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Gpr37 Adenosine A2a Receptor Receptor Interaction As A New Pharmacological Target For Parkinsons Disease Treatment
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Book Synopsis GPR37-ADENOSINE A2A Receptor-receptor Interaction as a New Pharmacological Target for Parkinson's Disease Treatment by : Xavier Morató Arús
Download or read book GPR37-ADENOSINE A2A Receptor-receptor Interaction as a New Pharmacological Target for Parkinson's Disease Treatment written by Xavier Morató Arús and published by . This book was released on 2017 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Novel Therapeutic Approaches to the Treatment of Parkinson’s Disease by : Corey R. Hopkins
Download or read book Novel Therapeutic Approaches to the Treatment of Parkinson’s Disease written by Corey R. Hopkins and published by Springer. This book was released on 2016-06-23 with total page 158 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
Book Synopsis The Adenosinergic System by : Micaela Morelli
Download or read book The Adenosinergic System written by Micaela Morelli and published by Springer. This book was released on 2015-10-01 with total page 344 pages. Available in PDF, EPUB and Kindle. Book excerpt: Adenosine A2A receptor antagonists have shown great promise in the treatment of Parkinson's Disease and alleviation of symptoms. This book addresses various aspects of this class of drugs from their chemical development to their clinical use. Among the many insightful chapters contained in this book, there are three unique reviews that have not previously been published in any format: (1) a history of istradefylline, the first A2A antagonist approved for treatment of Parkinson's Disease, (2) an overview of neuroimaging studies in human death and disease and (3) a study of urate as a possible biomarker and neuroprotectant.
Book Synopsis Investigations of Adenosine A2A Receptor Antagonists, Dopamine D2 Receptor Agonists and Dual Acting Ligands for the Treatment of Parkinson's Disease by : Manuela Jorg
Download or read book Investigations of Adenosine A2A Receptor Antagonists, Dopamine D2 Receptor Agonists and Dual Acting Ligands for the Treatment of Parkinson's Disease written by Manuela Jorg and published by . This book was released on 2014 with total page 490 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this project, the adenosine A2A receptor and the dopamine D2 receptor were studied as potential targets for the treatment of Parkinson's disease. Investigated were both targets individually as well as the approach to target both receptors simultaneously with just one single molecule.Herein, present is the synthesis, characterization and pharmacological evaluation of the literature compound ZM 241385 and a series of structurally related adenosine A2A receptor antagonists. Further determined was a chemically and biologically suitable attachment position for linkers on the parent pharmacophores. From this research a triazolotriazine carboxylic acid congener with inhibitory potency equivalent to ZM 241385 has been established, allowing further functionalization towards the extracellular space of the adenosine A2A receptor. At the dopamine D2 receptor, a chemically and biologically suitable attachment position on the chemical structure of the dopamine D2 receptor agonist ropinirole was determined, allowing the development of an oxindole carboxylic acid and an oxindole amine congener. Based on these results a series of homobivalent ligands was synthesized, characterized and pharmacologically evaluated. The homobivalent ligands with a spacer length of 22 to 30 atoms exhibited up to an 80-fold increase in potency compared to the parent molecule ropinirole. Docking of the synthesized molecules in a dopamine D2 receptor dimer model indicated that the increase in potency of the homobivalent ligands was most likely due to an additional allosteric interaction and very unlikely due to interactions at two orthosteric sites across a homodimer. The research results from targeting each receptor individually formed the pillars for the synthesis, characterization and pharmacological evaluation of our dual acting ligands targeting the dopamine D2 and adenosine A2A receptors with just one molecule. A library of compounds ranging from classical heterobivalent ligands to more drug-like merged molecules was synthesized. The most encouraging higher integrated "drug-like" molecules exhibited promising initial blood-brain barrier permeability results and maintained similar EC50 values to the dopamine D2 receptor agonist ropinirole but showed a slight decrease in inhibitory potency compared to the adenosine A2A receptor antagonist ZM 241385. Conversely, the pharmacological evaluation of the dual acting ligands revealed that the most potent classical heterobivalent ligands showed comparable affinities to both original pharmacophores.
