Protein Allostery in Drug Discovery

Protein Allostery in Drug Discovery
Author: Jian Zhang
Publisher: Springer Nature
Total Pages: 384
Release: 2019-11-09
Genre: Medical
ISBN: 9811387192

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.

The Molecular Switch

The Molecular Switch
Author: Rob Phillips
Publisher: Princeton University Press
Total Pages: 436
Release: 2020-09
Genre: Science
ISBN: 0691200246

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.

Allostery

Allostery
Author: Aron W. Fenton
Publisher: Humana Press
Total Pages: 0
Release: 2011-11-04
Genre: Science
ISBN: 9781617793332

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.

Structural Biology in Drug Discovery

Structural Biology in Drug Discovery
Author: Jean-Paul Renaud
Publisher: John Wiley & Sons
Total Pages: 1367
Release: 2020-01-09
Genre: Medical
ISBN: 1118900502

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

Vertebrate and Invertebrate Respiratory Proteins, Lipoproteins and other Body Fluid Proteins

Vertebrate and Invertebrate Respiratory Proteins, Lipoproteins and other Body Fluid Proteins
Author: Ulrich Hoeger
Publisher: Springer Nature
Total Pages: 527
Release: 2020-03-18
Genre: Science
ISBN: 3030417697

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.

Electrochemical Biosensors

Electrochemical Biosensors
Author: Serge Cosnier
Publisher: CRC Press
Total Pages: 405
Release: 2015-01-26
Genre: Science
ISBN: 9814411477

Since four decades, rapid detection and monitoring in clinical and food diagnostics and in environmental and biodefense have paved the way for the elaboration of electrochemical biosensors. Thanks to their adaptability, ease of use in relatively complex samples, and their portability, electrochemical biosensors now are one of the mainstays of analy

Linkage Thermodynamics of Macromolecular Interactions

Linkage Thermodynamics of Macromolecular Interactions
Author:
Publisher: Academic Press
Total Pages: 473
Release: 1998-06-03
Genre: Science
ISBN: 9780120342518

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.

Physical Biology of the Cell

Physical Biology of the Cell
Author: Rob Phillips
Publisher: Garland Science
Total Pages: 1089
Release: 2012-10-29
Genre: Science
ISBN: 1134111584

Physical Biology of the Cell is a textbook for a first course in physical biology or biophysics for undergraduate or graduate students. It maps the huge and complex landscape of cell and molecular biology from the distinct perspective of physical biology. As a key organizing principle, the proximity of topics is based on the physical concepts that

The Molecules of Life

The Molecules of Life
Author: Kuriyan, John
Publisher: W.W. Norton & Company
Total Pages: 15
Release: 2012-07-25
Genre: Science
ISBN: 0815341881

This textbook provides an integrated physical and biochemical foundation for undergraduate students majoring in biology or health sciences. It is particularly suitable for students planning to enter the pharmaceutical industry. This new generation of molecular biologists and biochemists will harness the tools and insights of physics and chemistry to exploit the emergence of genomics and systems-level information in biology, and will shape the future of medicine.

Proteins

Proteins
Author: Paulo Almeida
Publisher: Garland Science
Total Pages: 416
Release: 2016-03-14
Genre: Medical
ISBN: 1317285433

Proteins: Concepts in Biochemistry teaches the biochemical concepts underlying protein structure, evolution, stability, folding, and enzyme kinetics, and explains how interactions in macromolecular structures determine protein function. Intended for a one-semester course in biochemistry or biophysical chemistry with a focus on proteins, this textbo