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Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts

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ISBN: 9783038426387 9783038426394 Year: Pages: VI, 250 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Therapeutics
Added to DOAB on : 2018-06-22 11:29:17
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The year 2017 marks the 20th anniversary of the molecular cloning of the long sought-after capsaicin receptor, now known as TRPV1 (Transient Receptor Potential Vanilloid 1). This seminal discovery has opened up a “hot” new field of basic research and launched drug discovery efforts into the large family (by the latest count, 28 mammalian members and 27 in humans) of TRP ion channels. Indeed, it took less than a decade for the first potent, small molecule TRPV1 antagonists to enter phase 1 clinical trials, closely followed by TRPA1 and TRPM8 antagonists. The literature on TRP channels is immense. TRPV1 alone is a keyword in over 5000 publications searchable in PubMed. Clearly, it is not possible to capture the entire literature in a single thematic issue. Consequently, the selection of articles presented in this book represents a sampling of the literature, and is admittedly subjective. We tried to survey the wide range of human diseases in which TRP channels have been implicated, ranging from chronic pain through asthma and diabetes to cancer, and highlight the channels that appear to hold the greatest promise for therapeutic targeting. With this book, we hope to convince readers that TRP channels constitute a formidable family of potential therapeutic targets that will likely continue to demand attention.

TRP Channels in Health and Disease

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ISBN: 9783039210824 9783039210831 Year: Pages: 266 DOI: 10.3390/books978-3-03921-083-1 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General)
Added to DOAB on : 2019-06-26 08:44:07
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Almost 25 years ago, the first mammalian transient receptor potential (TRP) channel was cloned and published. TRP channels now represent an extended family of 28 members fulfilling multiple roles in the living organism. Identified functions include control of body temperature, transmitter release, mineral homeostasis, chemical sensing, and survival mechanisms in a challenging environment. The TRP channel superfamily covers six families: TRPC with C for “canonical”, TRPA with A for “ankyrin”, TRPM with M for “melastatin”, TRPML with ML for “mucolipidin”, TRPP with P for “polycystin”, and TRPV with V for “vanilloid”. Over the last few years, new findings on TRP channels have confirmed their exceptional function as cellular sensors and effectors. This Special Book features a collection of 8 reviews and 7 original articles published in “Cells” summarizing the current state-of-the-art on TRP channel research, with a main focus on TRP channel activation, their physiological and pathophysiological function, and their roles as pharmacological targets for future therapeutic options.

Keywords

ion channel --- TRPC --- small molecules --- calcium --- chemical probes --- TRPV1 --- TRPV2 --- TRPV3 --- TRPV4 --- mucosal epithelium --- ulcerative colitis --- inflammatory bowel disease --- TRPM4 channel --- cardiovascular system --- physiology --- pathophysiology --- TRPC6 --- elementary immunology --- inflammation --- calcium --- sodium --- neutrophils --- lymphocytes --- endothelium --- platelets --- human medulla oblongata --- cuneate nucleus --- dorsal column nuclei --- TRPV1 --- calcitonin gene-related peptide --- substance P --- TRP channels --- calcium signaling --- salivary glands --- xerostomia --- radiation --- inflammation --- transient receptor potential channels --- TRPC3 pharmacology --- channel structure --- lipid mediators --- photochromic ligands --- transient receptor potential --- TRPC3 --- mGluR1 --- GABAB --- EPSC --- Purkinje cell --- cerebellum --- toxicology --- TRP channels --- organ toxicity --- chemicals --- pollutants --- chemosensor --- TRPM7 --- kinase --- inflammation --- lymphocytes --- calcium signalling --- SMAD --- TH17 --- hypersensitivity --- regulatory T cells --- thrombosis --- graft versus host disease --- 2D gel electrophoresis --- AP18 --- HEK293 --- HSP70 --- MALDI-TOF MS(/MS) --- nanoHPLC-ESI MS/MS --- proteomics --- sulfur mustard --- TRPA1 --- TRPC channels --- diacylglycerol --- TRPC4 --- TRPC5 --- NHERF --- TRP channel --- TRPY1 --- Saccharomyces cerevisiae --- calcium --- manganese --- oxidative stress --- ion channels --- overproduction --- production platform --- protein purification --- Saccharomyces cerevisiae --- sensors --- transient receptor potential (TRP) channels --- yeast --- adipose tissue --- bioavailable --- menthol --- topical --- TRPM8 --- n/a

Electrospun and Electrosprayed Formulations for Drug Delivery

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ISBN: 9783038979128 9783038979135 Year: Pages: 190 DOI: 10.3390/books978-3-03897-913-5 Language: English
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General) --- Therapeutics
Added to DOAB on : 2019-06-26 10:09:00
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This book is comprised of important reviews and cutting-edge original research papers concerning electrospun and electrosprayed formulations in drug delivery. Electrospinning and electrospraying have, in recent years, attracted increasing attention in the pharmaceutical sector, with research in the area advancing rapidly. It is now possible to prepare extremely complex systems using multi-fluid processes, and to increase production rates to an industrial scale. Electrospun formulations can be produced under GMP conditions and are in clinical trials. In this volume, we explore a range of topics around electrospinning and electrospraying in controlled drug delivery. Four reviews cover the exciting potential of cyclodextrin-containing fibers and the many potential biomedical applications of electrospun fibers. The use of electrospinning to prepare amorphous systems and improve the dissolution rate and solubility of poorly soluble active ingredients is addressed, and the possibilities of such materials in tissue engineering are comprehensively covered. The six original research papers cover the effect of molecular properties on API release from Eudragit-based electrospun fibers; ferulic acid solid dispersions; electrospun medicines to treat psoriasis; scale up of electrospinning and its use to produce low-dose tablets; transepithelial permeation of drugs released from electrospun fibers, and the possibilities for the synergistic chemophotothermal treatment of cancer.

