Biased Signaling and Allosteric Modulation of the Angiotensin II Type 1 Receptor

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ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (973 download)

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Book Synopsis Biased Signaling and Allosteric Modulation of the Angiotensin II Type 1 Receptor by : Stephanie Clement

Download or read book Biased Signaling and Allosteric Modulation of the Angiotensin II Type 1 Receptor written by Stephanie Clement and published by . This book was released on 2016 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: "G protein coupled receptors (GPCR) represent over 30% of drug targets and are involved in nearly all physiological and cellular responses. The angiotensin II (AngII) type I receptor (AT1R) is an important member of this receptor family. Its main endogenous ligand is the hormone angiotensin II (AngII), which regulates blood volume and vascular resistance, through the renin-angiotensin system (RAS). This hormone is involved in hypertension and other cardiovascular diseases. A way to improve today's therapeutic approach is to aim for the activation of the beneficial cellular responses without activating the ones responsible for undesirable effects. This type of response can be achieved using ligands that show functional selectivity, also known as biased signaling. This type of ligand imposes distinct conformations to the receptor, therefore promoting selective downstream effector activation. Moreover, our lab has recently shown that functional selectivity was possible using an allosteric modulator (a ligand binding to any site on a GPCR that is topographically distinct from the endogenous binding site). Our group has shown that a peptide mimic of a sequence derived from the second extracellular loop (ECL2) domains of the prostaglandin F2[alpha] (PGF2[alpha]) receptor (FP) acted as a biased-allosteric modulator of FP. We hypothesized that the ECL2 of other GPCRs can be used as putative biased-allosteric modulators. To test this, we used the angiotensin II (AngII) type I receptor (AT1R). We have examined the effects of peptides (SC0023/SC0024) derived from AT1R's ECL2 in vascular smooth muscle cells (VSMC). This was done using techniques including western blots, Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) and [3H]-Thymidine incorporation. We show in VSMCs that the SC0023 peptide decreases angiotensin II-induced ERK1/2 activation and inositol monophosphate (IP1) production, thus acting as a negative allosteric modulator (NAM) on these signaling pathways. Conversely, SC0024 has no effect on ERK1/2 while acting as a positive allosteric modulator (PAM) on IP1 production. Interestingly, the SC0023 peptide showed no modulatory effect on proliferation in response to angiotensin II, whereas the SC0024 peptide inhibited almost completely this response, hence acting as a NAM on AngII-mediated proliferation. In addition, structure-function studies underscored the importance of three residues (Phe-His-Tyr) of peptide SC0024 for its NAM effect on proliferation. More importantly, these peptides alone showed no effect on any of the pathways studied, thus only working in the presence of agonist, which is characteristic of most allosteric modulators. These data imply that these two peptides derived from the ECL of AT1R are allosteric modulators with biased signaling properties. Indeed, SC0023 acts as a NAM of ERK1/2 activation and IP1 production, while SC0024 acts as a PAM of IP1 production and a NAM of proliferation. Ultimately, understanding how the ECL2 is allosterically biasing its receptor will allow us to design new and more efficient therapeutics." --

The Angiotensin 2 Receptor Type 1 Biased Agonist [Sar1, Ile4, Ile8]-Ang II is a Negative Allosteric Modulator of Bradykinin B2 Receptor Signaling

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ISBN 13 :
Total Pages : 286 pages
Book Rating : 4.:/5 (94 download)

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Book Synopsis The Angiotensin 2 Receptor Type 1 Biased Agonist [Sar1, Ile4, Ile8]-Ang II is a Negative Allosteric Modulator of Bradykinin B2 Receptor Signaling by : Parker C. Wilson

Download or read book The Angiotensin 2 Receptor Type 1 Biased Agonist [Sar1, Ile4, Ile8]-Ang II is a Negative Allosteric Modulator of Bradykinin B2 Receptor Signaling written by Parker C. Wilson and published by . This book was released on 2012 with total page 286 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Structural Basis of Biased Signaling in the Angiotensin II Type 1 Receptor

