摘要：【关键词】 Selective Recent clinical studies reveal that selective agonists of group II metabotropic glutamate (mGlu) receptors have robust efficacy in treating positive and negative symptoms i...

摘要：【关键词】 Structure-Function The M2 muscarinic acetylcholine receptor (mAChR) possesses at least one binding site for allosteric modulators that is dependent on the residues 172EDGE175, Tyr177...

摘要：【关键词】 Desensitization When dopamine D1 and D2 receptors were coactivated in D1-D2 receptor hetero-oligomeric complexes, a novel phospholipase C-mediated calcium signal was generated。 In t...

摘要：【关键词】 N-Ethylmaleimide-Sensitive Recycling of G protein-coupled receptors determines the functional resensitization of receptors and is implicated in switching &beta。-Adrenoceptors play a...

摘要：【关键词】 Inhibition Cerebral microvascular endothelial cells form the anatomical basis of the blood-brain barrier (BBB), and the tight junctions of the BBB are critical for maintaining brain ...

摘要：【关键词】 Suppression N,N-Dimethyl-D-erythro-sphingosine (DMS) competitively inhibits sphingosine kinase (SPHK) and has been widely used to assess the role of SPHK during cellular events, incl...

摘要：【关键词】 Glitazones The glitazones (or thiazolidinediones) are synthetic compounds used in type-2 diabetes, but they also have broad antiproliferative and anti-inflammatory properties still n...

摘要：【关键词】 Multidrug Glucuronidation is a major hepatic detoxification pathway for endogenous and exogenous compounds, resulting in the intracellular formation of polar metabolites that require...

摘要：Caffeine Treatment of Cancer Cells。 Caffeine Inhibits Adenosine-Induced HIF-1 Protein Accumulation in Human Colon Cancer Cells。 Caffeine did not induce cell death, as shown in Fig。 Caffeine Inhi...

摘要：【关键词】 Identification diltiazem, whereas M4 and M6 metabolites displayed weak agonist activity, and the M8 and M9 metabolites were inactive。 Diltiazem is an L-type Ca2+ channel blocker dev...

摘要：【关键词】 5-Androstenediol 5-Androstenediol (5-AED) stimulates hematopoiesis and enhances survival in animals exposed to ionizing radiation (IR), suggesting that this steroid may act on hemato...

摘要：【关键词】 Transcriptional We have demonstrated previously that brain-derived neurotrophic factor (BDNF) signaling in the amygdala is required for the consolidation of fear memory。[Abstract/Fr...

摘要：【关键词】 β1 (KCNMB1) Among the nongenomic effects of steroids, control of vasomotion has received increasing attention。 Lithocholate (LC) and other physiologically relevant cholane-derived ...

摘要：【关键词】 Molecular Most nonpeptide antagonists for CC-chemokine receptors share a common pharmacophore with a centrally located, positively charged amine that interacts with the highly conser...

摘要：【关键词】 Critical We examined the role of sphingosine kinase-1 (SphK1), a critical regulator of the ceramide/sphingosine 1-phosphate (S1P) biostat, in the regulation of death and survival of ...

摘要：【关键词】 Characterization ATM and NBS1, mutation of which lead to the human autosomal recessive diseases ataxia telangiectasia and Nijmegen breakage syndrome (NBS), respectively, are essentia...

摘要：【关键词】 Novel The E-ring lactone is the Achilles‘ heel of camptothecin derivatives: although it is considered necessary for the inhibition of the enzyme topoisomerase I (topo1), the opening...

摘要：【关键词】 Bradykinin-Induced Bradykinin produced at sites of tissue injury and inflammation elicits acute pain and alters the sensitivity of nociceptive neurons to subsequent stimuli。 Bradyki...

摘要：【关键词】 Novel THRX-160209 is a potent antagonist at the M2 muscarinic acetylcholine (ACh) receptor subtype that was designed using a multivalent strategy, simultaneously targeting the orthos...

摘要：【关键词】 UR-1505 2-Hydroxy-4(-2,2,3,3,3-pentafluoropropoxy)-benzoic acid (UR-1505), a new molecule chemically related to salicylic acid, has immunomodulator properties and is currently under ...

摘要：【关键词】 Molecular The structurally unique amino-terminal domain of class II G protein-coupled receptors is critically important for ligand binding and receptor activation。 This was attached...

摘要：【关键词】 APETx1 We studied the mechanism of action and the binding site of APETx1, a peptide toxin purified from sea anemone, on the human ether-a-go-go-related gene (hERG) channel。1 channel...

摘要：【关键词】 Trapping Drugs that exhibit insurmountable antagonism are proposed to provide improved clinical efficacy through extended receptor blockade。 Mutational Analysis of the Second and Th...

摘要：【关键词】 Erlotinib Erlotinib, a small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, has been shown to have potent antitumor effects against human non-small-cell ...

摘要：【关键词】 Trapping Ligands Because gonadotropin-releasing hormone (GnRH) analogs constitute an important class of therapeutics for various reproductive and hormone-dependent disorders, many no...

摘要：【关键词】 Brain-Derived Brain-derived neurotrophic factor (BDNF), a member of the neurotrophin family, plays an important role in synaptic plasticity。

摘要：Heterotrimeric G-protein subunit secondary structure。 Heterotrimeric G-protein tertiary and quaternary structure。 Ballesteros JA, Jensen AD, Liapakis G, Rasmussen SG, Shi L,...