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High Density Lipoproteins: From Biological Understanding to Clinical Exploitation

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Book Series: Handbook of Experimental Pharmacology ISSN: 01712004 ISBN: 9783319096643 9783319096650 Year: Volume: 224 Pages: 694 DOI: 10.1007/978-3-319-09665-0 Language: English
Publisher: Springer
Subject: Manufactures --- Electrical and Nuclear Engineering --- Chemical Technology --- Business and Management --- Biotechnology --- Therapeutics --- Medicine (General)
Added to DOAB on : 2015-07-20 15:18:00
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n this Handbook of Experimental Pharmacology on “High Density Lipoproteins – from biological understanding to clinical exploitation” contributing authors (members of COST Action BM0904/HDLnet) summarize in more than 20 chapters our current knowledge on the structure, function, metabolism and regulation of HDL in health and several diseases as well as the status of past and ongoing attempts of therapeutic exploitation.The book is of interest to researchers in academia and industry focusing on lipoprotein metabolism, cardiovascular diseases and immunology as well as clinical pharmacologists, cardiologists, diabetologists, nephrologists and other clinicians interested in metabolic or inflammatory diseases.

The Emerging Discipline of Quantitative Systems Pharmacology

Authors: ---
Book Series: Frontiers Research Topics ISSN: 16648714 ISBN: 9782889196425 Year: Pages: 97 DOI: 10.3389/978-2-88919-642-5 Language: English
Publisher: Frontiers Media SA
Subject: Science (General) --- Therapeutics
Added to DOAB on : 2016-08-16 10:34:25
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In 2011, the National Institutes of Health (NIH), in collaboration with leaders from the pharmaceutical industry and the academic community, published a white paper describing the emerging discipline of Quantitative Systems Pharmacology (QSP), and recommended the establishment of NIH-supported interdisciplinary research and training programs for QSP. QSP is still in its infancy, but has tremendous potential to change the way we approach biomedical research. QSP is really the integration of two disciplines that have been increasingly useful in biomedical research; “Systems Biology” and “Quantitative Pharmacology”. Systems Biology is the field of biomedical research that seeks to understand the relationships between genes and biologically active molecules to develop qualitative models of these systems; and Quantitative Pharmacology is the field of biomedical research that seeks to use computer aided modeling and simulation to increase our understanding of the pharmacokinetics (PK) and pharmacodynamics (PD) of drugs, and to aid in the design of pre-clinical and clinical experiments. The purpose of QSP modeling is to develop quantitative computer models of biological systems and disease processes, and the effects of drug PK and PD on those systems. QSP models allow testing of numerous potential experiments “in-silico” to eliminate those associated with a low probability of success, avoiding the potential costs of evaluating all of those failed experiments in the real world. At the same time, QSP models allow us to develop our understanding of the interaction between drugs and biological systems in a more systematic and rigorous manner. As the need to be more cost-efficient in the use of research funding increases, biomedical researchers will be required to gain the maximum insight from each experiment that is conducted. This need is even more acute in the pharmaceutical industry, where there is tremendous competition to develop innovative therapies in a highly regulated environment, combined with very high research and development (R&D) costs for bringing new drugs to market (~$1.3 billion/drug). Analogous modeling & simulation approaches have been successfully integrated into other disciplines to improve the fundamental understanding of the science and to improve the efficiency of R&D (e.g., physics, engineering, economics, etc.). The biomedical research community has been slow to integrate computer aided modeling & simulation for many reasons: including the perception that biology and pharmacology are “too complex” and “too variable” to be modeled with mathematical equations; a lack of adequate graduate training programs; and the lack of support from government agencies that fund biomedical research. However, there is an active community of researchers in the pharmaceutical industry, the academic community, and government agencies that develop QSP and quantitative systems biology models and apply them both to better characterize and predict drug pharmacology and disease processes; as well as to improve efficiency and productivity in pharmaceutical R&D.

