GPCRs From Deorphanization to Lead Structure Identification

• Author : H. Bourne,Richard Horuk,J. Kuhnke,H. Michel
• Publisher : Springer Science & Business Media
• Release : 23 May 2007

This book offers an insight into the approaches taken by industry and academia to address GPCRs and depict how mature this target class-oriented research has become in the last decade. Coverage also reflects the actual trends in the fast-emerging field of GPCR research in academia and industry. It is based on the international workshop GPCRs: From Deorphanisation to Lead Structure Identification, held in Berlin in May 2006.

• Author : Beata Jastrzebska,Paul S.-H. Park
• Publisher : Academic Press
• Release : 11 September 2019

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

• Author : Andrea Strasser,Hans-Joachim Wittmann
• Publisher : Springer Science & Business Media
• Release : 13 August 2012

G protein coupled receptors (GPCRs) comprise an important protein family, which is involved in signal transduction in the cell. Besides that a large number of drugs, available on market, address GPCRs. For an efficient and improved development of appropriate drugs, molecular modelling of GPCRs is – in order to understand the ligand-receptor interactions and functionality of GPCRs on molecular level - an important tool. The book “Modelling of GPCRs – a practical handbook” is focussed onto a practical introduction into molecular modelling

• Author : Jae Young Seong,Hubert Vaudry
• Publisher : Frontiers E-books
• Release : 07 November 2014

The human genome encompasses ˜ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic was to assemble a series of

• Author : Annette Gilchrist
• Publisher : John Wiley & Sons
• Release : 19 September 2022

A thorough discussion of the structure, pharmacology, function, and role of G protein-coupled receptors In GPCRs as Therapeutic Agents, distinguished researcher Dr. Annette Gilchrist delivers an authoritative and in-depth compendium of a vibrant and active area of academic and industrial drug discovery. The book serves as an important reference for new and experienced researchers studying G protein-coupled receptors and discusses the molecular pharmacology of this important target class. It also includes up-to-date material on GPCR structures and structure-based drug design.

• Author : Guillaume Lebon
• Publisher : Springer
• Release : 01 August 2019

This book introduces readers to the latest advances in G protein-coupled receptor (GPCR) biology. It reviews our current understanding of the structural basis of ligand binding and allosteric mechanisms, following a decade of technological breakthroughs. Several examples of structure-based drug discovery are presented, together with the future challenges involved in designing better drugs that target GPCRs. In turn, the book illustrates the important concept of GPCR biased signaling in physiological contexts, and presents fluorescent- and light-based methodologies frequently used to

• Author : Simon Yona,Martin Stacey
• Publisher : Springer Science & Business Media
• Release : 26 June 2011

Upon completion of the human genome project over 800 G protein-coupled receptor 1 (GPCR) genes, subdivided into five categories, were identified. These receptors sense a diverse array of stimuli, including peptides, ions, lipid analogues, light and odour, in a discriminating fashion. Subsequently, they transduce a signal from the ligand–receptor complex into numerous cellular responses. The importance of GPCRs is further reflected in the fact that they constitute the most common target for therapeutic drugs across a 2 wide range of human disorders.

• Author : Dominique Massotte
• Publisher : Frontiers Media SA
• Release : 07 October 2015

G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them

• Author : Senthilkumar Rajagopal,Murugavel Ponnusamy
• Publisher : Springer
• Release : 19 November 2018

This book will provide current understandings about two ubiquitously expressed metabotropic GPCRs, G-coupled purinoreceptor type 2 (P2Y) and Takeda G-protein-coupled bile acid receptor 5 (TGR5). G protein coupled receptors (GPCRs) are the largest family of proteins implicated in majority of cellular responses. The two receptor sub-families play a central role in many physiological functions as well as in many pathological conditions. This book offers up-to-date information on the physiological functions, signaling pathways and regulatory mechanisms of P2Y and TGR5 receptors.

• Author : Guangyu Wu
• Publisher : Academic Press
• Release : 05 June 2015

G protein-coupled receptors (GPCRs) constitute the largest superfamily of cell surface receptors that regulate a variety of cell functions. Over the past few decades great progress has been made in defining the roles of intracellular trafficking in controlling the functionality of the receptors as well as in the development of various human diseases. This volume of Progress in Molecular Biology and Translational Science reviews the recent understanding of GPCR trafficking regulators and molecular mechanisms. Written by future leaders in the

• Author : Brian J. Arey,James A. Dias
• Publisher : Frontiers Media SA
• Release : 05 August 2016

G protein-coupled receptors (GPCRs) represent a large and physiologically important class of cell surface receptors. There are approximately 750 known GPCRs present in the human genome that can be subdivided into general classes based upon sequence homology within their transmembrane domains. Therapeutically, GPCRs represent a fertile source for the development of therapies as they are a significant percentage of our current pharmacopeia. Among the three subclasses of GPCRs, the Class A (rhodopsin-like) receptors are by far the most prevalent and extensively

• Author : Didier Rognan,Raimund Mannhold,Hugo Kubinyi,Gerd Folkers
• Publisher : John Wiley & Sons
• Release : 10 March 2006

1. G protein-coupled receptors in the human genome -- 2. Why G protein-coupled receptors databases are needed -- 3. A novel drug screening assay for G protein-coupled receptors -- 4. Importance of GPCR dimerization for function : the case of the class C GPCRs -- 5. Molecular mechanisms of GPCR activation -- 6. Allosteric properties and regulation of G protein-coupled receptors -- 7. Chemogenomics approaches to ligand design -- 8. Strategies for the design of pGPCR-targeted libraries -- 9. Ligand-based rational design : virtual screening -- 10. 3-D structure of G protein-coupled

• Author : Sameer Mohammad,Muheeb Beg,Manveen Kaur Gupta
• Publisher : Frontiers Media SA
• Release : 28 January 2022

• Author : Kevin R. Lynch
• Publisher : John Wiley & Sons
• Release : 10 May 1999

The past decade has seen tremendous advances in the study of G protein-coupled receptors (GPCRs), including the molecular cloning and identification of more than 100 hundred GPCR genes. But while GPCRs serve as targets for more than 300 medicines in the modern pharmacopoeia, the shrinking pool of known ligands and the continuing discovery of orphan GPCR genes have underscored the need for new approaches to ligand identification. Identification and Expression of G Protein-Coupled Receptors addresses this new direction in GPCR biochemistry-offering a

• Author : Gabriel Berstein
• Publisher : CRC Press
• Release : 24 April 2019

Covering recently developed methods in membrane-bound receptors, this book emphasizes receptor structure and function, knowledge of which is essential to the study of signal transduction. G Protein-Coupled Receptors has culled contributors from domestic and international sources, providing a broad base of knowledge. Some topics covered are the r