Journal: Molecular Pharmacology

Article Title: Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection

doi: 10.1124/mol.116.107755

Figure Lengend Snippet: In vitro pharmacological profiling of efavirenz, compound I, and compound II against targets for adverse drug reactions as described in Materials and Methods. Rows represent compounds tested and columns represent targets. Percentage inhibition at 10 µM concentration of the compounds is color -coded: <50% inhibition of target is labeled in green and >50% inhibition is labeled in red. Abbreviations: CYP, cytochrome P450; ADOR, adenosine receptor; ADR, adrenergic receptor; DHP, dihydropyridine or calcium channel L-type; CNR1, cannabinoid receptor; DRD, dopamine receptor; NMDAR, glutamate receptor; HRH1, histamine receptor; imidazole I2, imidazole I2 receptor; CHRM, muscarinic; nACHR, nicotinic acetylcholine; OPRM, opiate µ phorbol ester receptor, KATP, potassium channel; hERG, human ether-à-go-go-related gene; EP4, prostanoid receptor; rolipram, phosphodiesterase-4 inhibitor; 5-HT2B, serotonin receptor 2B; sigma σ1, sigma σ1receptor; Na channel, sodium channel; NET, norepinephrine transporter.

Article Snippet: Abbreviations: CYP, cytochrome P450; ADOR, adenosine receptor; ADR, adrenergic receptor; DHP, dihydropyridine or calcium channel L-type; CNR1, cannabinoid receptor; DRD, dopamine receptor; NMDAR, glutamate receptor; HRH1, histamine receptor; imidazole I 2 , imidazole I 2 receptor; CHRM, muscarinic; nACHR, nicotinic acetylcholine; OPRM, opiate µ phorbol ester receptor, KATP, potassium channel; hERG, human ether-à-go-go-related gene; EP4, prostanoid receptor; rolipram, phosphodiesterase-4 inhibitor; 5-HT2B, serotonin receptor 2B; sigma σ 1, sigma σ 1receptor; Na channel, sodium channel; NET, norepinephrine transporter.

Techniques: In Vitro, Inhibition, Concentration Assay, Labeling

Journal: Oncotarget

Article Title: Up-regulation of serotonin receptor 2B mRNA and protein in the peri-infarcted area of aged rats and stroke patients

doi: 10.18632/oncotarget.8277

Figure Lengend Snippet: A. - C. By day 14 the cortical infarcts were similar in size in both age groups i.e. 45% of total cortical volume in young rats and 55.7% in aged rats. D. By RT-PCR at day 3 post-stroke there was a 15-fold up-regulation in the expression of Htr2b mRNA that was 7-fold higher in the lesioned area of aged animals than in young animals ( N = 7/age group). Fluoxetine treatment, however, caused by day 28, a significant increase (1.9-fold) in the Htr2b mRNA levels in the perilesional area of aged rats E. . In the perinfarcted area of aged rats HTR2B-positive cells (green) were co-localized with NeuN-positive nuclei (red) at day3 after stroke in aged rat brains (arrows). F. Although the mRNA expression was largely down-regulated by day14 post-stroke, the HTR2B/NeuN co-localization persisted in the peri-infarcted area of aged rats (arrows).

Article Snippet: Of the genes possibly involved in post-stroke depression, we found by transcriptomics analysis using the Affymetrix platform, that the transcripts encoding the serotonin receptor 2B (Htr2b) but not Htr2a were upregulated after stroke in the aged rat stroke model.

Techniques: Reverse Transcription Polymerase Chain Reaction, Expressing

Journal: Oncotarget

Article Title: Up-regulation of serotonin receptor 2B mRNA and protein in the peri-infarcted area of aged rats and stroke patients

doi: 10.18632/oncotarget.8277

Figure Lengend Snippet: By chemical immunostaining, the HTR2B receptor in human subjects has a perinuclear localization ( A. , arrows; Vector blue-grey development) in the penumbral region of post-mortem stroke patients. By immunofluorescence, a similar co-localization was observed in the peri-infarcted area between HTR2B-positive cells (green) and cells labeled by beta III tubulin (red), a marker of mature neuronal cells ( B. , arrows). In addition to the neuronal co-localization, we also noted the co-localization with astrocytes labeled with FITC-GFAP ( C. , arrows) in the penumbral region of post-mortem stroke patients. However, there was no co-localization with astrocytes in the unlesioned, contralateral region of the same post-stroke patient ( D. , arrowheads). Bar, 100 μm. Abbreviations : PI, periinfarct.

Article Snippet: Of the genes possibly involved in post-stroke depression, we found by transcriptomics analysis using the Affymetrix platform, that the transcripts encoding the serotonin receptor 2B (Htr2b) but not Htr2a were upregulated after stroke in the aged rat stroke model.

Techniques: Immunostaining, Plasmid Preparation, Immunofluorescence, Labeling, Marker

Journal: Oncotarget

Article Title: Up-regulation of serotonin receptor 2B mRNA and protein in the peri-infarcted area of aged rats and stroke patients

doi: 10.18632/oncotarget.8277

Figure Lengend Snippet: A. In the peri-infarcted area of young animals, activated microglia (arrowheads) was seen in close association with HTR2B + neurons (arrows). The close proximity of HTR2B and brain microglia was less evident at day 14 post-stroke B. . C. In aged rats, numerous microglial cells immunopositive for IbaI were wrapped around neurons expressing HTR2B (arrowheads), suggesting a pre-phagocytic pathology. In addition, a robust co-localization of the microglia marker Iba1 with HTR2B-expressing blood vessels (inset; Bv). D. At day14, the co-localization between Iba1 and HtR2B was less evident in aged animals. E. In the peri-lesional area of human stroke victims we noted numerous phagocytic microglia expressing AIF1 (red), co-localized with HTR2B-expressing neurons (green). F. In remote areas with reference to the infarct core, numerous blood vessels were positive for HTR2B (green, arrows). Bar, 100 μm. Abbreviations : Bv, blood vessel; IC, infarct core; PI, periinfarct.

Article Snippet: Of the genes possibly involved in post-stroke depression, we found by transcriptomics analysis using the Affymetrix platform, that the transcripts encoding the serotonin receptor 2B (Htr2b) but not Htr2a were upregulated after stroke in the aged rat stroke model.

Techniques: Expressing, Marker

Journal: Cancers

Article Title: Drug Repurposing, an Attractive Strategy in Pancreatic Cancer Treatment: Preclinical and Clinical Updates

doi: 10.3390/cancers13163946

Figure Lengend Snippet: Predicted molecular targets and probability scores (≥0.6) for each repurposed drug according to the SwissTargetPrediction tool.

Article Snippet: Propranolol , Serotonin 2b (5-HT2b) receptor (1), Serotonin 1b (5-HT1b) receptor (1), Adrenergic receptor beta (1), Beta-1 adrenergic receptor (1), Serotonin 1a (5-HT1a) receptor (1), Serotonin 2a (5-HT2a) receptor (1), Serotonin 2c (5-HT2c) receptor (1), Serotonin transporter (1), Beta-3 adrenergic receptor (1), Sigma opioid receptor (1), Cytochrome P450 2D6 (1), Cytochrome P450 1A2 (1), Serotonin 6 (5-HT6) receptor (1).

Techniques: Binding Assay