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Small Molecule Drug Discovery

Small Molecule Drug Discovery
Methods, Molecules and Applications

by Andrea Trabocchi,Elena Lenci

  • Publisher : Elsevier
  • Release : 2019-11-23
  • Pages : 356
  • ISBN : 0128183500
  • Language : En, Es, Fr & De
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Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development
Theory and Case Studies

by C. Robin Ganellin,Roy Jefferis,Stanley M. Roberts

  • Publisher : Academic Press
  • Release : 2013-05-07
  • Pages : 472
  • ISBN : 0123977703
  • Language : En, Es, Fr & De
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Introduction to Biological and Small Molecule Drug Research and Development provides, for the first time, an introduction to the science behind successful pharmaceutical research and development programs. The book explains basic principles, then compares and contrasts approaches to both biopharmaceuticals (proteins) and small molecule drugs, presenting an overview of the business and management issues of these approaches. The latter part of the book provides carefully selected real-life case studies illustrating how the theory presented in the first part of the book is actually put into practice. Studies include Herceptin/T-DM1, erythropoietin (Epogen/Eprex/NeoRecormon), anti-HIV protease inhibitor Darunavir, and more. Introduction to Biological and Small Molecule Drug Research and Development is intended for late-stage undergraduates or postgraduates studying chemistry (at the biology interface), biochemistry, medicine, pharmacy, medicine, or allied subjects. The book is also useful in a wide variety of science degree courses, in post-graduate taught material (Masters and PhD), and as basic background reading for scientists in the pharmaceutical industry. For the first time, the fundamental scientific principles of biopharmaceuticals and small molecule chemotherapeutics are discussed side-by-side at a basic level Edited by three senior scientists with over 100 years of experience in drug research who have compiled the best scientific comparison of small molecule and biopharmaceuticals approaches to new drugs Illustrated with key examples of important drugs that exemplify the basic principles of pharmaceutical drug research and development

Small Molecule Medicinal Chemistry

Small Molecule Medicinal Chemistry
Strategies and Technologies

by Werngard Czechtizky,Peter Hamley

  • Publisher : John Wiley & Sons
  • Release : 2015-09-21
  • Pages : 528
  • ISBN : 1118771575
  • Language : En, Es, Fr & De
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Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting

Encyclopedia of Cancer

Encyclopedia of Cancer
A Book

by Manfred Schwab

  • Publisher : Springer Science & Business Media
  • Release : 2008-09-23
  • Pages : 3235
  • ISBN : 3540368477
  • Language : En, Es, Fr & De
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This comprehensive encyclopedic reference provides rapid access to focused information on topics of cancer research for clinicians, research scientists and advanced students. Given the overwhelming success of the first edition, which appeared in 2001, and fast development in the different fields of cancer research, it has been decided to publish a second fully revised and expanded edition. With an A-Z format of over 7,000 entries, more than 1,000 contributing authors provide a complete reference to cancer. The merging of different basic and clinical scientific disciplines towards the common goal of fighting cancer makes such a comprehensive reference source all the more timely.

Engineering the Microbial Platform for the Production of Biologics and Small-Molecule Medicines

Engineering the Microbial Platform for the Production of Biologics and Small-Molecule Medicines
A Book

by Dipesh Dhakal,Eung-Soo Kim,Mattheos Koffas

  • Publisher : Frontiers Media SA
  • Release : 2019-12-23
  • Pages : 329
  • ISBN : 2889632539
  • Language : En, Es, Fr & De
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Protein Degradation with New Chemical Modalities

Protein Degradation with New Chemical Modalities
Successful Strategies in Drug Discovery and Chemical Biology

by Hilmar Weinmann,Craig Crews

  • Publisher : Royal Society of Chemistry
  • Release : 2020-10-07
  • Pages : 359
  • ISBN : 1839160772
  • Language : En, Es, Fr & De
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Targeting protein degradation using small molecules is one of the most exciting small-molecule therapeutic strategies in decades and a rapidly growing area of research. In particular, the development of proteolysis targeting chimera (PROTACs) as potential drugs capable of recruiting target proteins to the cellular quality control machinery for elimination has opened new avenues to address traditionally ‘difficult to target’ proteins. This book provides a comprehensive overview from the leading academic and industrial experts on recent developments, scope and limitations in this dynamically growing research area; an ideal reference work for researchers in drug discovery and chemical biology as well as advanced students.

