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br Identification of the kinase that phosphorylates
2022-11-16
Identification of the kinase that phosphorylates P450c17 The first Ser/Thr kinase that phosphorylates P450c17 was identified only recently. Of the 518 kinases in the human ‘kinome’ 278 are Ser/Thr kinases (Manning et al., 2002), but microarrays identified only 145 Ser/Thr kinases in human NCI-H29
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Zhang et al screened three thousand compounds library and
2022-11-15
Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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Previously using a P lacZ reporter gene system
2022-11-15
Previously, using a P-lacZ reporter gene system, it has been shown that the β-galactosidase activity was 9-fold higher in the stationary phase GSK503 when compared with those of the exponential phase [15]. Furthermore, inositol supplementation did not have a major effect on the expression of β-gala
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The allosteric site of class C
2022-11-14
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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At the outset of targeting the two Gln side chain
2022-11-14
At the outset of targeting the two Gln756 side-chain rotamers, it was unclear which rotational isomer would lead to more potent ASK1 inhibitors. While such a preference might have been anticipated, the cohort of ASK1 inhibitors in Table 3 did not provide any guidance regarding which of the Gln756 am
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Given that neither case is derived from multiplex families
2022-11-14
Given that neither case is derived from multiplex p-Cresyl sulfate with affected individuals, principles of Mendelian segregation cannot be applied to implicate the T201S mutation in causing familial CJD. In addition, like many rare gene variants, it is not possible to apply practice guidelines suc
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It has been well established
2022-11-14
It has been well established that shortly after systemic inflammation, NADPH oxidase and iNOS activity were increased in the G007-LK synthesis and lead to overproduction of reactive oxygen species (ROS) and NO [66]. Moreover, previous studies indicated that Ang II induced an increased level of NADP
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Thus far a tight coupling has been observed
2022-11-11
Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solub
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There are several reports providing evidences that functiona
2022-11-11
There are several reports providing evidences that functional and mechanistic connection between Sirt1 and LKB1/AMPK in metabolic regulation [26], [32], [33]. It has been reported that the deacetylation of LKB1 by Sirt1 is one of the determining factors of the subcellular localization of LKB1. In ag
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In the late s Solvay Pharmaceuticals
2022-11-09
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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br Materials and methods br Results and discussion br Conclu
2022-11-09
Materials and methods Results and discussion Conclusion Amino-functionalized mesoporous TiO2-NH2 microparticles were used to immobilize ADA, followed by GLU cross-linking. The mesopores provided a natural microenvironment with sufficient room for the enzyme to efficiently perform its cataly
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doxorubicin hydrochloride australia The difficulty of charac
2022-11-09
The difficulty of characterizing nAChRs in the central nervous system is also exemplified by early observations that nicotine caused no detectable effect when applied on a brain slice and it is only with the focal and high time resolution of more recent experiments that the effects of nicotinic neu
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br Conflict of interest br Acknowledgments This work was
2022-11-09
Conflict of interest Acknowledgments This work was been partially supported by the following grants: C.I.S.I.A. project (Innovazione e Sviluppo del Mezzogiorno—Conoscenze Integrate per Sostenibilità ed Innovazione del Made in Italy Agroalimentare—Legge 191/2009) from the Italian Ministry of Ec
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btk inhibitor Then Autodock was employed for site directed
2022-11-09
Then, Autodock4.2 was employed for site directed docking on AD with the ligands of the cluster(s) having high binding affinities in VS II experiment (Morris et al., 2009). Docking protocols were followed as per our earlier report with 200 GA (genetic algorithm) run (Kalani et al., 2015). Likewise, l
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br Conclusions A large body
2022-11-09
Conclusions A large body of evidence indicates that oxidative stress is involved in the pathogenesis of NDDs. Hence, reducing oxidative stress or suppressing its downstream pathways may be beneficial for the treatment of these diseases, especially such chronic diseases as AD or glaucoma. Here we
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