Download or read book Protein Ligand Interactions written by Hans-Joachim Böhm and published by John Wiley & Sons. This book was released on 2006-03-06 with total page 262 pages. Available in PDF, EPUB and Kindle. Book excerpt: The lock-and-key principle formulated by Emil Fischer as early as the end of the 19th century has still not lost any of its significance for the life sciences. The basic aspects of ligand-protein interaction may be summarized under the term 'molecular recognition' and concern the specificity as well as stability of ligand binding. Molecular recognition is thus a central topic in the development of active substances, since stability and specificity determine whether a substance can be used as a drug. Nowadays, computer-aided prediction and intelligent molecular design make a large contribution to the constant search for, e. g., improved enzyme inhibitors, and new concepts such as that of pharmacophores are being developed. An up-to-date presentation of an eternally young topic, this book is an indispensable information source for chemists, biochemists and pharmacologists dealing with the binding of ligands to proteins.
Download or read book Receptor Ligand Interactions written by Hulme and published by . This book was released on with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Receptor ligand Interactions written by E. C. Hulme and published by Oxford University Press, USA. This book was released on 1992 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This is the final volume in a set of 3 books detailing practical methods for the investigation of biochemical receptors. This book deals with the performance and interpretation of receptor-ligand binding studies which are important in many areas of pharmacological and neurochemical research.
Download or read book Protein Ligand Interactions written by Holger Gohlke and published by John Wiley & Sons. This book was released on 2012-05-21 with total page 361 pages. Available in PDF, EPUB and Kindle. Book excerpt: Innovative and forward-looking, this volume focuses on recent achievements in this rapidly progressing field and looks at future potential for development. The first part provides a basic understanding of the factors governing protein-ligand interactions, followed by a comparison of key experimental methods (calorimetry, surface plasmon resonance, NMR) used in generating interaction data. The second half of the book is devoted to insilico methods of modeling and predicting molecular recognition and binding, ranging from first principles-based to approximate ones. Here, as elsewhere in the book, emphasis is placed on novel approaches and recent improvements to established methods. The final part looks at unresolved challenges, and the strategies to address them. With the content relevant for all drug classes and therapeutic fields, this is an inspiring and often-consulted guide to the complexity of protein-ligand interaction modeling and analysis for both novices and experts.
Download or read book Receptor Binding Techniques written by Anthony P. Davenport and published by Humana. This book was released on 2005-03-25 with total page 240 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive collection of readily reproducible methods for studying receptors in silico, in vitro, and in vivo. These cutting-edge techniques cover mining from curated databases, identifying novel receptors by high throughput screening, molecular methods to identify mRNA encoding receptors, radioligand binding assays and their analysis, quantitative autoradiography, and imaging receptors by positron emission tomography (PET). Highlights include phenotypic characterization of receptors in knockout mice, imaging receptors using green fluorescent protein and fluorescent resonance energy transfer, and quantitative analysis of receptor mRNA by TaqMan PCR. These book equips the researcher with techniques for exploring the unprecedented number of new receptor systems now emerging and the so-called "orphan" receptors whose activating ligand has not been identified.
Download or read book Protein Ligand Interactions written by Mark A. Williams and published by Humana. This book was released on 2016-11-17 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Proteins are the cell’s workers, their messengers and overseers. In these roles, proteins specifically bind small molecules, nucleic acid and other protein partners. Cellular systems are closely regulated and biologically significant changes in populations of particular protein complexes correspond to very small variations of their thermodynamics or kinetics of reaction. Interfering with the interactions of proteins is the dominant strategy in the development of new pharmaceuticals. Protein Ligand Interactions: Methods and Applications, Second Edition provides a complete introduction to common and emerging procedures for characterizing the interactions of individual proteins. From the initial discovery of natural substrates or potential drug leads, to the detailed quantitative understanding of the mechanism of interaction, all stages of the research process are covered with a focus on those techniques that are, or are anticipated to become, widely accessible and performable with mainstream commercial instrumentation. Written in the highly successful Methods in Molecular Biology series format, chapters contain introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and notes on troubleshooting and avoiding known pitfalls. Authoritative and accessible, Protein Ligand Interactions: Methods and Applications, Second Edition serves as an ideal guide for researchers new to the field of biophysical characterization of protein interactions – whether they are beginning graduate students or experts in allied areas of molecular cell biology, microbiology, pharmacology, medicinal chemistry or structural biology.