Book Synopsis The Adenosine Receptors by : Pier Andrea Borea
Download or read book The Adenosine Receptors written by Pier Andrea Borea and published by Humana Press. This book was released on 2018-07-28 with total page 603 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book traces the history of adenosine receptor research from molecular biology to medicinal chemistry to behavior, including their implications in disease and potential strategies as therapeutic targets. It provides the reader with a comprehensive overview of the adenosine receptors that includes information on all subtypes - A1, A2A, A2B and A3. Aspects addressed include the most up to date information on their functional distribution in the nervous and peripheral systems, behavioral roles in inflammation, cancer, pain and neurological diseases such as Huntington’s disease, Epilepsy, Parkinson’s disease and Alzheimer’s disease.
Book Synopsis Women in Experimental Pharmacology and Drug Discovery Pharmacology 2023 by : Patricia Rijo
Download or read book Women in Experimental Pharmacology and Drug Discovery Pharmacology 2023 written by Patricia Rijo and published by Frontiers Media SA. This book was released on 2024-07-24 with total page 147 pages. Available in PDF, EPUB and Kindle. Book excerpt: At present, according to UNESCO, less than 30% of researchers worldwide are women. Long-standing biases and gender stereotypes are discouraging girls and women away from science-related fields, and STEM research in particular. Science and gender equality are, however, essential to ensure sustainable development as highlighted by UNESCO. In order to change traditional mindsets, gender equality must be promoted, stereotypes defeated, and girls and women should be encouraged to pursue STEM careers.
Book Synopsis Computational Methods for GPCR Drug Discovery by : Alexander Heifetz
Download or read book Computational Methods for GPCR Drug Discovery written by Alexander Heifetz and published by Humana Press. This book was released on 2017-11-30 with total page 436 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume looks at modern computational strategies and techniques used in GPCR drug discovery including structure and ligand-based approaches and cheminformatics. The chapters in this book describe how these approaches can be applied to address key drug discovery issues, such as receptor structure modelling, function and dynamics, prediction of protein-water-ligand interactions and binding kinetics, free energy of binding, interconversion between agonists and antagonists, deorphanization of GPCRs, and the discovery of biased and allosteric modulators. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modelling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique,Computational Methods for GPCR Drug Discovery is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists, and drug designers.
Book Synopsis GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity by : Denis J. Dupré
Download or read book GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity written by Denis J. Dupré and published by Springer Science & Business Media. This book was released on 2012-11-19 with total page 298 pages. Available in PDF, EPUB and Kindle. Book excerpt: Main Question: G protein coupled receptors are involved in highly efficient and specific activation of signalling pathways. How do GPCR signalling complexes get assembled to generate such specificity? In order to answer this question, we need to understand how receptors and their signalling partners are synthesized, folded and quality-controlled in order to generate functional proteins. Then, we need to understand how each partner of the signalling complex is selected to join a complex, and what makes this assembly possible. GPCRs are known to be able to function as oligomers, what drives the assembly into oligomers and what will be the effects of such organization on specificity and efficacy of signal transduction. Once the receptor complexes are assembled, they need to reach different locations in the cell; what drives and controls the trafficking of GPCR signalling complexes. Finally, defects in synthesis, maturation or trafficking can alter functionality of GPCRs signalling complexes; how can we manipulate the system to make it function normally again? Pharmacological chaperones may just be part of the answer to this question.
Book Synopsis GPCRs: From Deorphanization to Lead Structure Identification by : H. Bourne
Download or read book GPCRs: From Deorphanization to Lead Structure Identification written by H. Bourne and published by Springer Science & Business Media. This book was released on 2007-07-03 with total page 275 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Book Synopsis Receptor and Ion Channel Detection in the Brain by : Rafael Luján
Download or read book Receptor and Ion Channel Detection in the Brain written by Rafael Luján and published by Humana. This book was released on 2016-02-02 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Receptor and Ion Channel Detection in the Brain provides state-of-the-art and up-to-date methodological information on molecular, neuroanatomical and functional techniques that are currently used to study neurotransmitter receptors and ion channels in the brain. The chapters have been contributed by world-wide recognized neuroscientists who explain in an easy and detailed way well established and tested protocols embracing molecular, cellular, subcellular, anatomical and electrophysiological aspects of the brain. This comprehensive and practical manual is presented in a simple, step-by-step manner for laboratory use, and also offers unambiguous detail and key implementation advice that proves essential for successful results and facilitate choosing the best method for the target proteins under study. This work serves as a useful guide for young researchers and students in training as well as for neurologists and established scientists who wish to extend their repertoire of techniques.