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ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (985 download)

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Book Synopsis Structural Basis of Biased Signaling in the Angiotensin II Type 1 Receptor by : Milos Matkovic

Download or read book Structural Basis of Biased Signaling in the Angiotensin II Type 1 Receptor written by Milos Matkovic and published by . This book was released on 2017 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:

Understanding the Molecular Determinants for Functional Selectivity of the Angiotensin II Type 1 Receptor

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ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (129 download)

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Book Synopsis Understanding the Molecular Determinants for Functional Selectivity of the Angiotensin II Type 1 Receptor by : Yubo Cao

Download or read book Understanding the Molecular Determinants for Functional Selectivity of the Angiotensin II Type 1 Receptor written by Yubo Cao and published by . This book was released on 2021 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: "Hypertension and its associated cardiovascular risks can be attributed to angiotensin II (AngII), which regulates blood volume and vascular resistance through the AngII type 1 receptor (AT1R). As a G protein-coupled receptor (GPCR), the AT1R signals by coupling to G proteins (G[alpha]q/11, G[alpha]12/13, G[alpha]i1/2/3) and [beta]-arrestins ([beta]-arr1 and 2, which act both as endocytic and signaling adaptors) to mediate its physiological effects. While most drugs that target the AT1R act by blocking the activation of the receptor and thereby attenuating all of its downstream signaling pathways indiscriminately, studies have highlighted that certain AT1R-mediated pathways may promote beneficial cardio-protective effects. Thus, recent efforts have been focused on developing ligands that stabilize unique conformations in the AT1R that promote selective signaling pathway and downstream effector activation - a phenomenon known as biased signaling or functional selectivity. However, development of such efficacious biased ligands have been met with major hurdles, as although it is proposed that AngII binding induces a conformational change in the AT1R that favors its coupling to G proteins and [beta]-arrs, the molecular determinants for activating specific signaling pathways remain unknown. Moreover, the involvement of each signaling pathway towards specific cellular outcomes is unresolved.In the first half of my thesis, I begin by describing the technical application of our enhanced bystander BRET biosensors to monitor [beta]-arr-mediated internalization and trafficking for different classes of GPCRs, published as a book chapter. These techniques, along with conformational fluorescein arsenical hairpin (FlAsH)-BRET sensors and high-resolution fluorescence microscopy, were used extensively in my second publication investigating the [beta]-arr-mediated trafficking and signaling of three naturally occurring AT1R variants: A163T, T282M, and C289W. We found that some variants, most notably T282M, imposed distinct conformations in [beta]-arrestin and decreased the avidity of the receptor for [beta]-arr and residency with [beta]-arr in endosomes. Ultimately, T282M decreased [beta]-arr-dependent ERK1/2 activation, increased the rate of receptor recycling to the PM, and impaired AngII-mediated proliferation, highlighting the importance of [beta]-arrestin-mediated MAPK activation and endosomal receptor-[beta]-arrestin complex stabilization in the mitogenic response of AT1R.The latter half of my thesis focuses on pinpointing the amino acid residues in the AT1R involved in engaging specific signaling pathways to identify the molecular determinants of the AT1R governing its functional selectivity. In my third manuscript (currently under review), using molecular dynamics simulations, dynamic allostery analysis, and functional BRET assays, we identified a network of residues involved in allosteric communication from the AngII binding site to the putative Gq coupling sites and another network to the [beta]-arrestin2 coupling sites. Finally in my fourth manuscript (currently in preparation), I've also conducted an alanine scan of the 359 amino acids in the AT1R to systematically characterize the Gq and [beta]-arrestin activation profile of these mutants. I identified novel orthosteric AngII binding sites and key residues in AT1R that elicit unique signal transduction behaviors, and by stratifying the different mutants according to their signaling profiles, establish networks of residues that are critical for distinct signaling pathways. Altogether, the findings in my thesis will help to understand the molecular mechanism for activating distinct AT1R signaling pathways and provide new insights towards the development of efficacious biased ligands and better-targeted therapeutics against the AT1R"--