Download or read book Receptor Binding Techniques written by Anthony P. Davenport and published by Humana Press. This book was released on 2012-06-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: A broad definition of a receptor is a specialized protein on or in a cell that recognizes and binds a specific ligand to undergo a conformational change, leading to a physiological response or change in cell function. A ligand can be an endogenous neurotransmitter, hormone, paracrine/autocrine factor, or a synthetic drug that may function as an agonist or antagonist. The third edition of Receptor Binding Techniques expands upon the methods and techniques used for studying receptors in silico, in vitro and in vivo. Comprehensive chapters describe how to use online resources for experimental research such as prediction of receptor-ligand interactions and mine the IUPHAR receptor database. Classical techniques of radioligand binding, quantitative autoradiography and their analyses are complemented by the use of immunocytochemistry for the cellular localization of receptor protein and hybridization to detect receptor mRNA. Protocols using fluorescent labeled ligands are described to visualise receptors in living cells, their interaction with beta-arrestin to measure ligand-induced internalisation and green fluorescent protein to study trafficking. Non-radioactive, chemiluminescent cAMP and arrestin assays facilitate the identification of novel ‘biased agonists’. Detailed methods are provided for in vivo imaging of receptors using positron emission tomography (PET). Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Receptor Binding Techniques, Third Edition, aids scientists in continuing to study receptor binding.
Download or read book Tailoring NK Cell Receptor Ligand Interactions an Art in Evolution 2nd Edition written by Ulrike Koehl and published by Frontiers Media SA. This book was released on 2018-11-13 with total page 407 pages. Available in PDF, EPUB and Kindle. Book excerpt: Recognition and killing of aberrant, infected or tumor targets by Natural Killer (NK) cells is mediated by positive signals transduced by activating receptors upon engagement of ligands on target surface. These stimulatory pathways are counterbalanced by inhibitory receptors that raise NK cell activation threshold through negative antagonist signals. While regulatory effects are necessary for physiologic control of autoimmune aggression, they may restrain the ability of NK cells to activate against disease. Overcoming this barrier to immune surveillance, multiple approaches to enhance NK-mediated responses are being investigated since two decades. Propelled by considerable advances in the understanding of NK cell biology, these studies are critical for effective translation of NK-based immunotherapy principles into the clinic. In humans, dominant inhibitory signals are transduced by Killer Immunoglobulin Like Receptors (KIR) recognizing cognate HLA class I on target cells. Conversely, KIR recognition of “missing self-HLA” - due to HLA loss or HLA/ KIR mismatch - triggers NK-mediated tumor rejection. Initially observed in murine transplant models, these antitumor effects were later found to have important implications for the clinical outcome of haplotype-mismatched stemcell transplantation. Here, donor NK subsets protect against acute myeloid leukemia (AML) relapse through missing self recognition of donor HLA-C allele groups (C1 or C2) and/or Bw4 epitope. These studies were subsequently extended by trials investigating the antileukemia effects of adoptively transferred haplotype-mismatched NK cells in non-transplant settings. Other mechanisms have been found to induce clinically relevant NK cell alloreactivity in transplantation, e.g., post-reconstitution functional reversal of anergic NK cells. More recently, activating KIR came into the spotlight for their potential ability to directly activate donor NK cells through in vivo recognition of HLA or other ligands. Novel therapeutic monoclonal antibodies (mAb) may optimize NK-mediated effects. Examples include obinutuzumab (GA101), a glyco-engineered anti-CD20 mAb with increased affinity for the FcγRIIIA receptor, enhancing antibody-dependent cellular cytotoxicity; lirilumab (IPH2102), a first-in-class NK-specific checkpoint inhibitor, blocking the interaction between the major KIR and cognate HLA-C antigens; and elotuzumab (HuLuc63), a humanized monoclonal antibody specific for SLAMF7, whose anti-myeloma therapeutic effects are partly due to direct activation of SLAMF7-expressing NK cells. In addition to conventional antibodies, NK cell-targeted bispecific (BiKEs) and trispecific (TriKEs) killer engagers have also been developed. These proteins elicit potent effector functions by binding target ligands (e.g., CD19, CD22, CD30, CD133, HLA class II, EGFR) on one arm and NK receptors on the other. An additional innovative approach to direct NK cell activity is genetic reprogramming with chimeric antigen receptors (CAR). To date, primary NK cells and the NK92 cell line have been engineered with CAR specific for antigens expressed on multiple tumors. Encouraging preclinical results warrant further development of this approach. This Research Topic welcomes contributions addressing mechanisms of NK-mediated activation in response to disease as well as past and contemporary strategies to enhance NK mediated reactivity through control of the interactions between NK receptors and their ligands.
