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Anti-Inflammatory Effects of Omega-3 Fatty Acids in the Brain: Physiological Mechanisms and Relevance to Pharmacology
10.1124/pr.117.014092 2018-01-01 Classically, polyunsaturated fatty acids (PUFA) were largely thought to be relatively inert structural components of brain, largely important for the formation of cellular membranes. Over the past 10 years, a host of bioactive lipid mediators that are enzymat... |
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RAL GTPases: Biology and Potential as Therapeutic Targets in Cancer
10.1124/pr.117.014415 2018-01-01 More than a hundred proteins comprise the RAS superfamily of small GTPases. This family can be divided into RAS, RHO, RAB, RAN, ARF, and RAD subfamilies, with each shown to play distinct roles in human cells in both health and disease. The RAS subfamily has a... |
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Connexins in Cardiovascular and Neurovascular Health and Disease: Pharmacological Implications
10.1124/pr.115.012062 2017-10-01 Connexins are ubiquitous channel forming proteins that assemble as plasma membrane hemichannels and as intercellular gap junction channels that directly connect cells. In the heart, gap junction channels electrically connect myocytes and specialized conductiv... |
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Small-Molecule Screens: A Gateway to Cancer Therapeutic Agents with Case Studies of Food and Drug Administration–Approved Drugs
10.1124/pr.117.013755 2017-10-01 High-throughput screening (HTS) of small-molecule libraries accelerates the discovery of chemical leads to serve as starting points for probe or therapeutic development. With this approach, thousands of unique small molecules, representing a diverse chemical ... |
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The Hyperpolarization-Activated Cyclic Nucleotide–Gated Channels: from Biophysics to Pharmacology of a Unique Family of Ion Channels
10.1124/pr.117.014035 2017-10-01 Hyperpolarization-activated, cyclic nucleotide–gated (HCN) channels are important members of the voltage-gated pore loop channels family. They show unique features: they open at hyperpolarizing potential, carry a mixed Na/K current, and are regulated by cycli... |
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International Union of Basic and Clinical Pharmacology. CII: Pharmacological Modulation of H2S Levels: H2S Donors and H2S Biosynthesis Inhibitors
10.1124/pr.117.014050 2017-10-01 Over the last three decades, an unprecedented explosion occurred in the understanding of the biologic roles of the gaseous molecules nitric oxide (NO), carbon monoxide (CO), and—over the last decade—in the area of hydrogen sulfide (H2S), the “third gasotransm... |
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Chemical Tools for Studying Lipid-Binding Class A G Protein–Coupled Receptors
10.1124/pr.116.013243 2017-07-01 Cannabinoid, free fatty acid, lysophosphatidic acid, sphingosine 1-phosphate, prostanoid, leukotriene, bile acid, and platelet-activating factor receptor families are class A G protein–coupled receptors with endogenous lipid ligands. Pharmacological tools are... |
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Botulinum Neurotoxins: Biology, Pharmacology, and Toxicology
10.1124/pr.116.012658 2017-04-01 The study of botulinum neurotoxins (BoNT) is rapidly progressing in many aspects. Novel BoNTs are being discovered owing to next generation sequencing, but their biologic and pharmacological properties remain largely unknown. The molecular structure of the la... |
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Systems Chronotherapeutics
10.1124/pr.116.013441 2017-04-01 Chronotherapeutics aim at treating illnesses according to the endogenous biologic rhythms, which moderate xenobiotic metabolism and cellular drug response. The molecular clocks present in individual cells involve approximately fifteen clock genes interconnect... |
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International Union of Basic and Clinical Pharmacology. CI. Structures and Small Molecule Modulators of Mammalian Adenylyl Cyclases
10.1124/pr.116.013078 2017-04-01
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