Protein Allostery in Drug Discovery PDF Download

Author: Jian Zhang
Publisher: Springer Nature
ISBN: 9811387192
Category : Medical
Languages : en
Pages : 386

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Book Description
The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.

Author: Rob Phillips
Publisher: Princeton University Press
ISBN: 0691200246
Category : Science
Languages : en
Pages : 436

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Book Description
A signature feature of living organisms is their ability to carry out purposeful actions by taking stock of the world around them. To that end, cells have an arsenal of signaling molecules linked together in signaling pathways, which switch between inactive and active conformations. The Molecular Switch articulates a biophysical perspective on signaling, showing how allostery—a powerful explanation of how molecules function across all biological domains—can be reformulated using equilibrium statistical mechanics, applied to diverse biological systems exhibiting switching behaviors, and successfully unify seemingly unrelated phenomena. Rob Phillips weaves together allostery and statistical mechanics via a series of biological vignettes, each of which showcases an important biological question and accompanying physical analysis. Beginning with the study of ligand-gated ion channels and their role in problems ranging from muscle action to vision, Phillips then undertakes increasingly sophisticated case studies, from bacterial chemotaxis and quorum sensing to hemoglobin and its role in mammalian physiology. He looks at G-protein coupled receptors as well as the role of allosteric molecules in gene regulation. Phillips concludes by surveying problems in biological fidelity and offering a speculative chapter on the relationship between allostery and biological Maxwell demons. Appropriate for graduate students and researchers in biophysics, physics, engineering, biology, and neuroscience, The Molecular Switch presents a unified, quantitative model for describing biological signaling phenomena.

Author: Aron W. Fenton
Publisher: Humana Press
ISBN: 9781617793332
Category : Science
Languages : en
Pages : 0

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Book Description
Despite considerable variability within the scientific community, allosteric regulation can best be defined functionally as how a macromolecule binds one ligand differently when a second ligand is or is not pre-bound to the macromolecule, which constitutes a vital aspect of protein structure/function. In Allostery: Methods and Protocols, expert researchers in the field provide key techniques to investigate this biological phenomenon. Focusing on heterotropic systems with some coverage of homotropic systems, this volume covers the monitoring of allosteric function, allosteric conformational changes, and allosteric changes in protein dynamics/sub-population distribution, as well as topics such as macromolecular and ligand engineering of allosteric functions and computational aids in the study of allostery. Written in the highly successful Methods in Molecular BiologyTM series format, the chapters include the kind of detailed description and implementation advice that is crucial for getting optimal results in the laboratory. Thorough and intuitive, Allostery: Methods and Protocols aids scientists in continuing to study ligand-induced, through-protein effects on protein function (ligand binding/catalysis), a phenomenon that is well recognized through the history of the life sciences and very poorly understood at the molecular level.

Author: Jean-Paul Renaud
Publisher: John Wiley & Sons
ISBN: 1118900502
Category : Medical
Languages : en
Pages : 1437

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Book Description
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Author:
Publisher: Academic Press
ISBN: 0080582249
Category : Science
Languages : en
Pages : 485

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Book Description
This volume commemorates the 50th anniversary of the appearance in Volume 4 in 1948 of Dr. Jeffries Wyman's famous paper in which he "laid down" the foundations of linkage thermodynamics. Experts in this area contribute articles on the state-of-the-art of this important field and on new developments of the original theory. Among the topics covered in this volume are electrostatic contributions to molecular free energies in solution; site-specific analysis of mutational effects in proteins; allosteric transitions of the acetylcholine receptor; and deciphering the molecular code of hemoglobin allostery.

Author: Ulrich Hoeger
Publisher: Springer Nature
ISBN: 3030417697
Category : Science
Languages : en
Pages : 527

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Book Description
This book focuses on respiratory proteins, the broad hemoglobin family, as well as the molluscan and arachnid hemocyanins (and their multifunctional roles). Featuring 20 chapters addressing invertebrate and vertebrate respiratory proteins, lipoproteins and other body fluid proteins, and drawing on the editors’ extensive research in the field, it is a valuable addition to the Subcellular Biochemistry book series. The book covers a wide range of topics, including lipoprotein structure and lipid transport; diverse annelid, crustacean and insect defense proteins; and insect and vertebrate immune complexes. It also discusses a number of other proteins, such as the hemerythrins; serum albumin; serum amyloid A; von Willebrand factor and its interaction with factor VIII; and C-reactive protein. Given its scope, the book appeals to biologists, biomedical scientists and clinicians, as well as advanced undergraduates and postgraduates in these disciplines. Available as a printed book and also as an e-book and e-chapters, the fascinating material included is easily accessible.

Author: Niels Bindslev
Publisher: CRC Press
ISBN: 1351660578
Category : Medical
Languages : en
Pages : 847

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Book Description
Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.

Author: Paulo Almeida
Publisher: Garland Science
ISBN: 1317285433
Category : Medical
Languages : en
Pages : 414

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Book Description
Proteins: Concepts in Biochemistry teaches the biochemical concepts underlying protein structure, evolution, stability and folding, and explains how interactions with macromolecular structures determine protein function. Intended for a one-semester biochemistry course with a focus on proteins, this textbook emphasizes the logic underlying biophysical chemical principles. Problems throughout the book encourage statistical and quantitative thinking. The text is ideal for senior undergraduates, first year graduate students, and practitioners in chemistry, biochemistry, biology, and biophysics.

Author: Herbert M. Sauro
Publisher: Future Skill Software
ISBN: 0982477317
Category : Science
Languages : en
Pages : 320

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Book Description
This book introduces fundamental concepts in kinetics that relate to system biology. Topics include basic kinetics, enzyme kinetics, generalized rate laws, gene regulation and introduction to elasticities. The text is suitable for junior/senior undergraduates and graduates who need access to information relevant to modeling biochemical pathways.

Author: Sydney Brenner
Publisher: Academic Press
ISBN:
Category : Medical
Languages : en
Pages : 654

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Book Description
Founded in 1959, by John Kendrew, the Journal of Molecular Biology was the first journal devoted to this new and revolutionary science. To celebrate the thirtieth anniversary of the Journal, the current editor, Sydney Brenner, has selected a number of papers from the first hundred volumes. They include the seminal papers on genetic regulation by Jacob and Monod and on allostery by Monod, Changeux and Jacob. Also included are many important papers on structural biology and molecular genetics and papers reflecting the initial developments in DNA cloning and sequencing. Of value to all biologists with an interest in the molecular basis of living systems, the book is a personal selection by the Editor. Readers are encouraged to compare it with their own choice from the Journal of Molecular Biology.