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Hymenialdisine the most potent inhibitor
2020-08-12
Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this Sumatriptan also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of CDK
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In the horse oviduct the EP
2020-08-12
In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial Flurbiprofen particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely reflects differen
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For immobilization of enzymes natural polymers depict
2020-08-12
For immobilization of enzymes, natural polymers depict several outstanding features as support. These materials are inert, non-toxic, biodegradable and biocompatible. As well as, they can be treated with different functional groups easily by chemical reactions that occur under gentle conditions in a
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Nitrid oxide NO and its potential endogenous production as a
2020-08-12
Nitrid oxide (NO) and its potential endogenous production as an endothelium-derived factor was the first gaseous molecule accepted to be a signaling mediator in the organism [4,5]. NO plays a key role in physiological regulation of the crizotinib and exerts physiological functions in the nervous an
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Further indirect evidence supporting an important role
2020-08-11
Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc
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In contrast to the methylation that is catalyzed
2020-08-11
In contrast to the methylation that is catalyzed exclusively by DNMTs, there have been suggested several pathways that could induce demethylation (Watt & Molloy, 1988). However, the existence and influencing of enzymes that promote active demethylation remains elusive. Studies aiming to gain more in
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br Results br Discussion The
2020-08-11
Results Discussion The structures presented here were solved at high Chromocarb and show in detail how DDR1 achieves high affinity for imatinib and ponatinib, respectively. Both type II inhibitors bind in their more potent extended conformations to the inactive DFG-out conformation of the kin
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br Application of the screening system for ITP binding prote
2020-08-11
Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human chloride channels because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or
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R 59-022 Introduction Cytochrome P CYP A
2020-08-11
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The R 59-022 level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A mul
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Interestingly ASV infusion in the dRN of saline pre treated
2020-08-11
Interestingly, ASV-30 infusion in the dRN of saline pre-treated rats had no effect on anxiety-like behaviors. This result may be due to the saline pre-treated group exhibiting relatively low levels of anxiety-like behaviors (when compared to saline pre-treated rat of the first experiment that were n
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One of the therapeutic proteins used in cancer therapy
2020-08-11
One of the therapeutic proteins used in cancer therapy is glucarpidase, also known as Carboxypeptidase G2, CPG2, which originates from the bacterium Variovorax paradoxus (old name, Pseudomonas sp. strain RS-16). It has no mammalian equivalent (Thompson et al., 1994; Kamlage, 1994) and is a zinc-depe
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Introduction Human cytomegalovirus CMV is
2020-08-11
Introduction Human cytomegalovirus (CMV) is a herpesvirus which has a ubiquitous and worldwide distribution, and is the most frequent cause of congenital infection (Kenneson and Cannon, 2007). The prevalence is around 0.5–1% of all live births and is the leading cause of sensorineural hearing loss
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perindopril erbumine Two additional hydrogen bonds are forme
2020-08-11
Two additional hydrogen-bonds are formed by the -substituted methoxy-group with Ser and Asp. Ser exerts the role of a gate keeper in CK1: Entry of the ATP in the binding-site causes a conformational change into the closed form by Ser, which locks the binding-site and prevents ATP-diffusion out of th
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br Experimental Procedures br Author Contributions
2020-08-11
Experimental Procedures Author Contributions H.G. and X.-Y.F. conceived and designed the project. H.G., D.V.D., and X.L. performed most of the experiments and analyzed the data. L.X. helped on Mettl8 KO ESC, RIP, and translational study. Y.S. performed FACS analysis. Y.W. helped with cardiomyo
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Another milestone in the field is the de novo
2020-08-11
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of KH CB19 , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways and biol
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