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A promising future for breast cancer therapy with hydroxamic acid-based histone deacetylase inhibitors.
Bioorg Chem
January 2025
Department of In Vitro Carcinogenesis and Cellular Chemotherapy, Chittaranjan National Cancer Institute, 37, S. P. Mukherjee Road, Kolkata 700026, India. Electronic address:
Histone deacetylases (HDACs) play a critical role in chromatin remodelling and modulating the activity of various histone proteins. Aberrant HDAC functions has been related to the progression of breast cancer (BC), making HDAC inhibitors (HDACi) promising small-molecule therapeutics for its treatment. Hydroxamic acid (HA) is a significant pharmacophore due to its strong metal-chelating ability, HDAC inhibition properties, MMP inhibition abilities, and more.
View Article and Find Full Text PDFChromatographic retention assisted in-silico prediction of anticancer potential of glucocorticoids on cancer cell lines.
J Chromatogr B Analyt Technol Biomed Life Sci
January 2025
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini St., Cairo 11562, Egypt.
Glucocorticoids (GCs) are hallmarks of anti-inflammatory activity. They are used as adjuvant therapy in oncology medications to alleviate some of the associated side effects. Although recent research has indicated that GCs have favorable anticancer potential, some scientific evidence suggests a pro-proliferation impact of GCs on cancer cells.
View Article and Find Full Text PDFRed blood cell urate levels are linked to hemolysis in vitro and post-transfusion as a function of donor sex, population and genetic polymorphisms in SLC2A9 and ABCG2.
Transfusion
January 2025
Department of Biochemistry and Molecular Genetics, University of Colorado Anschutz Medical Campus, Aurora, Colorado, USA.
Background: Storage of packed red blood cells (RBCs) for transfusion leads to biochemical and morphological changes, increasing hemolysis risk. Urate levels in blood bags at donation contribute to the molecular heterogeneity and hemolytic propensity of stored RBCs. However, studies to date have been underpowered to investigate at scale the contribution of donor demographics and genetics to the heterogeneity in urate levels across donations.
View Article and Find Full Text PDFEffect of Genetic Variants on Rosuvastatin Pharmacokinetics in Healthy Volunteers: Involvement of , and .
Int J Mol Sci
December 2024
Clinical Pharmacology Department, Hospital Universitario de La Princesa, Instituto de Investigación Sanitaria La Princesa (IIS-Princesa), 28006 Madrid, Spain.
Statins are the primary drugs used to prevent cardiovascular disease by inhibiting the HMG-CoA reductase, an enzyme crucial for the synthesis of LDL cholesterol in the liver. A significant number of patients experience adverse drug reactions (ADRs), particularly musculoskeletal problems, which can affect adherence to treatment. Recent clinical guidelines, such as those from the Clinical Pharmacogenetics Implementation Consortium (CPIC) in 2022, recommend adjusting rosuvastatin doses based on genetic variations in the and genes to minimize ADRs and improve treatment efficacy.
View Article and Find Full Text PDFPositioning Enzyme- and Transporter-Based Precipitant Drug-Drug Interaction Studies in Drug Design.
J Med Chem
January 2025
Department of Pharmacokinetics Dynamics & Metabolism, Pfizer Inc., Groton, Connecticut 06340, United States.
assessment of the potential of compounds to affect drug metabolizing enzymes and transporters and perpetrate drug-drug interactions (DDIs) is a common practice in drug research. For the development phase, regulators define an exhaustive list of enzymes and transporters to consider, but DDIs associated with many of these are minor and can be well-managed in the clinic; thus, progression of drug candidates that address unmet medical needs should not be curtailed due to this property. However, some enzymes and transporters are very important in drug disposition, so it is important to avoid/reduce inhibition or induction of these through drug design.
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