Search Results - "Insel, PA"

GPCR expression in tissues and cells: Are the optimal receptors being used as drug targets? by Insel, PA, Snead, A, Murray, F, Zhang, L, Yokouchi, H, Katakia, T, Kwon, O, Dimucci, D, Wilderman, A

“…G‐protein‐coupled receptors [GPCRs, also known as 7‐transmembrane (7‐TM) receptors] comprise the largest family of membrane receptors in humans and other…”
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Therapeutic Oligonucleotides: State of the Art by Smith, C.I. Edvard, Zain, Rula

“…Oligonucleotides (ONs) can interfere with biomolecules representing the entire extended central dogma. Antisense gapmer, steric block, splice-switching ONs,…”
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The Cellular Thermal Shift Assay: A Novel Biophysical Assay for In Situ Drug Target Engagement and Mechanistic Biomarker Studies by Martinez Molina, Daniel, Nordlund, Pär

“…A drug must engage its intended target to achieve its therapeutic effect. However, conclusively measuring target engagement (TE) in situ is challenging. This…”
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Role of Cell Death in Toxicology: Does It Matter How Cells Die? by Orrenius, Sten

“…My research activity started with studies on drug metabolism in rat liver microsomes in the early 1960s. The CO-binding pigment (cytochrome P450) had been…”
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Therapeutic Approaches to the Treatment of Tinnitus by Langguth, Berthold, Elgoyhen, Ana Belen, Cederroth, Christopher R

“…Tinnitus is a highly prevalent condition that is associated with hearing loss in most cases. In the absence of external stimuli, phantom perceptions of sounds…”
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Pharmacoepigenetics and Toxicoepigenetics: Novel Mechanistic Insights and Therapeutic Opportunities by Lauschke, Volker M, Barragan, Isabel, Ingelman-Sundberg, Magnus

“…Pharmacological treatment and exposure to xenobiotics can cause substantial changes in epigenetic signatures. The majority of these epigenetic changes, caused…”
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GPR68: An Emerging Drug Target in Cancer by Wiley, Shu Z, Sriram, Krishna, Salmerón, Cristina, Insel, Paul A

“…GPR68 (or ovarian cancer G protein-coupled receptor 1, OGR1) is a proton-sensing G-protein-coupled receptor (GPCR) that responds to extracellular acidity and…”
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Model-Informed Precision Dosing: Background, Requirements, Validation, Implementation, and Forward Trajectory of Individualizing Drug Therapy by Darwich, Adam S, Polasek, Thomas M, Aronson, Jeffrey K, Ogungbenro, Kayode, Wright, Daniel F.B, Achour, Brahim, Reny, Jean-Luc, Daali, Youssef, Eiermann, Birgit, Cook, Jack, Lesko, Lawrence, McLachlan, Andrew J, Rostami-Hodjegan, Amin

“…Model-informed precision dosing (MIPD) has become synonymous with modern approaches for individualizing drug therapy, in which the characteristics of each…”
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Application of Microphysiological Systems to Enhance Safety Assessment in Drug Discovery by Ewart, Lorna, Dehne, Eva-Maria, Fabre, Kristin, Gibbs, Susan, Hickman, James, Hornberg, Ellinor, Ingelman-Sundberg, Magnus, Jang, Kyung-Jin, Jones, David R, Lauschke, Volker M, Marx, Uwe, Mettetal, Jerome T, Pointon, Amy, Williams, Dominic, Zimmermann, Wolfram-Hubertus, Newham, Peter

“…Enhancing the early detection of new therapies that are likely to carry a safety liability in the context of the intended patient population would provide a…”
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The evolving role of lipid rafts and caveolae in G protein‐coupled receptor signaling: implications for molecular pharmacology by Ostrom, Rennolds S, Insel, Paul A