Essential Metals in Medicine: Therapeutic Use and Toxicity of Metal Ions in the Clinic

Essential Metals in Medicine: Therapeutic Use and Toxicity of Metal Ions in the Clinic
A Book

by Peggy L. Carver

  • Publisher : Walter de Gruyter GmbH & Co KG
  • Release : 2019-01-14
  • Pages : 455
  • ISBN : 3110526980
  • Language : En, Es, Fr & De
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Volume 19, entitled Essential Metals in Medicine: Therapeutic Use and Toxicity of Metal Ions in the Clinic of the series Metal Ions in Life Sciences centers on the role of metal ions in clinical medicine. Metal ions are tightly regulated in human health: while essential to life, they can be toxic as well. Following an introductory chapter briefly discussing several important metal-related drugs and diseases and a chapter about drug development, the focus is fi rst on iron: its essentiality for pathogens and humans as well as its toxicity. Chelation therapy is addressed in the context of thalassemia, its relationship to neurodegenerative diseases and also the risks connected with iron administration are pointed out. A subject of intense debate is the essentiality of chromium and vanadium. For example, chromium(III) compounds are taken as a nutritional supplement by athletes and bodybuilders; in contrast, chromate, Cr(VI), is toxic and a carcinogen for humans. The benefi cial and toxic effects of manganese, cobalt, and copper on humans are discussed. The need for antiparasitic agents is emphasized as well as the clinical aspects of metal-containing antidotes for cyanide poisoning. In addition to the essential and possibly essential ones, also other metal ions play important roles in human health, causing harm (like the metalloid arsenic, lead or cadmium) or being used in diagnosis or treatment of human diseases, like gadolinium, gallium, lithium, gold, silver or platinum. The impact of this vibrant research area on metals in the clinic is provided in 14 stimulating chapters, written by internationally recognized experts from the Americas, Europe and China, and is manifested by approximately 2000 references, and about 90 illustrations and tables. Essential Metals in Medicine: Therapeutic Use and Toxicity of Metal Ions in the Clinic is an essential resource for scientists working in the wide range from pharmacology, enzymology, material sciences, analytical, organic, and inorganic biochemistry all the way through to medicine ... not forgetting that it also provides excellent information for teaching.

Successful Drug Discovery

Successful Drug Discovery
A Book

by János Fischer,Christian Klein,Wayne E. Childers

  • Publisher : John Wiley & Sons
  • Release : 2019-07-20
  • Pages : 272
  • ISBN : 352781471X
  • Language : En, Es, Fr & De
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Provides unique insider insight into the current drug development process, and what it takes to achieve success In this fourth volume in the series, inventors and primary developers of drugs that made it to the market continue telling the story of the drugs? discovery and development, and discuss the sometimes twisted route from the first drug candidate molecule to the final marketed one. Beginning with a general section addressing overarching topics for drug discovery, the book offers seven chapters that feature selected case studies describing recently introduced drugs or drug classes. These include small molecule drugs as well as biopharmaceuticals and range across different therapeutic fields. Together, they provide a representative cross-section of the present-day drug development effort. Successful Drug Discovery: Volume 4 covers trends in peptide-based drug discovery and the physicochemical properties of recently approved oral drugs. The section on drug class studies looks at antibody-drug conjugates and the discovery, evolution, and therapeutic potential of dopamine partial agonists. Featured case studies examine the discovery of Etelcalcetide for the treatment of secondary hyper-parathyroidism in patients with chronic kidney disease; the development of Lenvatinib Mesylate; the discovery and development of Venetoclax; and more. -Focuses on recently introduced drugs that have not been featured in any textbooks or general references, including Ocrelizumab, a new generation of anti-CD-20 mAb for the treatment of multiple sclerosis, and Venetoclax, a selective antagonist of BCL-2 -Features personal experiences of successful drug developers from industry and academia -Endorsed and supported by the International Union of Pure and Applied Chemistry (IUPAC) Successful Drug Discovery: Volume 4 provides a fascinating and informative look into the process of drug discovery and would be a great reference for those in the pharmaceutical industry, organic and pharmaceutical chemists, and lecturers in pharmacy.

