Πλοήγηση ανά Θέμα "enzyme inhibition"
Αποτελέσματα 1-20 από 41
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3 '-Axial CH2OH Substitution on Glucopyranose does not Increase Glycogen Phosphorylase Inhibitory Potency. QM/MM-PBSA Calculations Suggest Why
(2012)Glycogen phosphorylase is a molecular target for the design of potential hypoglycemic agents. Structure-based design pinpointed that the 3'-position of glucopyranose equipped with a suitable group has the potential to form ... -
4-Arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects
(2006)In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR ... -
Affinity crystallography reveals the bioactive compounds of industrial juicing byproducts of Punica granatum for glycogen phosphorylase
(2018)Background: Glycogen phosphorylase (GP) is a pharmaceutical target for the discovery of new antihyperglycaemic agents. Punica granatum is a well-known plant for its potent antioxidant and antimicrobial activities but so ... -
The ammonium sulfate inhibition of human angiogenin
(2016)In this study, we investigate the inhibition of human angiogenin by ammonium sulfate. The inhibitory potency of ammonium sulfate for human angiogenin (IC50 = 123.5 ± 14.9 mm) is comparable to that previously reported for ... -
The architecture of hydrogen and sulfur σ-hole interactions explain differences in the inhibitory potency of C-β-D-glucopyranosyl thiazoles, imidazoles and an N-β-D glucopyranosyl tetrazole for human liver glycogen phosphorylase and offer new insights to structure-based design
(2020)C-Glucopyranosyl imidazoles, thiazoles, and an N-glucopyranosyl tetrazole were assessed in vitro and ex vivo for their inhibitory efficiency against isoforms of glycogen phosphorylase (GP; a validated pharmacological target ... -
Chemical Characterisation-Biological Evaluation of Greek Cultivar Cardoon Seeds (Cynara cardunculus)A By-product with Potential High Added Value
(2021)Cynara cardunculus (artichoke) is a perennial plant of the Mediterranean basin, known since antiquity as food and for its therapeutic properties. Cynara is a relatively small genus with two cultivated species and one wild ... -
Chios mastic gum: A plant-produced resin exhibiting numerous diverse pharmaceutical and biomedical prοperties
(2012)Chios mastic gum (CMG) is a resin produced by the plant Pistacia lentiscus var. chia. CMG is used to extract the mastic gum essential oil (MGO). CMG and MGO consist of nearly 70 constituents and have demonstrated numerous ... -
A comparative analysis between proteasome and immunoproteasome inhibition in cellular and humoral alloimmunity
(2017)Triggered by the successful administration of the proteasome inhibitor bortezomib in kidney transplant recipients with acute or chronic antibody-mediated rejection, we evaluated the effect of the proteasome inhibitor ... -
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors
(2010)Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- ... -
Dietary effects of Sideritis scardica “mountain tea” on human in vivo activities of xenobiotic metabolizing enzymes in healthy subjects
(2018)Sideritis scardica (S. scardica) is an endemic plant of the Balkan Peninsula traditionally used as herbal tea for inflammation and gastric disorders. Aqueous herbal extracts may affect the activity of Phase I and II enzymes ... -
Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors
(2010)Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic ... -
Effect of Leguminosae family plant extracts and polyphenolic fractions on topoisomerase I-induced nicking of DNA
(2008)Topoisomerase I constitutes one of the enzymes playing crucial role in replication, transcription, recombination, chromosome condensation and maintenance of genome stability. Because it is an essential enzyme for vital ... -
Effects of grape extracts on the in vitro activity of enzymes involved in oxidative stress regulation
(2011)Background/Aim: A number of in vitro and in vivo studies have investigated the potential preventive activity of grape extracts against different diseases, and have mostly focused on their antioxidant properties. The present ... -
Effects of peppermint tea consumption on the activities of CYP1A2, CYP2A6, Xanthine Oxidase, N-acetyltranferase-2 and UDP-glucuronosyltransferases-1A1/1A6 in healthy volunteers
(2017)Peppermint leaves are widely used for the symptomatic treatment of digestive disorders. Previous studies have shown significant effects of its natural products on human enzyme activity; however, there is no study available ... -
Effects of short-term saffron (Crocus sativus L.) intake on the in vivo activities of xenobiotic metabolizing enzymes in healthy volunteers
(2019)Crocus sativus L., a perennial plant grown mainly around the Mediterranean and Iran, has many medicinal properties including anti-inflammatory, anti-depressive and cancer preventing properties. Aqueous herbal extracts may ... -
ERK1/2 phosphorylates HIF-2α and regulates its activity by controlling its CRM1-dependent nuclear shuttling
(2019)Hypoxia-inducible factor 2 (HIF-2) is a principal component of the cellular response to oxygen deprivation (hypoxia). Its inducible subunit, HIF-2α (also known as EPAS1), is controlled by oxygen-dependent as well as ... -
Functional characterization and anti-cancer action of the clinical phase II cardiac Na+/K+ ATPase inhibitor istaroxime: In vitro and in vivo properties and cross talk with the membrane androgen receptor
(2016)Sodium potassium pump (Na+/K+ ATPase) is a validated pharmacological target for the treatment of various cardiac conditions. Recent published data with Na+/K+ ATPase inhibitors suggest a potent anti-cancer action of these ... -
Glucopyranosylidene-spiro-imidazolinones, a New Ring System: Synthesis and Evaluation as Glycogen Phosphorylase Inhibitors by Enzyme Kinetics and X-ray Crystallography
(2019)Epimeric series of aryl-substituted glucopyranosylidene-spiro-imidazolinones, an unprecedented new ring system, were synthesized from the corresponding Schiff bases of O-perbenzoylated (gluculopyranosylamine)onamides by ... -
HIF-1α-derived cell-penetrating peptides inhibit ERK-dependent activation of HIF-1 and trigger apoptosis of cancer cells under hypoxia
(2019)Hypoxia is frequently encountered in the microenvironment of solid tumors. Hypoxia-inducible factors (HIFs), the main effectors of cell response to hypoxia, promote cancer cell survival and progression. HIF-1α, the ... -
Inhibition of the Na-H + exchanger isoform-1 and the extracellular signal-regulated kinase induces apoptosis: A time course of events
(2006)Aims: The present study attempts to shed light on the role and the relative position of the Na +/H + exchanger isoform 1 (NHE1) and the extracellular signal-regulated kinase (ERK) in HEp-2 cell signaling pathways concerning ...