The Physiology and Pharmacology of Leucine-rich Repeat GPCRs

Authors: ---
Book Series: Frontiers Research Topics ISSN: 16648714 ISBN: 9782889199587 Year: Pages: 115 DOI: 10.3389/978-2-88919-958-7 Language: English
Publisher: Frontiers Media SA
Subject: Medicine (General) --- Internal medicine
Added to DOAB on : 2016-01-19 14:05:46
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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 studied. However, within the Class A receptors, sub-families of receptors can be distinguished based upon common sequence motifs within the transmembrane domains as well as extracellular and intracellular domains. One such family of Class A receptors is characterized by multiple leucine- rich repeats within their amino- terminal domains (the Leucine-rich Repeat family (LRR)). This family of GPCRs are best represented by the glycoprotein hormone receptors (LHR, FSHR and TSHR) which have been studied extensively but also includes receptors for the peptide hormone relaxin (RXFP1 and RXFP2 (RXFP2 also binds insulin-like peptide 3)) and three other receptors (LGR4, LGR5 and LGR6). LGR4-6 were, until recently, considered orphan receptors. However, emerging data have revealed that these proteins are the receptors for a family of growth factors called R-spondins. Over the last 20 years much has been learned about LRR receptors, including the development of synthetic agonists and antagonists, new insights into signaling (including signaling bias) and the physiological role these receptors play in regulating the function of many tissues. This topic will focus on what is known concerning the regulation of these receptors, their signaling pathways, functional consequences of activation and pharmacology.

Keywords

GPCR --- Leucine- rich repeat --- LH --- FSH --- TSH --- Relaxin --- R-spondin --- LRR --- Pharmacology

Molecular Pharmacology and Pathology of Strokes

Authors: ---
ISBN: 9783038975410 / 9783038975427 Year: Pages: 152 DOI: 10.3390/books978-3-03897-542-7 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General) --- Therapeutics --- Cardiovascular
Added to DOAB on : 2019-02-11 11:33:53
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Stroke, a progressively non-communicable disease, is the second leading cause of death after coronary heart disease in developed countries. The present treatment options for stroke are adapting lifestyle practices, diabetes treatment, drugs, and the management of other factors, but no cure is yet available, despite new insights into molecular and therapeutic targets. Discoveries related to explicating the molecular pharmacology in cerebrovascular function and thrombosis have led to significant advancements in the current treatment paradigm for patients with stroke. Hence, this Special Issue invited scientific papers and reviews from researchers to provide solid evidence from a molecular point of view to scrutinize the molecular pharmacology and pathology of strokes. Platelet activation plays a major role in cardio and cerebrovascular diseases. Platelets also play a key role in the hemostatic process and are associated with various pathological events, such as arterial thrombosis and atherosclerosis. While the currently used anti-platelet drugs such as aspirin and clopidogrel demonstrate efficacy in many patients, they exert undesirable side effects. Therefore, the development of effective therapeutic strategies for the prevention and treatment of thrombotic diseases is a significant priority. Recently, precious metal drugs have conquered the subject of metal-based drugs, and several investigators have moved their attention to the synthesis of various ruthenium (Ru) and iridium (Ir) complexes due to their prospective therapeutic values. We have published this e-book about the “Molecular Pharmacology and Pathology of Strokes” and anticipate that readers will find this book useful regarding the significant challenges and current advances that are presently being made in stroke research, with the possibility of inspiring the application of novel drug development to enrich the devotion and treatment of patients with cardiovascular diseases.

Simon of Genoa's Medical Lexicon

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ISBN: 9788376560236 Year: Pages: 164 DOI: 10.2478/9788376560236 Language: English
Publisher: De Gruyter
Subject: History
Added to DOAB on : 2014-03-05 13:12:22
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“Simon of Genoa's Medical Lexicon”, an edited volume based on the conference held on March 17th, 2012, is part of the Simon Online project – a dynamically growing Wiki edition of Simon of Genoa's Clavis sanationis, a Latin-Greek-Arabic medical dictionary from the late 13th century. In the individual articles, written by well-known scholars, authorities in their fields of research, Simon and his major work, are approached from different perspectives and as a whole. The volume offers a comprehensible and well-balanced collection of current research on Simon and Clavis sanationis.The volume demonstrates the importance of the Clavis, not only for the history of pharmacology and medicine, but also for Byzantine and medieval studies, Roman, Greek, Latin and Arabic philology and lexicography.Barbara Zipser (Doctor of Philosophy, Wellcome Trust University Award 2006, 2010) is a researcher at the Centre for the Study of the Body and Material Culture, History Department, Royal Holloway University of London. Her main field of research is Greek medicine from Galen to the late Middle Ages, with an emphasis on textual criticism, manuscript transmission, and the formation of Greek vernacular terminology. Dr Zipser is a well-known and promising young scholar in the field of Ancient and Medieval Medicine. She runs Simon Online (http://www.simonofgenoa.org) – the joint edition and translation project of Simon of Genoa's Clavis sanationis, a dictionary of Latin, Greek and Arabic medical terminology in Wiki format.

