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showing 10 items of 6731 documents
The Functional Role of the Second NPXY Motif of the LRP1 β-Chain in Tissue-type Plasminogen Activator-mediated Activation of N-Methyl-D-aspartate Rec…
2008
The low density lipoprotein receptor-related protein 1 (LRP1) emerges to play fundamental roles in cellular signaling pathways in the brain. One of its prominent ligands is the serine proteinase tissue-type plasminogen activator (tPA), which has been shown to act as a key activator of neuronal mitogen-activated protein kinase pathways via the N-methyl-D-aspartate (NMDA) receptor. However, here we set out to examine whether LRP1 and the NMDA receptor might eventually act in a combined fashion to mediate tPA downstream signaling. By blocking tPA from binding to LRP1 using the receptor-associated protein, we were able to completely inhibit NMDA receptor activation. Additionally, inhibition of …
Oxidative Stress, Induced by Sub-Lethal Doses of BDE 209, Promotes Energy Management and Cell Cycle Modulation in the Marine Fish Cell Line SAF-1
2019
The effects of sub-lethal doses of polybrominated diphenyl ether (PBDE)-209 in terms of toxicity, oxidative stress, and biomarkers were evaluated in the Sparus aurata fibroblast cell line (SAF-1). Vitality and oxidative stress status were studied after incubation with PBDE for 72 h. Concomitantly, the quantification of proteins related to cell cycle and DNA repair (p53), cell proliferation (extracellular signal&ndash
Comparative analysis of virtual screening approaches in the search for novel EphA2 receptor antagonists
2015
The EphA2 receptor and its ephrin-A1 ligand form a key cell communication system, which has been found overexpressed in many cancer types and involved in tumor growth. Recent medicinal chemistry efforts have identified bile acid derivatives as low micromolar binders of the EphA2 receptor. However, these compounds suffer from poor physicochemical properties, hampering their use in vivo. The identification of compounds able to disrupt the EphA2-ephrin-A1 complex lacking the bile acid scaffold may lead to new pharmacological tools suitable for in vivo studies. To identify the most promising virtual screening (VS) protocol aimed at finding novel EphA2 antagonists, we investigated the ability of…
Sub-lethal doses of polybrominated diphenyl ethers affect some biomarkers involved in energy balance and cell cycle, via oxidative stress in the mari…
2019
Abstract Polybrominated diphenyl ethers (PBDEs) are a class of persistent contaminants which are found all over the world in the marine environment. Sparus aurata fibroblast cell line (SAF-1) was exposed to increasing concentrations of PBDEs 47 and 99, until 72 h to evaluate the cytotoxicity, reactive oxygen species (ROS) production and the expression of some selected molecular markers related to cell cycle, cell signaling, energetic balance and oxidative stress (p53, erk-1, hif-1α and nrf-2), by real-time PCR. Furthermore, SAF-1 cells were exposed for 7 and 15 days to sub-lethal concentrations, in order to evaluate the response of some biomarkers by immunoblotting (p53, ERK-1, AMPK, HIF-1α…
Pyridinedicarboxylates, the first mechanism-derived inhibitors for prolyl 4-hydroxylase, selectively suppress cellular hydroxyprolyl biosynthesis. De…
1987
Two pyridinedicarboxylates, predicted [Hanauske-Abel (1983) M.D.-Ph.D. Thesis, Philipps Universität Marburg] and later found to be potent reversible inhibitors of purified prolyl 4-hydroxylase [Majaama, Hanauske-Abel, Günzler & Kivirikko (1984) Eur. J. Biochem. 138, 239-245] were investigated with respect to their effect on hydroxyprolyl biosynthesis in the fibroblast/collagen and the macrophage/Clq systems, and the effect was compared with that of the iron chelator 2,2′-dipyridyl, the compound usually employed to inhibit cellular hydroxyprolyl formation. Only the enzyme-mechanism-derived pyridinedicarboxylates were highly selective inhibitors, and only they lacked overt cytotoxicity. M…
Synthesis, spectroscopic studies and biological evaluation of acridine derivatives: The role of aggregation on the photodynamic efficiency.
2018
Two new photoactive compounds (1 and 2) derived from the 9-amidoacridine chromophore have been synthesized and fully characterized. Their abilities to produce singlet oxygen upon irradiation have been compared. The synthesized compounds show very different self-aggregating properties since only 1 present a strong tendency to aggregate in water. Biological assays were conducted with two cell types: hepatoma cells (Hep3B) and human umbilical vein endothelial cells (HUVEC). Photodynamic therapy (PDT) studies carried out with Hep3B cells showed that non-aggregating compound 2 showed photoxicity, ascribed to the production of singlet oxygen, being aggregating compound 1 photochemically inactive.…
Cell-Free Coelomic Fluid Extracts of the Sea Urchin Arbacia lixula Impair Mitochondrial Potential and Cell Cycle Distribution and Stimulate Reactive …
2020
Triple-negative breast cancer (TNBC) is a highly malignant tumor histotype which lacks effective targeted therapies, thereby being considered as the most aggressive form of breast carcinoma. To identify novel compounds which could counteract TNBC cell growth, we explored the in vitro effects of crude extracts and <
Pyrrolo[2',3':3,4]cyclohepta[1,2-d][1,2]oxazoles, a New Class of Antimitotic Agents Active against Multiple Malignant Cell Types
2020
A new class of pyrrolo[2',3':3,4]cyclohepta[1,2-d][1,2]oxazoles was synthesized for the treatment of hyperproliferative pathologies, including neoplasms. The new compounds were screened in the 60 human cancer cell lines of the NCI drug screen and showed potent activity with GI50 values reaching the nanomolar level, with mean graph midpoints of 0.08-0.41 μM. All compounds were further tested on six lymphoma cell lines, and eight showed potent growth inhibitory effects with IC50 values lower than 500 nM. Mechanism of action studies showed the ability of the new [1,2]oxazoles to arrest cells in the G2/M phase in a concentration dependent manner and to induce apoptosis through the mitochondrial…
Hemin induces germ tube formation in Candida albicans.
1997
Hemin induced germination of Candida albicans blastoconidia when cells grown up to the early exponential phase were shifted from 28 to 37 degrees C (70 to 75% of cells exhibited germ tubes). N-Acetyl-D-glucosamine (GlcNAc), another inducer of myceliation in this fungus, caused a similar effect. The combination of hemin and GlcNAc resulted in a higher percentage (95%) of blastoconidial germination. These results suggest that in addition to temperature, hemin levels and carbon source may coordinately regulate the expression of subsets of genes involved in the yeast-to-mycelium transition in C. albicans.