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Funding sources This study was funded by European
2020-02-22

Funding sources This study was funded by European Community’s Seventh Framework Programme under grant agreement No. 305662 (Project: Community-based scheduled screening and treatment of malaria in pregnancy for improved maternal and infant health: a cluster-randomized trial ‘COSMIC’). Acknowledg
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melanin inhibitor br Methods br Results br Discussion
2020-02-22

Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3
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In conclusion our work provides the
2020-02-22

In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer prostaglandin receptor and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly
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Cubic equations of state CEoS are particularly
2020-02-22

Cubic equations of state (CEoS) are particularly popular due to their simplicity and relatively good accuracy in predicting vapour-liquid equilibrium and liquid-liquid equilibrium for small, non-polar, non-associating molecules, such as light hydrocarbons. CEoS can match the phase boundaries (L/LL a
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It was reported that IVM modulates
2020-02-22

It was reported that IVM modulates various ion channels, such as type-A GABACls, α7 acetylcholine-gated cation channels, P2X4 ATP-gated cation channels, and glycine-gated chloride IWR-1-endo receptor in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Zemko
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To study the effect of DDR inhibition by imatinib
2020-02-22

To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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Vinblastine sulfate We also note that though the
2020-02-22

We also note that though the Vinblastine sulfate of the N-terminus in Ube2E1∆N46 or the mutations in Ube2E16KtoR enhanced their activity compared to the wild type, it failed to match Ube2D2 (Fig. 1). We concluded this difference to be multi-factorial as none of the Ube2E1∆N46 point mutants involving
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br Results br Discussion Our
2020-02-22

Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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Analysis of Table shows that compound b in
2020-02-22

Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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However in many of the above
2020-02-21

However, in many of the above mentioned studies, the NaCl concentrations in the extraction buffers were different from those used here. For instance, in the study that performed cathepsin D extraction from human AD PBIT tissue, the concentration was 150mM [30], while that for the extraction of the c
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Why then is leading strand DNA
2020-02-21

Why then is leading-strand DNA synthesis reduced relative to lagging-strand synthesis in rad53-1 mutant Tenatoprazole under replication stress? To gain insight into this question, we first determined whether the firing of late origins in rad53-1 mutant cells contributes to compromised leading-strand
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br Author contributions br Conflicts
2020-02-21

Author contributions Conflicts of interest Introduction Current the 5-year survival rates for lung and pancreatic cancers are 18% and 8%, respectively. These low survival rates are partially because of the late diagnosis of one-half of cases, in which 5-year survival decrease to 4% and 3%,
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To identify and characterize new
2020-02-21

To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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br Funding This work was supported by the PACA Region
2020-02-21

Funding This work was supported by the PACA Region and Avignon Université. Acknowledgements Introduction Cancer is a pivotal health problem all over the world [1]. In spite of enormous advances achieved in diagnosis and treatment over the past decades, it still accounts for over 22000 deat
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br Materials and Methods br Acknowledgements
2020-02-21

Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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