Triazolone Compounds and Uses Thereof
ABSTRACT The invention disclosed herein is directed to compounds of Formula (1a) and (1b) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocyticδ leukemia, melanoma and other...
Registered Report: Systematic identification of genomic markers of drug sensitivity in cancer cells
ABSTRACT The Reproducibility Project: Cancer Biology seeks to address growing concerns about the reproducibility in scientific research by conducting replications of selected experiments from a number of high-profile papers in the field of cancer biology. The papers,...
Profiling of vitamin D metabolic intermediates towards VDR using novel stable gene reporter cell lines IZ-VDRE and IZ-CYP24
ABSTRACT Variety of xenobiotics, including therapeutically used vitamin D analogues or environmental and alimentary endocrine disruptors, may interfere with vitamin D receptor (VDR) signalling, with serious physiological or pathophysiological consequences. Therefore,...
Novel synthesised flavone derivatives provide significant insight into the structural features required for enhanced anti-proliferative activity
ABSTRACT With many cancers showing resistance to current chemotherapies, the search for novel anti-cancer agents is attracting considerable attention. Natural flavonoids have been identified as useful leads in such programmes. However, since an in-depth understanding...
Biochemical Characterization of the Active Anti-hepatitis C virus Metabolites of 2,6-Diaminopurine Ribonucleoside Prodrug Compared to Sofosbuvir and BMS-986094
ABSTRACT Ribonucleoside analog inhibitors (rNAI) target the hepatitis C virus (HCV) RNA-dependent-RNA polymerase non-structural protein 5B (NS5B) and cause RNA chain-termination. Herein, we expand our studies on β-D-2’ -C-methyl-2,6-diaminopurine-ribonucleotide (DAPN)...
ROR Modulators and Their Uses
ABSTRACT There are high unmet medical needs in the few established therapies for several autoimmune, inflammatory and metabolic diseases. Despite the diverse clinical manifestations of these diseases, Retinoic Acid Receptor-Related Orphan Receptors (RORs) regulate and...
The Flavone Luteolin Inhibits Liver X Receptor Activation
ABSTRACT Luteolin is a dietary flavonoid with medicinal properties including antioxidant, antimicrobial, anticancer, antiallergic, and anti-inflammatory. However, the effect of luteolin on liver X receptors (LXRs), oxysterol sensors that regulate cholesterol...
Effects of cranberry extracts on gene expression in THP-1 cells
ABSTRACT Cranberry contains high levels of nutrients and bioactive molecules that have health-promoting properties. The purpose of the present studies was to determine if cranberry extracts (CEs) contain phytochemicals that exert anti-inflammatory effects. The human...
Biotransformation of the mineralocorticoid receptor antagonists spironolactone and canrenone by human CYP11B1 and CYP11B2: Characterization of the products and their influence on mineralocorticoid receptor transactivation
ABSTRACT Spironolactone and its major metabolite canrenone are potent mineralocorticoid receptor antagonists and are, therefore, applied as drugs for the treatment of primary aldosteronism and essential hypertension. We report that both compounds can be converted by...
Anti-diabetic effect of 3-hydroxy-2-naphtoic acid, an endoplasmic retiulum stress-reducing chemical chaperone
ABSTRACT Lots of experimental and clinical evidences indicate that chronic exposure to saturated fatty acids and high level of glucose is implicated in insulin resistance, beta cell failure and ultimately type 2 diabetes. In this study, we set up cell-based...