Download or read book Protein Ligand Interactions and Drug Design written by Flavio Ballante and published by . This book was released on 2021 with total page 327 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Cells Molecules and Mechanisms written by Eric Wong and published by Axolotl Academic Publishing. This book was released on 2009 with total page 283 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Yet another cell and molecular biology book? At the very least, you would think that if I was going to write a textbook, I should write one in an area that really needs one instead of a subject that already has multiple excellent and definitive books. So, why write this book, then? First, it's a course that I have enjoyed teaching for many years, so I am very familiar with what a student really needs to take away from this class within the time constraints of a semester. Second, because it is a course that many students take, there is a greater opportunity to make an impact on more students' pocketbooks than if I were to start off writing a book for a highly specialized upper- level course. And finally, it was fun to research and write, and can be revised easily for inclusion as part of our next textbook, High School Biology."--Open Textbook Library.
Download or read book DNA Ligand Interactions written by W. Guschlbauer and published by Springer Science & Business Media. This book was released on 2013-06-29 with total page 289 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume contains the texts of the nineteen lectures presented at the NATO-ASI - FEBS Course on "DNA - ligand interactions: from drugs to proteins." The Advanced Study Institute (ASIl was held from August 30th to September 11th. 1986 in the Abbey of Fontevraud (France). The ASI was attended by 112 participants from a wide scientific horizon and from twentyone different countries. It was in some way a follow-up of the ASI held in Maratea. Italy in May 1981 and which was published in the NATO ASI Life Science series as volume 45. While much has been learned about the way the cellular machinery maintains and transmits the genetic heritage. as well as how these processes are regulated. little is Known about how the interactions between the various partners involved are taKing place. The interactions of drugs and proteins with nucleic acids are of evident importance in the understanding of these problems. The spectacular advances in recombinant DNA technology and the increased sophistication of biophysical techniques. in particular >:-ray diffraction and nuclear magnetic resonance. have created a scientific environment which is highly promising for the future of research in molecular biology. These advances permH the serious hope that biology on the molecular level may become a r-eality. Some of the contributions at the ASI presented the most recent advances in this e>:citing field.
Download or read book Protein Ligand Interactions written by Holger Gohlke and published by John Wiley & Sons. This book was released on 2012-06-04 with total page 28 pages. Available in PDF, EPUB and Kindle. Book excerpt: Innovative and forward-looking, this volume focuses on recent achievements in this rapidly progressing field and looks at future potential for development. The first part provides a basic understanding of the factors governing protein-ligand interactions, followed by a comparison of key experimental methods (calorimetry, surface plasmon resonance, NMR) used in generating interaction data. The second half of the book is devoted to insilico methods of modeling and predicting molecular recognition and binding, ranging from first principles-based to approximate ones. Here, as elsewhere in the book, emphasis is placed on novel approaches and recent improvements to established methods. The final part looks at unresolved challenges, and the strategies to address them. With the content relevant for all drug classes and therapeutic fields, this is an inspiring and often-consulted guide to the complexity of protein-ligand interaction modeling and analysis for both novices and experts.
Download or read book Experimental Neurochemistry written by Abel Lajtha and published by Springer. This book was released on 1982-12-01 with total page 516 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second volume of the Handbook does not parallel any volume of the first edition; it is one more sign, or reflection, of the expansion of the field. By emphasizing the experimental approach, it illustrates the tools that have re cently become available for investigating the nervous system. Also, perhaps even more than other volumes, it illustrates the multidisciplinary nature of the field, requiring multidisciplinary methodology. It is now recognized that the availability of methodology is often the rate-limiting determinant of studies and that improvements or innovations in instrumentation can open up new avenues. A new improved method, although opening up new possibilities and being crucial to making advances, is only a tool whose use will determine its use fulness. If we do not recognize its possibilities, its use will be limited; if we do not recognize its limitations, it will mislead us. It is the possibilities and limitations and the results obtained that are illustrated here.
