Wnt/ß-catenin signaling is strongly implicated in neoplasia, but the role of this pathway in human breast cancer has been controversial. Here, we examined Wnt/ß-catenin pathway activation as a function of breast cancer progression, and tested for a relationship with HER2/neu expression, using a human tissue microarray comprising benign breast tissues, ductal carcinoma in situ (DCIS), and invasi...

1 Downregulation of Cdk6 kinase activity is crucial for TGF-ß induced growth inhibition (I) ………………………………………………………………………………….38 1.1 TGF-ß growth inhibition is attenuated by overexpression of wild type Cdk6 …………38 1.2 Cyclin D-related kinase activity is maintained in wild type Cdk6-overexpressing cells treated with TGF-ß …..……………………………………………………………….39 1.3 Cdk2-associated kinase activity is partia...

Complexation of celecoxib with ß-cyclodextrin and hydroxypropyl-ß-cyclodextrin in the presence and absence of polyvinylpyrrolidone and the effect of polyvinylpyrrolidone on the solubilizing efficiency of cyclodextrins and on the dissolution rate of celecoxib from the cyclodextrin complexes were investigated. The phase solubility studies indicated the formation of celecoxib-ß-cyclodextrin and ce...

Polyamines mediate acute metabolic effects and cardiac hypertrophy associated with β-adrenoceptor stimulation. They may also modulate β-adrenoceptors, causing functional responses in rat atria and tracheal smooth muscle. The aim of this study was to determine whether polyamines interact with human β(1)- and β(2)-adrenoceptors and the functional consequences of such an interaction. Chinese hamst...

Glucocorticoids (GCs) are well known to induce insulin resistance. However, the effect of GCs on insulin secretion has not been well characterized under physiological conditions in human. We here evaluated the effect of GCs on insulin secretion/ß-cell function precisely in a physiological condition. A population-based study of 1,071 Japanese individuals enrolled in the 2014 Iwaki study (390 men...

Thestimulatory effect of the extract of Portulaca oleracea (P. olerace) on β-adrenoceptor of tracheal smooth muscle was examined.To examine β-adrenoceptor stimulatory effect, concentration response curve to isoprenaline was obtained in pre-contracted tracheal smooth muscle in the presence of three concentrations of aqueous-ethanolic extract, propranolol, and saline. Values of EC50 (the effectiv...

The binding affinities of racemic derivatives of propranolol to ƒÀ-adrenoceptors were examined by means of radioligand binding assay to determine whether racemic propranolol shows biphasic binding to ,ƒÀ-adrenoceptors in a displacement experiment. Rat brain was used and the ƒÀadrenoceptor binding assay was carried out with 3H-dihydroalprenolol as the radioligand. A higher affinity of l-proprano...

The multifunctional protein ß-catenin governs as transcription factor the expression of a wide variety of genes relevant for cell proliferation and cell survival. In addition, ß-catenin is localized at the cell membrane and may influence the function of channels. The present study explored the possibility that ß-catenin participates in the regulation of the HERG K(+) channel. To this end, HERG ...

Changes in the activity of hypothalamic and brain-stem adrenergic neurons have been reported in young spontaneously hypertensive rats (SHR) prior to the development of hypertension. We have measured central alpha- and beta-adrenoceptor concentrations in 4-week-old SHR and Wistar-Kyoto (WKY) controls by direct radioligand binding studies using [3H]prazosin (alpha 1), [3H]clonidine (alpha 2), and...

The specific binding of [ 3 Hlclonidine to a,-adrenoceptors on neural membranes isolated from six brain areas was determined with rats treated for various periods of time with the muscarinic agonists, oxotremorine or pilocarpine, or with the muscarinic antagonists atropine, atropine methyl nitrate, scopolamine and scopolamine methyl bromide. Administration of pilocarpine, 10 mg/kg, twice daily ...