug-drug interactions, allowing researchers to address risk factors before a drug is put to market. The book covers both clinical and nonclinical aspects for understanding drug-drug interactions as well as in vitro and in vivo studies for use in studying interactions at the drug discovery stage.

Pharmaceutical Profiling in Drug Discovery for Lead Selection

Pharmaceutical Profiling in Drug Discovery for Lead Selection
  • Author : Ronald Borchardt,Edward Kerns,Christopher Lipinski,Dhrien Thakker,Binghe Wang
  • Publisher :Unknown
  • Release Date :2005-12-05
  • Total pages :482
  • ISBN : 0971176795
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Summary : This volume focuses on how to increase the efficiency of drug discovery and development. It is written by experienced discovery scientists from diverse disciplines, including chemistry, drug metabolism, and development sciences. The volume details in silico, in vitro, and in vivo tools for prediction, measurement, and application of compound properties to select and improve potential drug candidates.

Drug Discovery and Development, Third Edition

Drug Discovery and Development, Third Edition
  • Author : James J. O'Donnell,John Somberg,Vincent Idemyor,James T. O'Donnell
  • Publisher :Unknown
  • Release Date :2019-11-21
  • Total pages :668
  • ISBN : 9781351625142
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Summary : Drug Discovery and Development, Third Edition presents up-to-date scientific information for maximizing the ability of a multidisciplinary research team to discover and bring new drugs to the marketplace. It explores many scientific advances in new drug discovery and development for areas such as screening technologies, biotechnology approaches, and evaluation of efficacy and safety of drug candidates through preclinical testing. This book also greatly expands the focus on the clinical pharmacology, regulatory, and business aspects of bringing new drugs to the market and offers coverage of essential topics for companies involved in drug development. Historical perspectives and predicted trends are also provided. Features: Highlights emerging scientific fields relevant to drug discovery such as the microbiome, nanotechnology, and cancer immunotherapy; and novel research tools such as CRISPR and DNA-encoded libraries Case study detailing the discovery of the anti-cancer drug, lorlatinib Venture capitalist commentary on trends and best practices in drug discovery and development Comprehensive review of regulations and their impact on drug development, highlighting special populations, orphan drugs, and pharmaceutical compounding Multidiscipline functioning of an Academic Research Enterprise, plus a chapter on Ethical Concerns in Research Contributions by 70+ experts from industry and academia specialists who developed and are practitioners of the science and business

Relevance of Steroid Biosynthesis, Metabolism and Transport in Pathophysiology and Drug Discovery

Relevance of Steroid Biosynthesis, Metabolism and Transport in Pathophysiology and Drug Discovery
  • Author : Tea Lanišnik Rižner,Walter Jäger,Csilla Özvegy-Laczka
  • Publisher :Unknown
  • Release Date :2019-07-10
  • Total pages :229
  • ISBN : 9782889458875
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Summary : Steroid hormones have important roles in human physiology, but they are also implicated in the development of hormone-dependent cancers and various non-maligant diseases. Furthermore, changes in the concentrations of steroid hormones have important effects on the homeostasis of pre- and post-menopausal women, as well as of men in andropause. The associations of steroid hormones with pathophysiological processes and the altered mechanisms of their actions in disease are still not completely understood. It has been known for more than thirty years that in addition to their endocrine activity, steroid hormones act in an intracrine manner. In target organs, active androgens and estrogens can be formed from inactive, or less active, precursor steroid hormones, mainly dehydroepiandrosterone-sulfate (DHEA-S), and estrone-sulfate (E1-S) after their translocation into cells through the transporter proteins of the organic anion-transporting polypeptide (OATP) and organic anion-transporter (OAT) families. The combination of altered uptake of precursors, changed activation and action of estrogens and androgens, in concert with the changes in the metabolism and excretion may thus have major roles in the development of hormone-dependent malignant and non-malignant diseases. To date, the salient roles of the individual players in disease pathophysiology have not been precisely defined. The aim of this Research Topic is thus to highlight the progress made in the field of steroid transport and intracrine actions and metabolism, with special emphasis on the involvement of these processes in the pathophysiology of hormone-dependent disorders and on the identification of novel drug targets.

Mass Spectrometry in Drug Discovery

Mass Spectrometry in Drug Discovery
  • Author : David T. Rossi,Michael Sinz
  • Publisher :Unknown
  • Release Date :2001-11-07
  • Total pages :432
  • ISBN : 1420002473
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Summary : Mass Spectrometry in Drug Discovery summarizes the theory, instrumentation, techniques, and application of mass spectrometry and atmospheric pressure ionization to screening, evaluating, and improving the performance and quality of drug candidates. It provides time- and cost-efficient approaches for the generation and analysis of effective pharmaceuticals, covers advances in combinatorial chemistry, molecular biology, bioanalysis automation, and computing, and demonstrates the use of mass spectrometry in the assessment of disease states, drug targets, and potential drug agents.