Download or read book Monolithic Materials written by F. Svec and published by Elsevier. This book was released on 2003-04-29 with total page 800 pages. Available in PDF, EPUB and Kindle. Book excerpt: During the past decade, monolithic materials in the shape of discs, stacked layers, rolled sheets, sponges, irregular chunks, tubes, and cylinders have all been successfully demonstrated. These formats were prepared from a wide variety of materials including natural polymers such as cellulose, synthetic polymers that involved porous styrene-, methacrylate-, and acrylamide-based polymers, and inorganic materials, mainly silica. Each approach is interesting from the point of view of both preparation and application.Although the current papers and patents concerned with monolithic separation media are quite numerous, the information is scattered throughout a vast number of journals. This book therefore fills the gap in the market for a comprehensive reference book on this subject.Monolithic materials concerns all of the current formats of monolithic materials and provides an integrated view of this novel format of separation media. Since the flow pattern in monolithic devices is different from that in packed beds, the hydrodynamics of the system and mass transport differ considerably from those derived for packed columns. Therefore, this book presents contributions concerned with both flow and mass transfer in the monolithic materials. A significant proportion of the book is devoted to the applications of monolithic materials. It also provides the reader with valuable information about the sources of the specific materials, their properties, and potential applications. · Monolithic materials are currently very popular within several scientific areas such as chromatography, optics, catalysis, diagnostics, genomics, proteomics, and microfluidics.· Provides valuable information about the sources of the specific materials, their properties, and potential applications.· Chapters written by leading experts in the area.
Download or read book Cholinergic Ligand Interactions written by D. J. Triggle and published by Academic Press. This book was released on 2014-06-28 with total page 215 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cholinergic Ligand Interactions presents the papers read at a symposium held at the State University of New York at Buffalo, 25-26 May 1970. The recent purification and crystallization of acetylcholinesterase together with real progress in the purification of receptor components indicated the desirability of organizing a symposium to discuss not only these aspects but also the structural bases for cholinergic ligand interaction with these macromolecules, the conformational changes involved with ligand binding, the quantitation of cholinergic ligand binding sites, and the roles of acetylcholinesterase and its isozymes in muscle disease. The volume contains nine chapters and begins with a study on possible conformational changes in acetylcholinesterase. This is followed by separate chapters on the subunits of acetylcholinesterase; in vitro studies with the cholinergic receptor of the eel electroplax; identification and isolation of acetylcholine receptors; assay and properties of essential (junctional) cholinesterases of the rat diaphragm; and structural variations in cholinergic ligands. Subsequent chapters deal with ligand interactions at the muscarinic receptors and changes in cholinesterases isozymes during normal and dystrophic muscle development.
Download or read book Applied Biophysics for Drug Discovery written by Donald Huddler and published by John Wiley & Sons. This book was released on 2017-10-02 with total page 148 pages. Available in PDF, EPUB and Kindle. Book excerpt: Applied Biophysics for Drug Discovery is a guide to new techniques and approaches to identifying and characterizing small molecules in early drug discovery. Biophysical methods are reasserting their utility in drug discovery and through a combination of the rise of fragment-based drug discovery and an increased focus on more nuanced characterisation of small molecule binding, these methods are playing an increasing role in discovery campaigns. This text emphasizes practical considerations for selecting and deploying core biophysical method, including but not limited to ITC, SPR, and both ligand-detected and protein-detected NMR. Topics covered include: • Design considerations in biophysical-based lead screening • Thermodynamic characterization of protein-compound interactions • Characterizing targets and screening reagents with HDX-MS • Microscale thermophoresis methods (MST) • Screening with Weak Affinity Chromatography • Methods to assess compound residence time • 1D-NMR methods for hit identification • Protein-based NMR methods for SAR development • Industry case studies integrating multiple biophysical methods This text is ideal for academic investigators and industry scientists planning hit characterization campaigns or designing and optimizing screening strategies.
Download or read book Principles of Chemical Sensors written by Jiri Janata and published by Springer Science & Business Media. This book was released on 2010-03-14 with total page 382 pages. Available in PDF, EPUB and Kindle. Book excerpt: Do not learn the tricks of the trade, learn the trade I started teachinggraduate coursesin chemical sensors in early 1980s, ?rst as a o- quarter (30 h) class then as a semester course and also as several intensive, 4–5-day courses. Later I organized my lecture notes into the ?rst edition of this book, which was published by Plenum in 1989 under the title Principles of Chemical Sensors. I started working on the second edition in 2006. The new edition of Principles of Chemical Sensors is a teaching book, not a textbook. Let me explain the difference. Textbooks usually cover some more or less narrow subject in maximum depth. Such an approach is not possible here. The subject of chemical sensors is much too broad, spanning many aspects of physical and analytical chemistry, biochemistry, materials science, solid-state physics, optics, device fabrication, electrical engine- ing, statistical analysis, and so on. The challengefor me has been to present uniform logical coverage of such a large area. In spite of its relatively shallow depth, it is intended as a graduate course. At its present state the amount of material is more thancan be coveredin a one-semestercourse (45h). Two one-quartercourseswould be more appropriate. Because of the breadth of the material, the sensor course has a somewhat unexpected but, it is hoped, bene?cial effect.
