Selective inhibitors of individual subfamilies of G protein-coupled receptor kinases (GRKs) would serve as useful chemical probes as well as leads for therapeutic applications ranging from heart failure to Parkinson's disease. To identify such inhibitors, differential scanning fluorimetry was used to screen a collection of known protein kinase inhibitors that could increase the melting points o...

The 17β-HSD3 enzyme plays a key role in treatment of prostate cancer and small inhibitorscan be used to efficiently target it. In the present study, the multiple linear regression (MLR),and support vector machine (SVM) methods were used to interpret the chemical structuralfunctionality against the inhibition activity of some 17β-HSD3inhibitors. Chemical structuralinformation were described thro...

The multidrug transporter NorA contributes to the resistance of Staphylococcus aureus to fluoroquinolone antibiotics by promoting their active extrusion from the cell. Previous studies with the alkaloid reserpine, the first identified inhibitor of NorA, indicate that the combination of a chemical NorA inhibitor with a fluoroquinolone could improve the efficacy of this class of antibiotics. Sinc...

the cross-border symposium on hepatitis c, entitled “why treating now?” was held on 15th may 2013 during the 5th international tehran hepatitis congress. the present report summarizing communicated insights during this symposium is intended to help health care providers to make well-informed decisions when treating patients with chronic hepatitis c (chc). since today’s evolving science of hepat...

schizophrenia and various neurological disorders have some signs and symptoms. visual hallucinations are one of such disorders. the related studies in some diseases for example parkinson disease and lewy body dementia indicate that acetylcholine (ach) plays a significant role in neuropsychiatric manifestation and its association with visual hallucination; therefore, visual hallucinations occur ...

in this assay, the evaluation of lipophilicity of four ace-inhibitors and hydrochlorothiazide (hctz) with rp-tlc on cellulose layers was described using three binary solvent systems. the selected ace inhibitors had sufficiently different structures which can indicate the method suitability for their lipophilicity evaluation as the model substances in comparison with hctz. in addition, the linea...

objective diabetes mellitus is manifested by hyperglycaemia. different treatments such as diets and drugs are recommended for diabetes control. for various reasons in recent years traditional plant (herbal) therapies as prescribed by indigenous systems of medicine with different mechanisms have commonly been used. the digestive enzymes such as alpha glucosidase are among these herbal remedies. ...

background: factor viii administration to hemophilia a patients results in an immune response (inhibitor formation) which significantly complicates the therapy. the present study was performed to determine the prevalence of inhibitor development in hemophilia a patients receiving recombinant factor viii therapy. materials and methods: this was an observational descriptive study. clotting factor...

a series of structurally related 2,4-dioxopyrimidine-1-carboxamide derivatives as highly potent inhibitors against acid ceramidase were subjected to hologram quantitative structure-activity relationship (hqsar) analysis. a training set containing 24 compounds served to establish the hqsar model. the best hqsar model was generated using atoms, bond, connectivity, donor and acceptor as fragment d...