Πλοήγηση ανά Θέμα "enzyme inhibition"
Αποτελέσματα 21-40 από 41
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Kinetics of inhibition of ribonuclease P activity by peptidyltransferase inhibitors: Effect of antibiotics on RNase P
(2003)A cell-free system derived from Dictyostelium discoideum has been used to study the kinetics of inhibition of RNase P by puromycin, amicetin and blasticidin S. Detailed kinetic analysis showed that the type of inhibition ... -
MacroDevelopment of an assay to assess genotoxicity by particulate matter extract
(2017)The current study describes a method for assessing the oxidative potential of common environmental stressors (ambient air particulate matter), using a plasmid relaxation assay where the extract caused single-strand breaks, ... -
Metabolism of isovanillin by aldehyde oxidase, xanthine oxidase, aldehyde dehydrogenase and liver slices
(2005)Aromatic aldehydes are good substrates of aldehyde dehydrogenase activity but are relatively poor substrates of aldehyde oxidase and xanthine oxidase. However, the oxidation of xenobiotic-derived aromatic aldehydes by the ... -
MYCing and YAPing the escape of tumor cell growth arrest after chronic PI3K/mTOR inhibition
(2017)[No abstract available] -
Nanomolar Inhibitors of Glycogen Phosphorylase Based on β- D -Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study
(2017)Aryl substituted 1-(β-d-glucosaminyl)-1,2,3-triazoles as well as C-β-d-glucosaminyl 1,2,4-triazoles and imidazoles were synthesized and tested as inhibitors against muscle and liver isoforms of glycogen phosphorylase (GP). ... -
Nicotinic cholinergic system and COVID-19: In silico identification of interactions between α7 nicotinic acetylcholine receptor and the cryptic epitopes of SARS-Co-V and SARS-CoV-2 Spike glycoproteins
(2021)SARS-CoV-2 is the coronavirus that originated in Wuhan in December 2019 and has spread globally. Studies have shown that smokers are less likely to be diagnosed with or be hospitalized for COVID-19 but, once hospitalized, ... -
On the immunoregulatory role of statins in multiple sclerosis: the effects on Th17 cells
(2019)Statins, the cholesterol-lowering drugs, also possess immunomodulatory properties, affecting among others T cell activation and differentiation, antigen presentation, and regulatory T cell (Tregs) maintenance and ... -
P38 MAPK signaling in pemphigus: Implications for skin autoimmunity
(2013)p38 mitogen activated protein kinase (p38 MAPK) signaling plays a major role in the modulation of immune-mediated inflammatory responses and therefore has been linked with several autoimmune diseases. The extent of the ... -
Pesticides and cardiotoxicity. Where do we stand?
(2018)Cardiovascular diseases are among the most significant causes of mortality in humans. Pesticides toxicity and risk for human health are controlled at a European level through a well-developed regulatory network, but ... -
Proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors to treat hypercholesterolemia: Effect on stroke risk
(2016)Background/purpose A reduction of cardiovascular events has been reported in phase 2 and 3 trials of the proprotein convertase subtilisin kexin 9 (PCSK9) inhibitors alirocumab and evolocumab. We aimed to investigate the ... -
The proteasome as a target for cancer treatment: Focus on bortezomib
(2005)Targeted degradation of key regulatory proteins is an essential element of cell-cycle control. The proteasome plays a pivotal role in the degradation of such proteins and has, therefore, become an important therapeutic ... -
Regulation of aromatase expression by hormones, drugs pesticides and environmental pollutants in canine mammary CMT-U27 cells
(2010)Aromatase, the enzyme that coverts testosterone to 17β-estradiol, has attracted attention lately because of its involvement in some forms of breast cancer in women. Studies are now undergoing on a variety of species to ... -
RNase P: A promising molecular target for the development of new drugs
(2004)RNase P is an ubiquitous and essential endonuclease in tRNA biogenesis, which generates the mature 5′-termini of tRNAs. RNase P activities have been identified in all three kingdoms of life (Bacteria, Archaea, Eukarya). ... -
The role of MiRNA-21 in gliomas: Hope for a novel therapeutic intervention?
(2020)Gliomas are the most common primary brain tumors in adults. They are generally very resistant to treatment and are therefore associated with negative outcomes. MicroRNAs (miRNAs) are small, non-coding RNA molecules that ... -
Specific inhibition of hif activity: Can peptides lead the way?
(2021)Reduced oxygen availability (hypoxia) is a characteristic of many disorders including cancer. Central components of the systemic and cellular response to hypoxia are the Hypoxia Inducible Factors (HIFs), a small family of ... -
Statins in bacteremia, sepsis and pneumonia: Have we found the holy grail?
(2009)Statins, beyond their lipid lowering properties, have pleiotropic properties that may modulate the inflammatory cascade and potentially could be useful in the management of inflammatory conditions such as bacteremia and ... -
Synthetic, enzyme kinetic, and protein crystallographic studies of C-β-D-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase
(2016)C-β-D-Glucopyranosyl pyrrole derivatives were prepared in the reactions of pyrrole, 2-, and 3-aryl-pyrroles with O-peracetylated β-D-glucopyranosyl trichloroacetimidate, while 2-(β-D-glucopyranosyl) indole was obtained by ... -
Testosterone and dihydrotestosterone modulate the redox homeostasis of endothelium
(2022)The predominance of cardiovascular diseases among men compared to premenopausal women has been attributed to testosterone, which is implicated in vascular remodeling. Molecular mechanisms underlying its role have not been ... -
Triazole double-headed ribonucleosides as inhibitors of eosinophil derived neurotoxin
(2015)Eosinophil derived neurotoxin (EDN) is an eosinophil secretion protein and a member of the Ribonuclease A (RNase A) superfamily involved in the immune response system and inflammatory disorders. The pathological actions ... -
Truncation and optimisation of peptide inhibitors of cyclin-dependent kinase 2-cyclin A through structure-guided design
(2009)The cyclin-dependent kinase 2-cyclin A complex is an important regulator of the DNA-synthesis phase of the mammalian cell cycle, which is frequently deregulated in cancer. Rather than blocking the ATP-binding site of the ...