Book Synopsis Neurotransmitter Transporters by : Maarten E. A. Reith
Download or read book Neurotransmitter Transporters written by Maarten E. A. Reith and published by Springer Science & Business Media. This book was released on 2002 with total page 540 pages. Available in PDF, EPUB and Kindle. Book excerpt: Neurotransmission is a multicomponent process. Transmitters, released by neuronal activity, act on pre- and postsynaptic receptors, and many books detail advances in the receptor field. In addition, after their release from nerve endings, transmitters are removed from the neuronal vicinity by uptake into neuronal or glial cells by specific tra- porter proteins that have been studied intensely over the last 30 years; this information is scattered throughout numerous publishing vehicles. Therefore, the primary aim of this second edition of N- rotransmitter Transporters: Structure, Function, and Regulation is to offer a comprehensive picture of the characterization of neurotransmitter transporters and their biological roles. The transporter field has moved forward in stages. In the first phase, progress came from the use of substrate or blocker ligands selectively targeting transporters, the application of model systems allowing the study of transmitter tra- port shielded from storage, and the development of mathematical models for describing transport phenomena. In the second phase, roughly covering the last decade, advances in DNA techniques allowed the cloning of numerous genes coding for different transporter proteins. In the current, third stage, a wealth of information is being accumulated in studies relating transporter structure with function, experiments addressing regulation by posttranslational transfor- tion, investigations into transport modulation by trafficking processes and genomic influences, characterization of channel properties of tra- porters by electrophysiological approaches, and the creation of transgenic animals under- or overexpressing a given transporter protein.
Book Synopsis Latest Advances on Excitatory Synapse Biology by : Kimberly M. Huber
Download or read book Latest Advances on Excitatory Synapse Biology written by Kimberly M. Huber and published by Frontiers Media SA. This book was released on 2021-11-25 with total page 195 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Structure and Function of GPCRs by : Guillaume Lebon
Download or read book Structure and Function of GPCRs written by Guillaume Lebon and published by Springer. This book was released on 2019-08-01 with total page 289 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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 measure GPCR signaling or to trace their dynamics in cells upon ligand activation. Taken together, the chapters provide an essential overview and toolkit for new scientific investigators who plan to develop GPCR projects. All chapters were written by experts in their respective fields, and share valuable insights and powerful methodologies for the GPCR field.
Book Synopsis Co-Immunoprecipitation Methods for Brain Tissue by : Yuji Odagaki
Download or read book Co-Immunoprecipitation Methods for Brain Tissue written by Yuji Odagaki and published by Humana Press. This book was released on 2019-02-04 with total page 166 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume covers various aspects of co-immunoprecipitation (co-IP) methods and its relevant use in studying protein-protein interactions (PPIs) in health and diseases of the Central Nervous System. The chapters in this book discuss topics such as using co-IP to detect G protein-coupled receptors (GPCR), receptor tyrosine kinases (RTK) and ion channels heteroreceptor complexes in brain tissue; the histoblot technique; interaction strength between synaptic proteins using COS-7; and co-IP analysis of the protein-protein interactions in the neurons of Polymita. In Neuromethods series style, chapters include the kind of detail and key advice from the specialists needed to get successful results in your laboratory. Cutting-edge and thorough, Co-Immunoprecipitation Methods for Brain Tissue is a valuable resource for any researcher interesting in learning more about this developing field.
Book Synopsis Parkinson's Disease and Related Disorders by : Peter Riederer
Download or read book Parkinson's Disease and Related Disorders written by Peter Riederer and published by Springer Science & Business Media. This book was released on 2006-11-23 with total page 484 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book gives a comprehensive overview on current clinical and basic research issues related to Parkinson’s disease and its related disorders. The book is the result of the 16th International Congress of Parkinson’s Disease and Related disorders congress 2005. Its contents are suitable for neurologists, psychiatrists, neurosurgeons, basic researchers, geneticians and patients as well as their relatives.
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:
Book Synopsis Receptor Binding Techniques by : Anthony P. Davenport
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.