Mechanical and Chemical Activation of the Angiotensin II Type 1 Receptor

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ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.:/5 (14 download)

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Book Synopsis Mechanical and Chemical Activation of the Angiotensin II Type 1 Receptor by : Bharat Poudel

Download or read book Mechanical and Chemical Activation of the Angiotensin II Type 1 Receptor written by Bharat Poudel and published by . This book was released on 2023 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Angiotensin II Type 1 (AT1) receptor is one of the most widely studied G-protein coupled receptors (GPCRs) within the context of biased signaling. Unlike other GPCRs, the AT1 receptor is activated not only by agonists such as the peptide AngII, but also by mechanical stimuli including membrane stretch and shear in the absence of a ligand. These various chemical and mechanical modes of activation induce different cellular signaling pathways. Despite the importance of mechanical activation of the AT1 receptor in biological processes such as vasoconstriction, little is known about the structural changes induced by external physical stimuli mediated by the surrounding lipid membrane. Here, we present a systematic molecular dynamics (MD) simulation study that characterizes the activation of the AT1 receptor under various membrane environments and mechanical stimuli along with the AT1 receptor complexes with agonists and a G-protein mimicking nanobody. First, we characterized the stability of the active state of the AT1 receptor and its sensitivity to changes in the surrounding membrane environment from variations in the lipid acyl chain length, head-group chemistry, and membrane tension (i.e., mechanical stretch). MD simulations of the apo AT1 receptor in DMPC, POPC, and SOPC show that there is an optimal bilayer thickness that favors activation (POPC), while shorter (DMPC) and longer (SOPC) lipids promote inactivation within a few microseconds. Addition of SOPE lipids, which have a more negative spontaneous curvature, to the SOPC membrane in a 1:1 ratio also stabilizes the active state despite having a larger bilayer thickness compared to SOPC. Similarly to changing the acyl chain length, we found that membrane tension stabilizes the AT1 receptor's active state in a value-dependent manner, where intermediate tensions around 10 mN/m are optimal. Structural comparison of membrane-mediated vs.~agonist-induced activation shows that the AT1 receptor has distinct active conformations. This is supported by long multi-microsecond unbiased simulations and free energy calculations that show unique landscapes for the inactive and various active states. In addition to the mechanical activation of the AT1 receptor, we also explored the role of biased agonists as well as constitutive mutations. Our MD simulations and free energy calculations show that G-protein and [Beta]-arrestin biased agonists stabilize active-like states with different structural features. Finally, we explore the constitutively active double mutant F77A/N111G, which has been shown experimentally to increase the basal activity of the AT1 receptor, has a highly dynamic structure that can readily explore active and inactive states. Our modeling results provide structural insights into the mechanical and chemical activation of the AT1 receptor and how it may produce different functional outcomes within the framework of biased agonism.

Biased Signaling in Physiology, Pharmacology and Therapeutics

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Publisher : Elsevier
ISBN 13 : 0124115071
Total Pages : 317 pages
Book Rating : 4.1/5 (241 download)

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Book Synopsis Biased Signaling in Physiology, Pharmacology and Therapeutics by : Brian J Arey

Download or read book Biased Signaling in Physiology, Pharmacology and Therapeutics written by Brian J Arey and published by Elsevier. This book was released on 2014-06-05 with total page 317 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biased Signaling in Physiology, Pharmacology and Therapeutics is a unique and essential reference for the scientific community concerning how conformational-dependent activation is a common phenomenon across many classes of receptors or signaling molecules. It discusses the role of conformational dynamics in leading to signaling bias across different classes of receptors and signaling molecules. By providing a broader view of signaling bias, this resource helps to explain common mechanisms shared across receptor classes and how this can be utilized to elucidate their cellular activity and better understand their therapeutic potential. Written for both new and established scientists in pharmacology, cell biology, biochemistry, and signal transduction, as well as physicians, this book clearly illustrates how biased receptor signaling can be utilized to develop and understand complex pharmacology. Chapters are each focused on a specific class of receptor or other important topic and make use of real-world examples illustrating how the latest research in signal transduction has led to a better understanding of pharmacology and cell biology. This structure creates a basis for understanding that physiological signalling bias has been selected by nature in order to provide complex and tissue- specific biological responses in the face of limited receptors and signaling pathways. This book provides a framework to reveal that these physiological mechanisms are not restricted to one receptor type or family and thus presents receptor signaling from a newer, more global perspective. Offers a unique and valuable resource on biased receptor signaling that provides a global view for better understanding pharmacology across many receptor families Integrates biased receptor signaling, physiology, and pharmacology to place this emerging science within the context of treating disease Includes important chapters on both the pharmaceutical and therapeutic implications of biased signaling

