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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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Abstract

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: eng
Publisher: MDPI - Multidisciplinary Digital Publishing Institute
Subject: Medicine (General)
Added to DOAB on : 2019-06-26 08:44:07
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Abstract

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

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