Targeting Protein-Protein Interactions by Small Molecules

Targeting Protein-Protein Interactions by Small Molecules
A Book

by Chunquan Sheng,Gunda I. Georg

  • Publisher : Springer
  • Release : 2018-06-26
  • Pages : 329
  • ISBN : 9811307733
  • Language : En, Es, Fr & De
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This book comprehensively reviews the state-of-the-art strategies developed for protein-protein interaction (PPI) inhibitors, and highlights the success stories in new drug discovery and development. Consisting of two parts with twelve chapters, it demonstrates the design strategies and case studies of small molecule PPI inhibitors. The first part discusses various discovery strategies for small molecule PPI inhibitors, such as high throughput screening, hot spot-based design, computational approaches, and fragment-based design. The second part presents recent advances in small molecule inhibitors, focusing on clinical candidates and new PPI targets. This book has broad appeal and is of significant interest to the pharmaceutical science and medicinal chemistry communities.

Small-molecule Transcription Factor Inhibitors in Oncology

Small-molecule Transcription Factor Inhibitors in Oncology
A Book

by David E Thurston,Khondaker Miraz Rahman

  • Publisher : Royal Society of Chemistry
  • Release : 2018-09-05
  • Pages : 199
  • ISBN : 1788015274
  • Language : En, Es, Fr & De
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Oncogenic transcription factors are an increasingly important target for anticancer therapies. Inhibiting these transcription factors could allow tumour cells to be "reprogrammed", leading to apoptosis or differentiation from the malignant phenotype. As the use of kinase inhibitors is gradually declining, transcription factor inhibition is the next hot topic for oncology research and merits much attention. This book highlights recent progress in the development of small-molecule inhibitors of oncogenic transcription factors. It also presents the evidence that this important protein class can be modulated in a number of ways to develop novel classes of therapeutic agents. The broad range of aspects covered by the book is noteworthy and renders it enormously valuable. This title serves as a unique reference book for postgraduates, academic researchers and practitioners working in the fields of biochemistry, biotechnology, cell and molecular biology and bio-inorganic chemistry.

Biophysical Techniques in Drug Discovery

Biophysical Techniques in Drug Discovery
A Book

by Angeles Canales

  • Publisher : Royal Society of Chemistry
  • Release : 2017-11-14
  • Pages : 320
  • ISBN : 1788012860
  • Language : En, Es, Fr & De
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Biophysical techniques are used in many key stages of the drug discovery process including in screening for new receptor ligands, in characterising drug mechanisms, and in validating data from biochemical and cellular assays. This book provides an overview of the biophysical methods applied in drug discovery today, including traditional techniques and newer developments. Perspectives from academia and industry across a spectrum of techniques are brought together in a single volume. Small and biotherapeutic approaches are covered and strengths and limitations of each technique are presented. Case studies illustrate the application of each technique in real applied examples. Finally, the book covers recent developments in areas such as electron microscopy with discussions of their possible impact on future drug discovery. This is a go-to volume for biophysicists, analytical chemists and medicinal chemists providing a broad overview of techniques of contemporary interest in drug discovery.

The Use of Antibodies in Small-Molecule Drug Discovery

The Use of Antibodies in Small-Molecule Drug Discovery
A Book

by Anonim

  • Publisher : Unknown Publisher
  • Release : 2014
  • Pages : 329
  • ISBN : 9876543210XXX
  • Language : En, Es, Fr & De
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Antibodies are powerful research tools that can be used in many areas of biology to probe, measure, and perturb various biological structures. Successful drug discovery is dependent on the correct identification of a target implicated in disease, coupled with the successful selection, optimization, and development of a candidate drug. Because of their specific binding characteristics, with regard to specificity, affinity, and avidity, coupled with their amenability to protein engineering, antibodies have become a key tool in drug discovery, enabling the quantification, localization, and modulation of proteins of interest. This review summarizes the application of antibodies and other protein affinity reagents as specific research tools within the drug discovery process.