A Pharmacology Primer

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Publisher : Academic Press
ISBN 13 : 0128139587
Total Pages : 488 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis A Pharmacology Primer by : Terry Kenakin

Download or read book A Pharmacology Primer written by Terry Kenakin and published by Academic Press. This book was released on 2018-10-26 with total page 488 pages. Available in PDF, EPUB and Kindle. Book excerpt: A Pharmacology Primer: Techniques for More Effective and Strategic Drug Discovery, Fifth Edition features the latest ideas and research regarding the application of pharmacology to the process of drug discovery. Written by well-respected pharmacologist, Terry P. Kenakin, this primer is an indispensable resource for all those involved in drug discovery. This updated edition has been thoroughly revised to include material on quantifying drug efficacy through bias and cluster analysis, the impact of molecular dynamics and protein structural analysis, the real time kinetic analysis of drug effect, virtual screening for new drug chemical scaffolds, and much more. With full color illustrations and new examples throughout, this book remains a top reference for all industry and academic scientists that is also ideal for students directly involved in drug discovery or pharmacologic research. Highlights changes surrounding strategies for drug discovery, providing a comprehensive reference and featuring advances in the methods involved Includes multiple new sections, such as development and utilization of models in pharmacology, de-orphanization of new drug targets, predicting impact of disease on drug pharmacokinetics, and the impact of enzyme kinetics on drug-drug interactions Illustrates the application of rapid inexpensive assays to predict activity in the therapeutic setting, showing data outcomes and the limitations inherent in interpreting this data

Theranostics and Precision Medicine for the Management of Hepatocellular Carcinoma, Volume 1

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Publisher : Academic Press
ISBN 13 : 0323993648
Total Pages : 388 pages
Book Rating : 4.3/5 (239 download)

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Book Synopsis Theranostics and Precision Medicine for the Management of Hepatocellular Carcinoma, Volume 1 by : Ganji Purnachandra Nagaraju

Download or read book Theranostics and Precision Medicine for the Management of Hepatocellular Carcinoma, Volume 1 written by Ganji Purnachandra Nagaraju and published by Academic Press. This book was released on 2022-02-16 with total page 388 pages. Available in PDF, EPUB and Kindle. Book excerpt: Theranostics and Precision Medicine for the Management of Hepatocellular Carcinoma, Volume One: Biology and Pathophysiology provides comprehensive information about ongoing research and clinical data surrounding liver cancer. The book presents detailed descriptions about diagnostics and therapeutic options for easy understanding, with a focus on precision medicine approaches to improve treatment outcomes. This volume discusses topics such as tumor microenvironment in hepatocellular carcinoma, endoplasmic reticulum stress and unfolded protein response, effects of cirrhosis and hepatitis on the prognosis of HCC, mitochondrial metabolism, next generation sequencing, and telomerase. In addition, it discusses exosomes role in HCC progression, metastasis and chemokines. This is a valuable resource for cancer researchers, oncologists, graduate students, hepathologists and members of biomedical research who need to understand more about liver cancer for their research work or clinical setting. Provides an updated literature review and detailed understanding of liver cancer tumor biology Discusses abnormal changes in the liver caused, resulting from, or associated with hepatocellular carcinoma from a holistic view Presents the content with fully colored images and summarizing tables for easy understanding of complex topics

