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By secreting proteases such as cathepsins and matrix metalloproteinases (MMPs), macrophage foam cells may be a major cause of ruptured atherosclerotic plaques. The aims of the present study were to investigate in vitro role of human macrophage foam cells in degrading type I collagen, a major...
The aim of our work was to establish flow cytometry methods for the characterization of mitochondrial Ca 2+ levels, plasma membrane potential, and superoxide generation and to relate kinetics to that of cytoplasmic Ca 2+ levels during short-term activation of T-lymphocytes. We monitored the...
Traditional drug discovery efforts have resulted in the approval of a handful of receptor tyrosine kinase (RTK) inhibitors; however, their discovery relied solely on screening recombinant kinases, often with poor cellular activity outcome. The ability to screen RTKs in their natural environment...
In vitro chemosensitivity assays are invaluable for assessing chemotherapeutic agents' effects on cancer cells. Yet the dose–response curves generated by those assays, usually approximated by four-parameter logistic (4PL) models, are oftentimes difficult to interpret, with no clear indication...
Hepatotoxicity is a major concern for both drug development and toxicological evaluation of environmental chemicals. The assessment of compound-induced hepatotoxicity has traditionally relied on in vivo testing; however, it is being replaced by human in vitro models due to an emphasis on the...
Interactions with extracellular matrices (ECM) shape the signaling and functions of many types of cells and receptors, and distinct ECM coatings have been used in a wide range of substrates for drug discovery processes. Here, we investigate the influence of ECM protein coatings on the signaling...
Agonist-induced glucocorticoid receptor (GR) transport from the cytoplasm to the nucleus was used as a model to identify dynein-mediated cargo transport inhibitors. Cell-based screening of the library of pharmacologically active compound (LOPAC)-1280 collection identified several small molecules...
The emergence and spread of multidrug-resistant Plasmodium falciparum and recent detection of potential artemisinin-resistant strains in Southeast Asia highlight the importance of developing novel antimalarial therapies. Using a previously generated stable transgenic P. falciparum line with...
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