Drug Discovery Toxicology

Drug Discovery Toxicology
From Target Assessment to Translational Biomarkers

by Yvonne Will,J. Eric McDuffie,Andrew J. Olaharski,Brandon D. Jeffy

  • Publisher : John Wiley & Sons
  • Release : 2016-03-22
  • Pages : 584
  • ISBN : 1119053390
  • Language : En, Es, Fr & De
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As a guide for pharmaceutical professionals to the issues and practices of drug discovery toxicology, this book integrates and reviews the strategy and application of tools and methods at each step of the drug discovery process. • Guides researchers as to what drug safety experiments are both practical and useful • Covers a variety of key topics – safety lead optimization, in vitro-in vivo translation, organ toxicology, ADME, animal models, biomarkers, and –omics tools • Describes what experiments are possible and useful and offers a view into the future, indicating key areas to watch for new predictive methods • Features contributions from firsthand industry experience, giving readers insight into the strategy and execution of predictive toxicology practices

Introduction to Biological and Small Molecule Drug Research and Development

Introduction to Biological and Small Molecule Drug Research and Development
Chapter 3. The small molecule drug discovery process – from target selection to candidate selection

by Michael Stocks

  • Publisher : Elsevier Inc. Chapters
  • Release : 2013-05-07
  • Pages : 472
  • ISBN : 0128061936
  • Language : En, Es, Fr & De
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Drug discovery of small molecules from target selection through to clinical evaluation is a very complex, challenging but rewarding area of drug discovery. There are many obstacles along the journey from initial hit-finding activities, through optimization of compounds and eventually to delivery of robust candidate drugs (CDs) for clinical evaluation. This chapter presents key issues and literature solutions with respect to the optimization of hits into CDs. Details of the key hit-finding activities namely high-throughput screening, virtual screening, natural products, fragment-based drug discovery and fast-follower approaches are discussed. Key aspects of compound quality such as lipophilicity, solubility, drug metabolism and pharmacokinetic, plasma protein binding and cytochrome P450 inhibition/induction are discussed as well as potential safety liabilities such as human ether-a-go-go related gene, genotoxicity and phospholipidosis, Finally successful hit-to-lead and lead optimization case studies are presented to illustrate and highlight the key principles.

Managing the Drug Discovery Process

Managing the Drug Discovery Process
How to Make It More Efficient and Cost-Effective

by Walter Moos,Susan Miller,Stephen Munk,Barbara Munk

  • Publisher : Woodhead Publishing
  • Release : 2016-11-08
  • Pages : 536
  • ISBN : 0081006322
  • Language : En, Es, Fr & De
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Managing the Drug Discovery Process: How to Make It More Efficient and Cost-Effective thoroughly examines the current state of pharmaceutical research and development by providing chemistry-based perspectives on biomedical research, drug hunting and innovation. The book also considers the interplay of stakeholders, consumers, and the drug firm with attendant factors, including those that are technical, legal, economic, demographic, political, social, ecological, and infrastructural. Since drug research can be a high-risk, high-payoff industry, it is important to researchers to effectively and strategically manage the drug discovery process. This book takes a closer look at increasing pre-approval costs for new drugs and examines not only why these increases occur, but also how they can be overcome to ensure a robust pharmacoeconomic future. Written in an engaging manner and including memorable insights, this book is aimed at redirecting the drug discovery process to make it more efficient and cost-effective in order to achieve the goal of saving countless more lives through science. A valuable and compelling resource, this is a must-read for all students and researchers in academia and the pharmaceutical industry. Considers drug discovery in multiple R&D venues, including big pharma, large biotech, start-up ventures, academia, and nonprofit research institutes Analyzes the organization of pharmaceutical R&D, taking into account human resources considerations like recruitment and configuration, management of discovery and development processes, and the coordination of internal research within, and beyond, the organization, including outsourced work Presents a consistent, well-connected, and logical dialogue that readers will find both comprehensive and approachable

Natural Small Molecule Drugs from Plants

Natural Small Molecule Drugs from Plants
A Book

by Guan-Hua Du

  • Publisher : Springer
  • Release : 2018-11-19
  • Pages : 741
  • ISBN : 9811080224
  • Language : En, Es, Fr & De
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This book discusses 120 types of natural, small-molecule drugs derived from plants. They are grouped into 7 parts according their clinical uses, such as drugs for cardiovascular diseases, for metabolic diseases, for neuropsychiatric diseases, for immune-mediated inflammatory diseases, anti-tumor drugs, and drugs for parasites and bacterial infection. Each chapter systematically summarizes one drug, including its physicochemical properties, sources, pharmacological effects and clinical applications. To help readers understand the drug better, the research and pharmacological activity for each drug is also described, which serves as a salutary lesson for future drug development. Written by frontline researchers, teachers and clinicians working in field of pharmacy and pharmacology it provides an overview of natural, small-molecule drugs derived from plants for researchers in the field.