“…The many components of G‐protein‐coupled receptor (GPCR) signal transduction provide cells with numerous combinations with which to customize their responses…”
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Autophagy in Toxicology: Cause or Consequence? by ORRENIUS, Sten, KAMINSKYY, Vitaliy O, ZHIVOTOVSKY, Boris

“…Research on autophagy and its effects on cell metabolism and physiology has increased dramatically during recent years. Multiple forms of autophagy have been…”
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Inhibition of Cardiac Myofibroblast Formation and Collagen Synthesis by Activation and Overexpression of Adenylyl Cyclase by Swaney, James S., Roth, David M., Olson, Erik R., Naugle, Jennifer E., Meszaros, J. Gary, Insel, Paul A., Seegmiller, J. Edwin

“…Transformation of fibroblasts to myofibroblasts, characterized by expression of α-smooth muscle actin (α-SMA) and production of extracellular matrix (ECM)…”
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Autonomic Nervous System Pharmacogenomics: A Progress Report by Kirstein, Shelli L, Insel, Paul A

“…Pharmacogenetics, the inherited basis for interindividual differences in drug response, has rapidly expanded with the advent of new molecular tools and the…”
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The Pro-apoptotic Protein Bim Is a Convergence Point for cAMP/Protein Kinase A- and Glucocorticoid-promoted Apoptosis of Lymphoid Cells by Zhang, Lingzhi, Insel, Paul A

“…The mechanisms by which cAMP mediates apoptosis are not well understood. In the current studies, we used wild-type (WT) S49 T-lymphoma cells and the kin –…”
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G-protein-coupled Receptor Signaling Components Localize in Both Sarcolemmal and Intracellular Caveolin-3-associated Microdomains in Adult Cardiac Myocytes by Head, Brian P., Patel, Hemal H., Roth, David M., Lai, N. Chin, Niesman, Ingrid R., Farquhar, Marilyn G., Insel, Paul A.

“…This study tests the hypothesis that G-protein-coupled receptor (GPCR) signaling components involved in the regulation of adenylyl cyclase (AC) localize with…”
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Forskolin as a tool for examining adenylyl cyclase expression, regulation, and G protein signaling by Insel, Paul A, Ostrom, Rennolds S

“…1. As initially shown by Seamon and Daly, the diterpene forskolin directly activates adenylyl cyclase (AC) and raises cyclic AMP levels in a wide variety of…”
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Multi-Tasking RGS Proteins in the Heart: The Next Therapeutic Target? by Riddle, Evan L, Schwartzman, Raúl A, Bond, Meredith, Insel, Paul A

“…Regulator of G-protein–signaling (RGS) proteins play a key role in the regulation of G-protein–coupled receptor (GPCR) signaling. The characteristic hallmark…”
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Protein kinase C isozymes and the regulation of diverse cell responses by Dempsey, E C, Newton, A C, Mochly-Rosen, D, Fields, A P, Reyland, M E, Insel, P A, Messing, R O

“…Individual protein kinase C (PKC) isozymes have been implicated in many cellular responses important in lung health and disease, including permeability,…”
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Receptor Number and Caveolar Co-localization Determine Receptor Coupling Efficiency to Adenylyl Cyclase by Ostrom, Rennolds S., Gregorian, Caroline, Drenan, Ryan M., Xiang, Yang, Regan, John W., Insel, Paul A.

“…Recent evidence suggests that many signaling molecules localize in microdomains of the plasma membrane, particularly caveolae. In this study, overexpression of…”
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Inhibition of Apoptosis in Normal and Transformed Intestinal Epithelial Cells by cAMP through Induction of Inhibitor of Apoptosis Protein (IAP)-2 by Nishihara, Hiroshi, Kizaka-Kondoh, Shinae, Insel, Paul A., Eckmann, Lars

“…Cyclooxygenase (COX)-2, a rate-limiting enzyme of prostaglandin (PG) production, is overexpressed in colorectal adenomas and adenocarcinomas, and its…”
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