Reversible Ligand Binding

Presents the physical background of ligand binding and instructs on how experiments should be designed and analyzed Reversible Ligand Binding: Theory and Experiment discusses the physical background of protein-ligand interactions—providing a comprehensive view of the various biochemical considerations that govern reversible, as well as irreversible, ligand binding. Special consideration is devoted to enzymology, a field usually treated separately from ligand binding, but actually governed by identical thermodynamic relationships. Attention is given to the design of the experiment, which aids in showing clear evidence of biochemical features that may otherwise escape notice. Classical experiments are reviewed in order to further highlight the importance of the design of the experiment. Overall, the book supplies students with the understanding that is necessary for interpreting ligand binding experiments, formulating plausible reaction schemes, and analyzing the data according to the chosen model(s). Topics covered include: theory of ligand binding to monomeric proteins; practical considerations and commonly encountered problems; oligomeric proteins with multiple binding sites; ligand binding kinetics; hemoglobin and its ligands; single-substrate enzymes and their inhibitors; two-substrate enzymes and their inhibitors; and rapid kinetic methods for studying enzyme reactions. Bridges theory of ligand binding and allostery with experiments Applies historical and physical insight to provide a clear understanding of ligand binding Written by a renowned author with long-standing research and teaching expertise in the area of ligand binding and allostery Based on FEBS Advanced Course lectures on the topic Reversible Ligand Binding: Theory and Experiment is an ideal text reference for students and scientists involved in biophysical chemistry, physical biochemistry, biophysics, molecular biology, protein engineering, drug design, pharmacology, physiology, biotechnology, and bioengineering.

Vital information for discovering and optimizing new drugs "Understanding the data and the experimental details that support it has always been at the heart of good science and the assumption challenging process that leads from good science to drug discovery. This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors." -Paul S. Anderson, PhD This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications. Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address: * What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? * How are inhibitors evaluated for potency, selectivity, and mode of action? * What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo? * What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization? Beginning with a discussion of the advantages of enzymes as targets for drug discovery, the publication then explores the reaction mechanisms of enzyme catalysis and the types of interactions that can occur between enzymes and inhibitory molecules that lend themselves to therapeutic use. Next are discussions of mechanistic issues that must be considered when designing enzyme assays for compound library screening and for lead optimization efforts. Finally, the publication delves into special forms of inhibition that are commonly encountered in drug discovery efforts, but can be easily overlooked or misinterpreted. This publication is designed to provide students with a solid foundation in enzymology and its role in drug discovery. Medicinal chemists and pharmacologists can refer to individual chapters as specific issues arise during the course of their ongoing drug discovery efforts.

Ninfa/Ballou/Benore is a solid biochemistry lab manual, dedicated to developing research skills in students, allowing them to learn techniques and develop the organizational approaches necessary to conduct laboratory research. Ninfa/Ballou/Benore focuses on basic biochemistry laboratory techniques with a few molecular biology exercises, a reflection of most courses which concentrate on traditional biochemistry experiments and techniques. The manual also includes an introduction to ethics in the laboratory, uncommon in similar manuals. Most importantly, perhaps, is the authors' three-pronged approach to encouraging students to think like a research scientist: first, the authors introduce the scientific method and the hypothesis as a framework for developing conclusive experiments; second, the manual's experiments are designed to become increasingly complex in order to teach more advanced techniques and analysis; finally, gradually, the students are required to devise their own protocols. In this way, students and instructors are able to break away from a "cookbook" approach and to think and investigate for themselves. Suitable for lower-level and upper-level courses; Ninfa spans these courses and can also be used for some first-year graduate work.

Providing a cutting-edge profile of research progress in this important field of study, Cholinergic Mechanisms: Function and Dysfunction contains a compilation of the proceedings of the Eleventh ISCM, held in St. Moritz, May 2002. Bringing together 250 contributors from 30 countries, the book presents a comprehensive picture of the cholinergic field. It provides a survey of current understanding of molecular, pharmacological, toxicological, behavioral, and clinical aspects of the cholinergic system. This volume offers a state-of-the-art account of progress in the field from the molecule in the test tube through the cell and the synapse, to the organism and the patient.

Throughout human history, we have long encountered the combination of promise, risk, and uncertainty that accompanies emerging technologies. Nanotechnology is a recent example of an emerging technology that promises to drastically improve existing products as well as allow for creative development of new goods and services. This new technology also has its potential downsides. Industry, academia, and regulatory agencies are all working overtime to assess risks accurately while keeping up with the pace of development. Subtle changes in the physicochemical properties of engineered nanomaterials (ENMs) can influence their toxicity and behavior in the environment and so can be used to help control potential ENM risks. This book attempts to encompass the state of the science regarding physicochemical characterization of ENMs. It illuminates the effort to understand these properties and how they may be used to ensure safe ENM deployment in existing or future materials and products.

Comprehensive and authoritative, Opioid Receptors and Antagonists: From Bench to Clinic offers neuroscientists, pharmacologists and interested clinicians a unique survey of the extensive and diverse research efforts currently employed with opioid antagonists to develop novel innovative drug therapies. Summarizes the present understanding of the chemistry, pharmacology and molecular biology of opioid receptors and their subtypes Highlights differences and similarities between the opioid pharmacology of animals and human Describes current and potential therapeutic areas for opioid antagonists, including substance abuse, alcohol and ingestive behaviors, behavioral disorders and other medical indications, supported by nonclinical and clinical evidence Focuses on the development of exciting and innovative drug delivery approaches that are being used with opioid antagonists for the above medical indications

Progress in Medicinal Chemistry, Volume 62 provides a review of eclectic developments in medicinal chemistry, with each chapter written by an international board of authors. Provides extended, timely reviews of topics in medicinal chemistry Contains targets and technologies relevant to the discovery of tomorrow’s drugs Presents analyses of successful drug discovery programs