Natural Products and Drug Discovery

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ISBN: 9783039287468 / 9783039287475 Year: Pages: 392 DOI: 10.3390/books978-3-03928-747-5 Language: eng
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Science (General) --- Biology
Added to DOAB on : 2020-06-09 16:38:57
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Natural products hold a prominent position in the current discovery and development of drugs and have diverse indications for both human and animal health. Plants, in particular, play a leading role as a source of specialized metabolites with medical effects. Other organisms, such as marine and terrestrial animals and microorganisms, produce very important drug candidate molecules. Specialized metabolites from these varied natural sources can be used directly as bioactive compounds or drug precursors. In addition, due to their broad chemical diversity, they can act as drug prototypes and/or be used as pharmacological tools for different targets. Some examples of natural metabolites that have been developed into useful medical drug are cardiotonic digoxin from Digitalis sp., antimalarial artemisinin from Artemisia annua, anti-cancer taxol from Taxus sp., or podophyllotoxin from Podophyllum peltatum, which served as a synthetic model for the anti-cancer etoposide. The study of natural products is still attracting great scientific attention and their current importance, as a valuable lead for drug discovery, is undebatable. I cordially invite authors to contribute original articles, as well as survey articles, that give the readers of Molecules **MOLECULES NEEDS TO BE ITALICIZED** updated and new perspectives on natural products in drug discovery, including but not limited to natural sources, identification and separation of bioactive phytochemicals, standardization, new biological targets, pre-clinical and clinical trials, pharmacological effects/side effects, and bioassays.

Keywords

cytotoxicity-guided --- phenolic derivatives --- Dryopteris fragrans --- chemical derivatization --- immuno-regulation activity --- Imperata cylindrica --- HPLC --- ESI-MS/MS --- growth inhibitory activity --- cancer --- cardamonin --- antinociceptive --- TRPV1 --- glutamate --- opioid --- siphonous green algae --- sulfated coumarins --- Dasycladus vermicularis --- isolation and quantification --- Orobanche s.l. --- Orobanchaceae --- Lamiales --- natural products --- secondary metabolites --- phenylpropanoid glycosides --- phenylethanoid glycosides --- bioactivities of natural products --- chemosystematics --- FSE --- T2DM --- GLUT4 --- Ca2+ --- L6 cell --- marine peptides --- proliferation --- migration --- angiogenesis --- zebrafish --- antioxidant activity --- flavonoids --- isoflavones --- phenolics --- proanthocyanidins --- Trifolium --- Leea indica --- HPLC-ESI-microTOF-Q-MS/MS --- phenolics --- dihydrochalcones --- Humulus lupulus --- prenylated phenolic compounds --- antimicrobial agents --- methicillin-resistant Staphylococcus aureus --- Leishmania mexicana mexicana --- Trypanosoma brucei brucei --- Astragalus boeticus L. --- spectroscopic analysis --- cytotoxic activity --- human colon cancer cell lines --- acetylated astragalosides --- Fabaceae --- aging --- cancer --- cardiovascular disease --- dementia --- diabetes --- inflammation --- oxidative stress --- Harpagophytum procumbens --- devil’s claw --- harpagoside --- spagyric tincture --- antioxidant activity --- Cleistocalyx operculatus --- 2?,4?-dihydroxy-6?-methoxy-3?,5?-dimethylchalcone (DMC) --- pPancreatic cancer --- PANC-1 --- ACE inhibitory peptide --- antihypertensive --- bioactive peptides --- hypertension --- marine resources --- terpenes --- terpenoids --- antimicrobial resistance --- synergy --- Phyllanthus orbicularis --- C-glycoside --- flavonoid --- natural products --- traditional medicine --- Cuba --- Phyllanthus chamacristoides --- chromatography --- mass spectrometry --- NMR --- circular dichroism --- stereochemistry --- Fideloside --- cytokines --- anti-inflammatory activity --- metabolomics --- multivariate data analysis --- molecular network --- Bacopa monnieri --- LC-MS --- diabetic neuropathy --- neuropathic pain --- glucosinolates --- Eruca sativa --- glucoerucin --- H2S --- Kv7 potassium channels --- artemisinin --- Physcomitrella patens --- sesquiterpenoids --- malaria --- biotechnology --- ketamine --- psychosis --- cerebellum --- celastrol --- oxidative stress --- NADPH oxidases --- n/a

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