GPCR Signaling in Cancer

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Publisher : Academic Press
ISBN 13 : 0128202300
Total Pages : 164 pages
Book Rating : 4.1/5 (282 download)

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Book Synopsis GPCR Signaling in Cancer by :

Download or read book GPCR Signaling in Cancer written by and published by Academic Press. This book was released on 2020-03-06 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: GPCR Signaling in Cancer, Volume 145, the latest release in the Advances in Cancer Research series, highlights recent developments in the area of GPCRs and cancer biology. Chapters included in this volume cover several GPCRs and their downstream effectors as case examples to highlight their fundamental understanding and therapeutic potential. Specific chapters address the Role of GRKs and beta-arrestins in cancer, Atypical GPCRs in cancer, the Role of a chemokine receptor (CCR) 5 in cancer, Targeting G protein-coupled receptors for therapeutics in cancer, Emerging GPCR signaling pathways in cancer, and more. G protein-coupled receptors (GPCRs) constitute a large family of cell surface receptors which are involved in nearly every cellular and physiological event. These receptors can recognize a broad array of ligands and they are targeted by nearly one third of the currently prescribed drugs including anti-cancer therapeutics. Covers the latest concepts in GPCR signaling and their relevancy to cancer biology Presents new indications for anti-cancer therapeutic programs Includes sections on cross-talk and signaling networks of GPCRs and effectors in molecular oncology and therapeutics

Structure-Based Drug Design

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Publisher : Routledge
ISBN 13 : 1351413066
Total Pages : 665 pages
Book Rating : 4.3/5 (514 download)

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Book Synopsis Structure-Based Drug Design by : Pandi Veerapandian

Download or read book Structure-Based Drug Design written by Pandi Veerapandian and published by Routledge. This book was released on 2018-03-29 with total page 665 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introducing the most recent advances in crystallography, nuclear magnetic resonance, molecular modeling techniques, and computational combinatorial chemistry, this unique, interdisciplinary reference explains the application of three-dimensional structural information in the design of pharmaceutical drugs. Furnishing authoritative analyses by world-renowned experts, Structure-Based Drug Design discusses protein structure-based design in optimizing HIV protease inhibitors and details the biochemical, genetic, and clinical data on HIV-1 reverse transcriptase presents recent results on the high-resolution three-dimensional structure of the catalytic core domain of HIV-1 integrase as a foundation for divergent combination therapy focuses on structure-based design strategies for uncovering receptor antagonists to treat inflammatory diseases demonstrates a systematic approach to the design of inhibitory compounds in cancer treatment reviews current knowledge on the Interleukin-1 (IL-1) system and progress in the development of IL-1 modulators describes the influence of structure-based methods in designing capsid-binding inhibitors for relief of the common cold and much more!

Biology of Vascular Smooth Muscle: Vasoconstriction and Dilatation

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Publisher : Springer
ISBN 13 : 981104810X
Total Pages : 287 pages
Book Rating : 4.8/5 (11 download)

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Book Synopsis Biology of Vascular Smooth Muscle: Vasoconstriction and Dilatation by : Yuansheng Gao

Download or read book Biology of Vascular Smooth Muscle: Vasoconstriction and Dilatation written by Yuansheng Gao and published by Springer. This book was released on 2017-06-14 with total page 287 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides a concise yet comprehensive review of the morphological, biochemical, electrical, mechanical, and metabolic properties of vascular smooth muscle, the regulation of vascular activities and the intracellular signaling involved. It particularly focuses on recently identified vasoactive agents, enzymes and transduction mechanisms. It also discusses the latest findings in the regulation of cerebral, coronary and pulmonary circulation as well as vascular activity under hypoxia and ageing. The contraction and dilatation activities of vasculature are of fundamental importance for maintaining circulation homeostasis and adapting physiological changes. Over the last four decades, there have been significant advances in our understanding of the biochemical, structural, genetic, physiological, and pharmacological aspects of vascular activity regulation, and these insights into the responsiveness of blood vessels under normal and pathophysiological conditions help to provide valuable weapons in the fight vascular diseases. The book is of interest to researchers and graduate students, both in basic research and in clinic settings, in the field of vascular biology.

