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br The modulation of ER from SERMs to TSECs Continued
2021-05-14
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective ml7 receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, despite lack
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PF 04418948 We recently employed a functional drug screening
2021-05-14
We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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More than thirty enzymes with
2021-05-14
More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos
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Glycolysis is important to maintain the vital functions
2021-05-14
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its Volasertib metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress from host cel
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Previous studies have indicated that hSSB may
2021-05-13
Previous studies have indicated that hSSB1 may be phosphorylated at threonine residue 117 (T117) [13] and acetylated at lysine residue 94 (K94) [15], both of which promote hSSB1 function in response to ionising radiation exposure. Mass spectrometry screens of proteins immunoprecipitated with phospho
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br UVC induced DNA damage a model to
2021-05-13
UVC-induced DNA damage: a model to study DNA damage tolerance The UV components of sunlight that reaches the Earth surface are one of the most carcinogenic agents humans are exposed to, and the leading cause of skin cancer [4,12]. UV light causes different types of DNA damage through indirect and
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The larger eukaryotic ligases such as LigI
2021-05-13
The larger eukaryotic ligases, such as LigI and LigIV, also possess an additional N-terminal DNA-binding domain (DBD) that is required for efficient ligation (Fig. 1c) and enables these ligases to encircle DNA [17]. An equivalent helix–hairpin–helix domain is also present in the bacterial NAD-depend
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These data raised from human tissues suggested a
2021-05-13
These data raised from human tissues suggested a potential link between TGF-β1 signaling and linear invadosome machinery that may explain TGF-β involvement in HCC progression and invasion. Using HCC cultured cells, we confirmed that TGF-β1 stimulation increases the production and secretion of collag
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Some mechanistic experiments performed in the early s
2021-05-13
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects trifluoperazine hydrochloride from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apop
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Despite the significant associations between TNF and TRAIL
2021-05-13
Despite the significant associations between TNF-α and TRAIL in our results, the use of a single top cytokine in predicting sPTB is limited, and the previous study using the specific candidate cytokines failed to accurately predict the risk for sPTB in asymptomatic women, with AUC ranged from 0.48 t
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In addition to an action via
2021-05-13
In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se
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Dexamethasone DEX a potent synthetic glucocorticoid
2021-05-13
Dexamethasone (DEX), a potent synthetic glucocorticoid drug, is effective for treatment of a range of inflammatory and autoimmune conditions as well as the reduction of side effects associated with chemotherapy. On the Czech Republic pharmaceutical market, DEX is incorporated into eighteen drugs use
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Preliminary studies evidenced the presence of CRFr in gamma
2021-05-13
Preliminary studies evidenced the presence of CRFr in gamma-aminobutyric acid-ergic (GABAergic) neurons of the hippocampus (Yan et al., 1998). In fact, in this JSH-23 receptor area, CRF inhibits glutamate release through CRF1r (Bagosi et al., 2015), leading to a decrease in the GABA concentration i
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Previous studies from our laboratory in
2021-05-13
Previous studies from our laboratory in CD1 mice using the incisional postoperative pain model have shown that the incision induces significant mechanical postoperative hyperalgesia lasting between 7 and 10days, with peak effect between 4h-2days (Cabañero et al., 2009a, Cabañero et al., 2009b, Campi
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IAA sensitive Cl channels were
2021-05-13
IAA-94-sensitive Cl channels were shown to mediate cardioprotection due to IPC (Diaz et al., 1999) and cyclosporine A (Diaz et al., 2013). CLIC-like channel activity was also observed in cardiac mitoplast (Misak et al., 2013) but the molecular identity of these intracellular Cl channels and their pr
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