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Compounds were profiled for their inhibitory activity agains
2022-11-01

Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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br LOX in pancreatic cancer LOX is a key
2022-11-01

5-LOX in pancreatic cancer 5-LOX is a key player in pancreatic cancer (PC) progression. The upregulation of 5-LOX mRNA has been observed in pancreatic adenocarcinoma (PDAC) and also in neoplastic pancreatic tissues (Kennedy et al., 2003). Higher levels of 5-LOX transcripts (messengers) are presen
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ret proto oncogene br Results br Discussion Our finding
2022-11-01

Results Discussion Our finding that AXL overexpression is significantly associated with poor survival in patients with high-grade serous OC is consistent with previous reports indicating that AXL regulates tumor growth in some cancers, as well as reports showing that AXL activity is involved i
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Fencilli et al reported derivatives of PHA
2022-11-01

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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To maintain ATP levels postmortem muscle mobilizes its glyco
2022-11-01

To maintain ATP levels, postmortem muscle mobilizes its glycogen reserves to yield glatiramer acetate 6-phsphate that proceeds through glycolysis. Glycogen degradation was affected by the interaction between treatment and time (Pinitiation of the experiment. We expected that if myosin ATPase is li
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In this study we have isolated genes
2022-11-01

In this study, we have isolated VER155008 that encode ACL from G. zeae through random mutagenesis by restriction enzyme-mediated integration (REMI). The mutant Z39P186 where the ACL gene had been disrupted showed defects in vegetative growth, asexual and sexual development, virulence, and trichothe
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br Summary br Introduction With readily synthetic methods an
2022-11-01

Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually, o
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In this study we have generated
2022-10-31

In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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In conclusion we demonstrated that in the
2022-10-31

In conclusion, we demonstrated that, in the skeletal muscle of rats with T1DM, CRBN levels increased and AMPK, Akt, GLUT4, PGC-1α, and FNDC5 levels decreased, resulting in increased fasting glucose levels. Aerobic exercise training decreased levels of CRBN, which was possibly mediated by AMPK, Akt,
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Among all the compounds the novel
2022-10-31

Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The Boc-D-FMK receptor 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91
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leukotriene receptor antagonists A more versatile cellular d
2022-10-31

A more versatile cellular delivery system for adenosine was generated by engineering mouse embryonic stem cells to lack both leukotriene receptor antagonists of Adk (Fedele et al., 2004). Using a step-wise differentiation protocol (Okabe et al., 1996) Adk−/− ES cells were differentiated into transp
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br Introduction br Rac dependent ROS
2022-10-31

Introduction Rac1-dependent ROS and tranylcypromine regulation in neuronal functions NOX-mediated ROS have an important role as physiological messengers. One remarkable example regarding such a function is during axonal formation. In this line, increased p40phox/NOX2 levels and co-localizatio
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Application of the broad acting HTR antagonist methiothepin
2022-10-31

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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Several dehidropregnenolone derivatives functionalized at C
2022-10-31

Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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NOXA a BH only protein is best known as a
2022-10-31

NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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