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Modulating protein stability specifically inhibiting
2020-11-24
Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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WES and validation by Sanger
2020-11-23
WES and validation by Sanger sequencing in PNGS-252 revealed an apparent homozygous c.4C>G missense alteration (GenBank: NM_014176.3), resulting in the amino rq 1 australia substitution p.Gln2Glu (Figure 1A). This mutation must be very rare, because this is not listed in the NHLBI Exome Sequencing
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The component E of PDHc PDHc E catalyzes the
2020-11-23
The component E1 of PDHc (PDHc-E1) catalyzes the first step of multistep processes, using thiamine diphosphate (ThDP) and Mg2+ as cofactors.15, 16 Especially, this PDHc-E1 catalyzed process is a rate limiting step among multistep processes. Accordingly, the PDHc should be inactive by inhibiting the
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Several studies have indicated that ICT induces activation o
2020-11-23
Several studies have indicated that ICT induces activation of ERK and p38 kinase in a variety of cells. The ERK pathway was involved in and partly contributed to the neuroprotective effects in rat neuronal vps34 [14] and anticancer effects in several cancer cells [5], [7], [8]. ICT could also simul
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It is well known that
2020-11-23
It is well known that, nanostructured transition metal oxides are the most promising candidates as electrode for pseudocapacitors due to their attractive properties such as environmentally friendly, high theoretical capacitance, low cost and easily abundant [15], [16]. Numerous investigations have b
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Introduction Mycobacterium leprae the causative agent of lep
2020-11-23
Introduction Mycobacterium leprae, the causative agent of leprosy, affects skin, peripheral nerves and upper respiratory tract [1]. Although leprosy has been eradicated from most of the countries, it still affects approximately a quarter of a million people from India [2]. Details of many bacteriol
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A novel series of DHODH inhibitors was developed by
2020-11-23
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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br Acknowledgements br Membrane bound proton translocating i
2020-11-23
Acknowledgements Membrane-bound proton-translocating inorganic pyrophosphatases (H-PPase; EC 3.6.1.1) belong to a recently identified category of proton pumps, distinct from F-, P-, and V-ATPases, which utilize pyrophosphate hydrolysis as the driving force for H movement across biological membr
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Although it is believed that CYP induction is regulated
2020-11-23
Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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In contrast to chordates authentic chemokine
2020-11-23
In contrast to chordates, authentic chemokine and receptor orthologues can be found in the agnathan fishes (Bajoghli, 2013, Kuroda et al., 2003, Nomiyama et al., 2011, Nomiyama et al., 2013); sea lamprey has at least five chemokine receptor genes, one CXCR4 (Ensembl Acc. No.: ENSPMAP00000007678) (Ku
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20(S)-Hydroxycholesterol australia As previously stated the
2020-11-23
As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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hUcn II influence on MAP is
2020-11-23
hUcn II influence on MAP is mediated by the activation of CRF2 receptors. In vitro binding studies established that hUcn II is a selective ligand for CRF2 receptors with a slightly higher affinities for CRF2β compared with CRF2α and low or no affinity for CRF1 receptor [13], [19], [24]. Recent in vi
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br Results and discussion br
2020-11-23
Results and discussion Conclusion In this research, several anti-inflammatory agents with pyrazolo[3,4-d]pyrimidine cores were synthesized. Such choice of large core than regular pyrazole was valid as a proper modification. That most of the prepared compounds showed excellent AI activity. In a
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The effect of the simple
2020-11-23
The effect of the simple dopaminergic tonic/phasic model on cognitive processing has been investigated by a few studies (Nolan et al., 2004; Rosa et al., 2010). Rosa et al. (2010), using a Stroop task that requires different levels of cognitive flexibility and stability, observed an association betw
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Another significant finding in our study was the demonstrati
2020-11-23
Another significant finding in our study was the demonstration that the axon-protective action associated with CK2 inhibition correlated with preservation of mitochondrial structure and function in T16Ainh - A01 (Fig. 11). Because of the consistent protection conferred by CK2 inhibition during OGD,
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