Steroid hormones exert their glucocorticoid activity by binding reversibly to a receptor protein in the cytoplasm of target cells [ 1,2]. We have shown [3] that Ca2+ inhibit the rate of association of dexamethasone, a semi-synthetic glucocorticoid, with the glucocorticoid receptor. The half-maximum effect was seen at 0.3 PM free Ca2+, a concentration within the range (0. l1 PM) of fluctuations ...

Persistent androgen receptor (AR) activation drives therapeutic resistance to second-generation AR pathway inhibitors and contributes the progression of advanced prostate cancer. One mechanism is point mutations in ligand binding domain that can transform antagonists into agonists. The F877L mutation, identified patients treated with enzalutamide or apalutamide, confers both apalutamide. Compou...

Childrenwith Helicobacter infection need treatment. The aim of treatment is elimination of H.Pylori. Most patients with this infection are asymptomatic and without peptic disease. Treatment and management of these patients are controversy. Conventional Treatment: The best treatment for H. pylori eradication regimens should have cure rates of at least 80%, be without major side effects, and indu...

fire blight is an important worldwide disease of pome fruits that control of which through antibiotics is particularly critical. in this case and in absence of another chemical methods, the biocontrol methods can be considered as the best alternative for control of fire blight. in this study efficacy of 5 isolates of antagonistic bacteria belongs to pseudomonas fluorescens and pantoea agglomera...

Inhibiting the renin-angiotensin system has proven to be one of the most fruitful therapeutic strategies in cardiovascular medicine. Believed to have evolved to maintain blood volume and perfusion pressure in conditions of hemorrhage or hypovolemia, the renin-angiotensin-aldosterone system (RAAS) is upregulated in the setting of left ventricular (LV) dysfunction or heart failure (1). Pharmacolo...

Myelin of the adult central nervous system (CNS) is one of the major sources of inhibitors of axon regeneration following injury. The three known myelin-derived inhibitors (Nogo, MAG, and OMgp) bind with high affinity to the Nogo-66 receptor (NgR) on axons and limit neurite outgrowth. Here we show that RNA aptamers can be generated that bind with high affinity to NgR, compete with myelin-derive...

Aims Liquid chromatography-mass spectrometry (LC-MS/MS) is an objective new technique to assess non-adherence medications. We used this method study the prevalence, predictors and outcomes of in patients with heart failure reduced left ventricular ejection fraction (HFrEF). Methods results This included 1296 HFrEF from BIOSTAT-CHF, a that aimed optimise guideline-recommended therapies. Angioten...

DC-SIGN antagonists were designed combining one selective monovalent glycomimetic ligand with trivalent dendrons separated by a rigid core of controlled length. The design combines multiple multivalency effects to achieve inhibitors of HIV infection, which are active in nanomolar concentration.

Bovine adrenal zona fasciculata (AZF) cells express bTREK-1 background K+ channels that set the resting membrane potential. Whole-cell and single-channel patch-clamp recording were used to compare five Ca2+ channel antagonists with respect to their potency as inhibitors of native bTREK-1 K+ channels. The dihydropyridine (DHP) Ca2+ channel antagonists amlodipine and niguldipine potently and spec...

2,3-Benzodiazepine (2,3-BDZ) compounds represent a group of structurally diverse, small-molecule antagonists of (R, S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptors. Antagonists of AMPA receptors are drug candidates for potential treatment of a number of neurological disorders such as epilepsy, stroke and amyotrophic lateral sclerosis (ALS). How to make better inhib...