Drug Discovery and Development

Drug Discovery and Development
From Molecules to Medicine

by Omboon Vallisuta,Suleiman Olimat

  • Publisher : BoD – Books on Demand
  • Release : 2015-06-03
  • Pages : 330
  • ISBN : 9535121286
  • Language : En, Es, Fr & De
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It is very important for scientists all over the globe to enhance drug discovery research for better human health. This book demonstrates that various expertise are essential for drug discovery including synthetic or natural drugs, clinical pharmacology, receptor identification, drug metabolism, pharmacodynamic and pharmacokinetic research. The following 5 sections cover diverse chapter topics in drug discovery: Natural Products as Sources of Leading Molecules in Drug Discovery; Oncology and Drug Discovery; Receptors Involvement in Drug Discovery; Management and Development of Drugs against Infectious Diseases; Advanced Methodology.

New Therapeutic Strategies for Type 2 Diabetes

New Therapeutic Strategies for Type 2 Diabetes
Small Molecule Approaches

by Rob M Jones

  • Publisher : Royal Society of Chemistry
  • Release : 2012-09-30
  • Pages : 466
  • ISBN : 1849735328
  • Language : En, Es, Fr & De
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The diabetes mellitus epidemic is unfolding across the globe with the World Health Organization (WHO) reporting a worldwide prevalence of 177 million patients with diabetes. Type 2 diabetes accounts for approximately ninety percent of all diabetes cases. Long-term complications of type 2 diabetes include atherosclerosis, heart disease, stroke, end-stage renal disease, retinopathy leading to blindness, nerve damage, sexual dysfunction, frequent infections, and difficult-to-treat foot ulcers, sometimes resulting in lower limb amputation. Diabetics are twice as likely to develop cardiovascular disease or have a stroke, two to six times more likely to have transient ischemic attacks, and fifteen to forty times more likely to require lower-limb amputation compared with the general population. In 2002, the total economic cost of diabetes was estimated to be $132 billion accounting for one in every ten health care dollars spent in the United States. As a direct consequence of this economic impact and in light of the fact that current approved therapies fail to provide adequate therapeutic advantage in preventing hyperglycemia, industry has been heavily focused on addressing new fundamental cellular mechanisms that will potentially address this unmet need. New Therapeutic Strategies for Type 2 Diabetes provides the reader with the most comprehensive survey to-date of the most innovative small molecule research strategies targeted at treating the burgeoning type 2 diabetes epidemic. Each chapter is written by a recognised thought-leader in this field. The book will be an invaluable reference for researchers and medicinal chemists that concisely explains the biological mechanisms underpinning each cutting-edge therapeutic strategy along with key medicinal chemistry rationales and up-to- date clinical findings.

Physico-Chemical and Computational Approaches to Drug Discovery

Physico-Chemical and Computational Approaches to Drug Discovery
A Book

by F. Javier Luque,Xavier Barril

  • Publisher : Royal Society of Chemistry
  • Release : 2012
  • Pages : 418
  • ISBN : 1849733538
  • Language : En, Es, Fr & De
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Provides an updated view of the current challenges faced by computational tools to decipher the basis of ligand-receptor interaction and modeling of biomolecular systems and drug discovery.

Structure-based Drug Discovery

Structure-based Drug Discovery
A Book

by Harren Jhoti,Andrew R. Leach

  • Publisher : Springer Science & Business Media
  • Release : 2007-05-24
  • Pages : 250
  • ISBN : 1402044070
  • Language : En, Es, Fr & De
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This book describes some of the most exciting developments for the discovery of new drugs, such as Fragment-based methods. It contains the latest developments in technologies that can be used to obtain the 3-D structures. This book includes experimental approaches using X-ray crystallography and NMR for Fragment-based screening as well as other biophysical methods for studying protein/ligand interactions.