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br A brief history of RBR E
2020-09-14

A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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A growing number of other post translational modifications a
2020-09-14

A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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Aprepitant In conclusion our results demonstrate that
2020-09-14

In conclusion, our results demonstrate that CCLP promoted osteoblast proliferation, differentiation, and mineralization via activation of ERK, p38, and Smad1/5/8 (Fig. 9). The residues of the GGKQNVGFGP-sequence in CCLP showed the highest significant binding relationship with the target activin rece
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Introduction Amphetamine AMPH methamphetamine MA and ethylen
2020-09-14

Introduction Amphetamine (AMPH), methamphetamine (MA), and 3,4-ethylenedioxymethamphetamine (MDMA) are widely abused psychoactive substances, with the basic chemical structure of phenylethylamine [1]. The abuse of these drugs is associated with psychostimulant, anorectic and hallucinogenic properti
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The present study was set to
2020-09-14

The present study was set to characterise the DNMT gene orthologs and describe the expression patterns of these genes during seed development in natural diploid apomict B. divaricarpa and diploid sexual B. stricta. Material and methods Results The B. stricta genome v1.2, was sequenced and ass
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Compound was advanced to a chronic efficacy study in db
2020-09-14

Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, CHIR-090 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily fo
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Multiple protein species are known to naturally exist
2020-09-14

Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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br Results br Discussion The structures
2020-09-14

Results Discussion The structures presented here were solved at high Deacetylase Inhibitor Cocktail 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 con
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The positive correlation between ATG and DCTPP TCGA
2020-09-14

The positive correlation between ATG7 and DCTPP1 (TCGA data) suggested our hypothesis that DCTPP1 may affect the phenotype of prostate tumor, or maybe other types of tumors as well, through its role in autophagy. To test this hypothesis, we carried out western-blot experiments in which the ratios of
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Compounds and administered orally to fasted Harlan Sprague D
2020-09-14

Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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Investigations of mice lacking up to three CDKs
2020-09-14

Investigations of mice lacking up to three CDKs identified the mitosis-regulating kinase CDK1 as the main essential component for the cell cycle, whereas ablation of other Peramivir regulators such as CDK2, CDK4, or CDK6 did not result in defective proliferation 12, 13. Mouse models and specific CD
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Introduction We have recently identified that caseinkinase C
2020-09-11

Introduction We have recently identified that caseinkinase 2 (CK2) inhibition protects white matter (WM) from ischemic injury. We focused our research on CK2 because upregulation of CK2 activity is associated with many diseases, including ischemic injury [1,[6], [7], [8]]. This review highlights an
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Although the analysis described above goes far to explain th
2020-09-11

Although the analysis described above goes far to explain the mechanism of Castanospermine sale perturbations through CHK1 inhibition, it raises important questions about the mechanism by which WT RAS isoforms promote CHK1 S280 phosphorylation. Previous reports have shown that both the MAPK-RSK and
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Given the potency enhancing effect
2020-09-11

Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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p and p which are downstream
2020-09-11

p21 and p16, which are downstream of pAkt and pERK1/2, are tumor suppressors which induce cell senescence and Kisspeptin 234 arrest [[56], [57], [58]]. Inhibitors of pAkt or pERK1/2 can activate p21 and p16 and promote cell senescence and cell cycle arrest [11,12,[59], [60], [61]]. It is well known
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