Computational and Experimental Approaches in Multi-Target Pharmacology

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Book Series: Frontiers Research Topics ISSN: 16648714 ISBN: 9782889452521 Year: Pages: 122 DOI: 10.3389/978-2-88945-252-1 Language: English
Publisher: Frontiers Media SA
Subject: Science (General) --- Therapeutics
Added to DOAB on : 2018-02-27 16:16:44
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The next frontier in pharmacology is the development of multi-target strategies in which pathological processes are controlled by pharmacologically manipulating them at many different points at once. Designing multi-target strategies will require deep understanding of the complex physiology that underlies pathological processes. It will also require the development of single drugs with multiple targets, or combinations of drugs with compatible pharmacokinetics that work synergistically to maximize desirable effects while minimizing unwanted side effects. This e-Book contains ten original articles, each addressing a different aspect of this challenge. Together they open new perspectives and show the way forward in the development of multi-target therapeutics.

Coupled Enzyme Activity and Thermal Shift Screening of the Maybridge Rule of 3 Fragment Library Against Trypanosoma brucei Choline Kinase; A Genetically Validated Drug Target (Book chapter)

Authors: --- ---
ISBN: 9789535109068 Year: DOI: 10.5772/52668 Language: English
Publisher: Intech Grant: Wellcome Trust - 067441
Subject: Medicine (General)
Added to DOAB on : 2019-01-17 11:47:01
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In this study we interrogate 630 compounds of the Maybridge Rule of 3 Fragment Library for compounds that interact with, and inhibit TbCK. The Maybridge Rule of 3 Fragment Library is a small collection of quantifiable diverse, pharmacophoric rich, chemical entities that comply with the following criteria; MW ≤ 300, cLogP ≤ 3, H-Bond Acceptors ≤ 3, H-Bond Donors ≤ 3, Rotatable bonds (Flexibility Index) ≤ 3, Polar Surface Area ≤ 60 Å2 and aqueous solubility ≥ 1 mM using LogS and high purity (≥ 95%). Comparisons between two different screening methods, a coupled enzyme activity assay and differential scanning fluorimetry, has allowed identification of compounds that interact and inhibit the T. brucei choline kinase, several of which possess selective trypanocidal activity. Screening of a comparatively small fragment library by two different screening methods has allowed identification of several compounds that interact with and inhibit TbCK, a genetically validated drug target against African sleeping sickness. Some of the inhibitory fragments were also selectively trypanocidal, considering these are relatively simple molecules with no optimization, finding low μΜ inhibitors is very encouraging. Moreover some of the morphological phenotypes of these trypanocidal compounds include cell-cycle arrests similar to those observed for the TbCK conditional knockout grown under permissive conditions.

Keywords

pharmacology --- toxicology

Molecular and Biotechnological Advancements in Hypericum Species

Authors: --- ---
Book Series: Frontiers Research Topics ISSN: 16648714 ISBN: 9782889451173 Year: Pages: 159 DOI: 10.3389/978-2-88945-117-3 Language: English
Publisher: Frontiers Media SA
Subject: Science (General) --- Botany
Added to DOAB on : 2017-07-06 13:27:36
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Hypericum is an important genus of the family Hypericaceae and includes almost 500 species of herbs, shrubs and trees. Being the home for many important bioactive compounds, these species have a long traditional value as medicinal plants. Currently, several species of this genus have been used in ailments as knowledge-based medicine in many countries. In the recent past, several pharmacological studies have been performed using crude extracts to evaluate the traditional knowledge. Results of those studies have revealed that Hypericum extract exert multiple pharmacological properties including antidepressant, antimicrobial, antitumor and wound healing effects. Phytochemical analyses revealed that these species produce a broad spectrum of valuable compounds, mainly naphthodianthrones (hypericin and pseudohypericin), phloroglucinols (hyperforin and adhyperforin), flavonoids (hyperoside, rutin and quercitrin), benzophenones/xanthones (garcinol and gambogic acid), and essential oils. Noticeably, Hypericum perforatum extracts have been used to treat mild to moderate depression from ancient to present times and the antidepressant efficacy of Hypericum extracts has been attributed to its hyperforin content, which is known to inhibit the re-uptake of aminergic transmitters such as serotonin and noradrenaline into synaptic nerve endings. Neurodegenerative diseases and inflammatory responses are also linked with Reactive Oxygen Species (ROS) production. A wide range of flavonoids present in Hypericum extracts, namely, rutin, quercetin, and quercitrin exhibit antioxidant/free radical scavenging activity. Hypericin, beside hyperforin, is the active molecule responsible for the antitumor ability of Hypericum extracts and is seen as a potent candidate to treat brain tumor. Recent attempts of using hypericin in patients with recurrent malignant brain tumors showed promising results. Collectively, Hypericum species contain multiple bioactive constituents, suggesting their potential to occupy a huge portion of the phytomedicine market. Today, studies on medicinal plants are rapidly increasing because of the search for new active molecules, and for the improvement in the production of plants and molecules for the herbal pharmaceutical industries. In the post genomic era, application of molecular biology and genomic tools revolutionized our understanding of major biosynthetic pathways, phytochemistry and pharmacology of Hypericum species and individual compounds. This special issue mainly focuses on the recent advancements made in the understanding of biosynthetic pathways, application of biotechnology, molecular biology, genomics, pharmacology and related areas.