GPCRs

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Publisher : Academic Press
ISBN 13 : 0128167289
Total Pages : 500 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis GPCRs by : Beata Jastrzebska

Download or read book GPCRs written by Beata Jastrzebska and published by Academic Press. This book was released on 2019-09-11 with total page 500 pages. Available in PDF, EPUB and Kindle. Book excerpt: GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer’s disease, Parkinson’s disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth. Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology

Allosteric Modulation of G Protein-Coupled Receptors

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Publisher : Academic Press
ISBN 13 : 0128197722
Total Pages : 214 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Allosteric Modulation of G Protein-Coupled Receptors by : Robert Laprairie

Download or read book Allosteric Modulation of G Protein-Coupled Receptors written by Robert Laprairie and published by Academic Press. This book was released on 2022-02-05 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization

Receptor-Receptor Interactions

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Publisher : Springer Science & Business Media
ISBN 13 : 1468454153
Total Pages : 577 pages
Book Rating : 4.4/5 (684 download)

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Book Synopsis Receptor-Receptor Interactions by : Kjell Fuxe

Download or read book Receptor-Receptor Interactions written by Kjell Fuxe and published by Springer Science & Business Media. This book was released on 2013-03-13 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Principles of Endocrinology and Hormone Action

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Publisher : Springer
ISBN 13 : 9783319446745
Total Pages : 0 pages
Book Rating : 4.4/5 (467 download)

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Book Synopsis Principles of Endocrinology and Hormone Action by : Antonino Belfiore

Download or read book Principles of Endocrinology and Hormone Action written by Antonino Belfiore and published by Springer. This book was released on 2018-02-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.

The Metabotropic Glutamate Receptors

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Publisher : Springer Science & Business Media
ISBN 13 : 1475722982
Total Pages : 284 pages
Book Rating : 4.4/5 (757 download)

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Book Synopsis The Metabotropic Glutamate Receptors by : P. Jeffrey Conn

Download or read book The Metabotropic Glutamate Receptors written by P. Jeffrey Conn and published by Springer Science & Business Media. This book was released on 2013-03-09 with total page 284 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Metabotropic Glutamate Receptors offers state-of-the-art summaries and reviews of virtually everything known today about metabotropic glutamate receptors (mGluRs), including their molecular biology, pharmacology, anatomical distribution, and physiological and pathological roles. Illuminating the overall role played by this crucial class of receptors in brain function, the book also pinpoints those areas in which there is the greatest continuing need for focused research. Because mGluRs have the potential for participating in virtually all known functions of the central nervous system (CNS), the opportunity now exists to develop pharmacological agents that can potentially alter many brain disease processes by selective interaction with precise CNS functions. With its critical and insightful reviews, The Metabotropic Glutamate Receptors will immediately become your essential key to the development of novel treatment strategies for the widest variety of neurological disorders.

Encyclopedia of Signaling Molecules

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Publisher : Springer
ISBN 13 : 9781493968008
Total Pages : 6330 pages
Book Rating : 4.9/5 (68 download)

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Book Synopsis Encyclopedia of Signaling Molecules by : Sangdun Choi

Download or read book Encyclopedia of Signaling Molecules written by Sangdun Choi and published by Springer. This book was released on 2017-12-15 with total page 6330 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second edition of this encyclopedia presents over 400 biologically important signaling molecules and the content is built on the core concepts of their functions along with early findings written by some of the world’s foremost experts. The molecules are described by recognized leaders in each molecule. The interactions of these single molecules in signal transduction networks will also be explored. This encyclopedia marks a new era in overview of current cellular signaling molecules for the specialist and the interested non-specialist alike. Currently, there are more than 30,000 genes in human genome. However, not all the proteins encoded by these genes work equally in order to maintain homeostasis. Understanding the important signaling molecules as completely as possible will significantly improve our research-based teaching and scientific capabilities.