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Publikováno v:
Molecular Pharmacology. 88:816-824
Sustained activation of G protein–coupled receptors can lead to a rapid decline in signaling through acute receptor desensitization. In the case of the μ-opioid receptor (MOPr), this desensitization may play a role in the development of analgesic
Publikováno v:
Molecular Pharmacology. 87:277-285
Re-epithelialization begins early during skin wound healing and is regulated by various growth factors and cytokines. Angiotensin II promotes the migration of keratinocytes and thereby contributes to wound healing. We investigated the mechanism by wh
Publikováno v:
Molecular Pharmacology. 86:243-251
Many cells express both P2X cation channels and P2Y G-protein-coupled receptors that are costimulated by nucleotides released during physiologic or pathophysiologic responses. For example, during hemostasis and thrombosis, ATP-gated P2X1 channels and
Autor:
Pierre Formstecher, Marie-Edith Rafestin-Oblin, Bernadette Masselot, Jérôme Fagart, Michel Fay, Dominique Hetuin, Thierry Idziorek, Xavier Dezitter, Solenne Taront
Publikováno v:
Molecular Pharmacology. 85:226-236
There is a therapeutic need for glucocorticoid receptor (GR) ligands that distinguish between the transrepression and transactivation activity of the GR, the later thought to be responsible for side effects. These ligands are known as “dissociated
Autor:
Suchitra Joshi, Jaideep Kapur
Publikováno v:
Molecular Pharmacology. 84:1-11
Neurosteroids are endogenous allosteric modulators of GABAA receptors (GABARs), and they enhance GABAR-mediated inhibition. However, GABARs expressed on hippocampal dentate granule neurons of epileptic animals are modified such that their neurosteroi
Publikováno v:
Molecular Pharmacology. 83:781-792
With the recent interest of protease-activated receptors (PAR) 1 and PAR4 as possible targets for the treatment of thrombotic disorders, we compared the efficacy of protease-activated receptor (PAR)1 and PAR4 in the generation of procoagulant phenoty
Autor:
Lisa A. Opanashuk, Daniel P. Dever
Publikováno v:
Molecular Pharmacology. 81:669-678
The aryl hydrocarbon receptor (AhR), a ligand-activated member of the basic helix-loop-helix (bHLH)/PER-ARNT-SIM (PAS) transcription superfamily, is known to regulate the toxicity of polyaromatic halogenated hydrocarbon environmental chemicals, most
Publikováno v:
Molecular Pharmacology. 81:587-597
Opioids potently modulate neuronal functions, for example, by regulating the activity of transcription factors. Here, we investigated the effect of morphine on the activity of the transcription factor nuclear factor κB (NF-κB). Establishing cellula
Autor:
Abhishek Tripathi, Leanne L. Cribbs, Bharath K. Mani, Christina Robakowski, Matthias Majetschak, Kenneth L. Byron, Lyubov I. Brueggemann
Publikováno v:
Molecular pharmacology. 89(3)
Kv7 (KCNQ) channels, formed as homo- or heterotetramers of Kv7.4 and Kv7.5 α-subunits, are important regulators of vascular smooth muscle cell (VSMC) membrane voltage. Recent studies demonstrate that direct pharmacological modulation of VSMC Kv7 cha
Autor:
Anton Simeonov, Ganesha Rai, Victor Kenyon, David J. Maloney, Theodore R. Holman, Michael Holinstat, Joanne Vesci, Olivier Boutaud, Jennifer Yeung, Patrick L. Apopa, Ajit Jadhav
Publikováno v:
Molecular Pharmacology. 81:420-430
Platelet activation is important in the regulation of hemostasis and thrombosis. Uncontrolled activation of platelets may lead to arterial thrombosis, which is a major cause of myocardial infarction and stroke. After activation, metabolism of arachid