摘要：【关键词】 42 Nicotinic Receptors 4 and 2 nicotinic acetylcholine receptor (nAChR) subunits expressed heterologously assemble into receptors with high (HS) and low (LS) sensitivity to acetylcho...

摘要：【关键词】 Capacitative Although the molecular identity of capacitative Ca2+ entry (CCE) channels remains elusive, transient receptor potential channel (TRPC) family members 3, 6, and 7, which ...

摘要：【关键词】 Divergent Activities Azathioprine is a thiopurine prodrug clinically used for immunosuppression in the treatment of inflammatory diseases and in pharmacological regimens of organ tra...

摘要：【关键词】 Interaction Studies This study investigated the reciprocal cross-interactions between two distinct allosteric sites on the M4 muscarinic acetylcholine receptor (mAChR) in the absence...

摘要：【关键词】 Cross-Talk between Gs- Human mast cells express functional A2A and A2B adenosine receptors。 Gs-linked pathways also play a role in the A2B receptor-dependent stimulation of IL-4 sec...

摘要：【关键词】 State-Dependent Verapamil Block Verapamil is a potent phenylalkylamine antihypertensive believed to exert its therapeutic effect primarily by blocking high-voltage-activated L-type c...

摘要：【关键词】 Validation Asthma and chronic obstructive pulmonary disease (COPD) are characterized by chronic airway inflammation。 Proinflammatory cytokines, including interleukin (IL)-1 and tumo...

摘要：【关键词】 Mechanisms Execution of apoptotic program in mitochondria is associated with accumulation of cardiolipin peroxidation products required for the release of proapoptotic factors into t...

摘要：【关键词】 Simultaneous Activation Hetero-oligomerization among G protein-coupled receptors has been proposed to contribute to signal integration。 Because sensory neuron-specific receptors (SN...

摘要：【关键词】 Agonist-Selective Mechanisms The ability of two opioid agonists, [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO) and morphine, to induce µ。 Both DAMGO and morphine activated GIRK...

摘要：【关键词】 Allosteric Interactions Required Dihydropyridines (DHPs) are an important class of drugs, used extensively in the treatment of angina pectoris, hypertension, and arrhythmia。 An Allo...

摘要：【关键词】 Differences in Kinetics Xanomeline is a functionally selective M1/M4 muscarinic acetylcholine receptor agonist that nevertheless binds with high affinity to all five subtypes of musc...

摘要：【关键词】 Three-Substituted Mechanisms of lethality of the three-substituted indolinone and putatively selective cyclin-dependent kinase (CDK)2 inhibitor 3-[1-(3H-imidazol-4-yl)-meth-(Z)-ylide...

摘要：【关键词】 Polysaccharide Ganoderma lucidum is a medicinal mushroom in China and other Asian countries。 lucidum (PS-G) is a branched (16)--D-glucan moiety。 In this study, we examined the effe...

摘要：【关键词】 Hepatocyte Hepatitis C virus (HCV) is known to induce hepatic oxidative stress that is implicated in the up-regulation of multidrug resistance proteins (MRPs)。 The relationship betw...

摘要：【关键词】 A Novel Class We recently reported a novel class of compounds, represented by 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide (CD-PPB), that act as positive allosteric modulators (...

摘要：【关键词】 Transformed Cells We determined one mechanism by which the putative phosphoinositide-dependent kinase (PDK)-1 inhibitor 2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyraz...

摘要：【关键词】 Oligomerization In this study, we report the homo- and hetero-oligomerization of the human histamine H4R by both biochemical (Western blot and immobilized metal affinity chromatograp...

摘要：【关键词】 Tamoxifen The bulky side chains of antiestrogens hinder folding of the ligand binding domain (LBD) of estrogen receptors (ERs) into a transcriptionally active conformation。 Tamoxife...

摘要：【关键词】 Mapping Residues The serotonin 5-HT3 receptor (5-HT3R) is a member of the cys-loop ligand-gated ion channel family。

摘要：【关键词】 Discovery Shp2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene。 Moreover, gain-of-function Shp2 mutations have been found in childhood leukemias and N...

摘要： Fernandez-Salguero PM, Hilbert DM, Rudikoff S, Ward JM, and Gonzalez FJ (1996) Aryl-hydrocarbon receptor-deficient mice are resistant to 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced to...

摘要：【关键词】 Regulation The dopamine (DA) transporter (DAT) mediates the removal of released DA。 DAT is the major molecular target responsible for the rewarding properties and abuse potential of...

摘要：【关键词】 Mammalian In the present study, we identified the CUB5 domain of mammalian Tolloid (mTLD) as a novel protein binding to 1A-adrenergic receptor (AR) using the yeast two-hybrid system。...

摘要：【关键词】 Transforming Transforming growth factor- (TGF) is a major mediator of normal wound healing and of pathological conditions involving fibrosis, such as idiopathic pulmonary fibrosis。 ...

摘要：【关键词】 5‘-O-Tritylated Thymidine phosphorylase (TPase) is one of the key enzymes involved in the pyrimidine nucleoside salvage pathway。 Evaluation of the Anti-TPase Activity of 5‘-O-Trit...

摘要：【关键词】 Lithium Inhibits Ceramide- Lithium confers cell protection against stress and toxic stimuli。 Lithium and OA abrogated ceramide- and etoposide-induced Bcl-2 dephosphorylation at seri...

摘要：【关键词】 Isoliquiritigenin Isoliquiritigenin, one of the major constituents of Glycyrrhiza uralensis (licorice), is a natural pigment with a simple chalcone structure 4,2‘,4‘-trihydroxychal...

摘要：【关键词】 Fluoxetine Once bound to methylated CpG sites, methyl-CpG-binding protein 2 (MeCP2) is thought to silence transcription of downstream genes by recruiting a histone deacetylase (HDAC)...

摘要：【关键词】 Novel Monkeys are widely used as a primate model to study drug metabolism because they generally show a metabolic pattern similar to humans。 In this study, we report identification ...

摘要：【关键词】 Pregabalin Reduces Pregabalin [S-[+]-3-isobutylGABA or (S)-3-(aminomethyl)-5-methylhexanoic acid, Lyrica] is an anticonvulsant and analgesic medication that is both structurally and ...

摘要：【关键词】 Rescue Blockage of the p53 tumor suppressor has been found to impair nerve growth factor (NGF)-induced neurite outgrowth in PC-12 cells。 We report herein that such impairment could ...

摘要：【关键词】 Cimetidine The present study demonstrates a possible mechanism for the improvement of gastrointestinal cancer patients‘ prognosis by the histamine receptor type 2 (H2R) antagonist c...

摘要：【关键词】 C Terminus G protein-coupled receptors are endowed with carboxyl termini that vary greatly in length and sequence。

摘要：【关键词】 Pharmacology The contribution by Micheva et al。 467) in this issue of Molecular Pharmacology adds to our understanding of the action of pregabalin, a drug used for treatment of part...

摘要：Mechanisms of Chromatin Remodeling。

摘要：【关键词】 OSU-03012 In an article presented in this issue of Molecular Pharmacology, Yacoub et al。 589) examine the actions of 2-amino-N{4-5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1...