Mind the gap! Gap junction channels and their importance in pathogenesis

Authors: --- ---
Book Series: Frontiers Research Topics ISSN: 16648714 ISBN: 9782889192380 Year: Pages: 252 DOI: 10.3389/978-2-88919-238-0 Language: English
Publisher: Frontiers Media SA
Subject: Neurology --- Medicine (General) --- Therapeutics --- Science (General)
Added to DOAB on : 2015-11-16 15:44:59
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"Cells live together, but die singly", this sentence wrote the German physiologist Theodor Engelmann in 1875 and although he had no particular knowledge of gap junction channels (their structure was discovered around 100 years later) he described their functions very well: gap junction channels are essential for intercellular communication and crucial for the development of tissue and organs. But besides providing an opportunity for cells to communicate gap junction channels might also prevent intercellular communication by channel closure thereby preserving the surrounding healthy tissue in case of cellular necrosis. According to today’s understanding gap junction channels play an important role during embryonic development, during growth, wound healing and cell differentiation and are also involved in the process of learning. In the past decades most intensive research was done not only to unravel the physiological role of gap junction channels but also to extend our knowledge of the contribution of these channels in pathogenesis. A new frontier emerges in the field "pharmacology of gap junctions" with the aim to control growth, differentiation, or electrical coupling via targeting gap junction channels pharmacologically. As we know today disturbances in gap junction synthesis, assembly and cellular distribution may account for various organic disorders from most different medical fields, such as the Charcot-Marie-Tooth neuropathy, epilepsy, Chagas-disease, Naxos-syndrome, congenital cardiac malformations, arrhythmias, cancer and as a very common disease in industrial countries atherosclerosis. Point mutations in gap junction channels have been found to cause hereditary diseases like the congenital deafness or the Charcot-Marie-Tooth neuropathy but the exact molecular mechanisms of gap junction malfunction from most of the mentioned illnesses are not fully understood. Moreover, in the last few years research has expanded on the role and function of connexin hemichannels and on a relatively new field the pannexins. The purpose of this volume is to give a comprehensive overview of the involvement of gap junction channels, hemichannels and pannexins on pathogenesis of inborn and acquired diseases and on emerging pharmacological strategies to target these channels. We welcome our colleagues to contribute their findings on the influence of gap junctions on pathogenesis and to unravel the secrets of intercellular communication. Take the lid off!

Biological Activity of Natural Secondary Metabolite Products

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ISBN: 9783038971740 9783038971757 Year: Pages: 466 DOI: 10.3390/books978-3-03897-175-7 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Anthropology --- Biology --- Social and Public Welfare
Added to DOAB on : 2018-09-20 12:02:36
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ca. 200 words; this text will present the book in all promotional forms (e.g. flyers). Please describe the book in straightforward and consumer-friendly terms.[Natural secondary metabolite products, which are isolated from plants, animals, microorganisms, etc., are classified as polyketides, isoprenoids, aromatics (phenylpropanoids), alkaloids, etc. Their chemical diversity and variety of biological activities have attracted the attention of chemists, biochemists, biologists, etc. The Special Issue on "Biological Activity of Natural Secondary Metabolite Products" is intended to offer biological active natural products as candidates and/or leads for pharmaceuticals, dietary supplements, functional foods, cosmetics, food additives, etc. The research fields of this Special Issue include natural products chemistry, phytochemistry, pharmacognosy, food chemistry, bioorganic synthetic chemistry, chemical biology, molecular biology, molecular pharmacology, and other related research fields of bioactive natural secondary metabolite products. Original research and review articles on all topics in these research fields are invited. I am looking forward to receiving many submissions from outstanding experts in these research fields.]

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