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Introduction br CK in the
2020-06-04
Introduction CK1 in the Regulation of Hh Pathway CK1 was initially identified as a negative regulator of Hh signaling at the level of transcription factor Ci by genetic studies in Drosophila and genome-wide RNAi screen in Drosophila cultured GSK 2830371 synthesis (Jia et al., 2005, Lum et al.,
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Propranolol initially discovered in is first
2020-06-04
Propranolol, initially discovered in 1964, is first and most widely studied as a non-selective beta-blocker. Propranolol through β-adrenergic receptor blockade has reduced heart rate and blood pressure and have anti-arrhythmogenic and anti-ischemic effects, and been proposed as an effective strategy
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Interest in DGKs increased as
2020-06-03
Interest in DGKs increased as it became clear that not only are they important for lipid homeostasis, they serve to modulate the relative levels of diacylglycerol (DAG) and phosphatidic Entrectinib (PtdOH) that play critical roles in a variety of signaling pathways (Eichmann and Lass, 2015; Liu et
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For the SAR optimization of
2020-06-03
For the SAR optimization of the right hand side, it was decided to explore the inclusion of the key carboxylic SirReal2 synthesis moiety present in the original DGAT-1 inhibitors from . Analogs were constructed by the synthetic routes outlined in , . In , the methylene-oxy linker was introduced by
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Alvocidib flavopiridol is a piperidine chromenone http www
2020-06-03
Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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Many studies have used paradigms based on
2020-06-03
Many studies have used paradigms based on animal models to understand human emotional behavior because it appears to be correlated with fear- and anxiety-related defensive patterns in non-human mammals (Blanchard et al., 2001). In this case, defensive reactions are used to study the neural substrate
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This approach is similar to
2020-06-03
This approach is similar to that suggested by the previous edition of the GL [6]. Not surprisingly, the questions to be answered are the same (i.e., was the event TLOC? In cases of TLOC, is this R 59-022 sale of syncopal or non-syncopal origin? In cases of suspected syncope, is there a clear aetiol
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UVRAG is a mammalian ortholog of yeast
2020-06-03
UVRAG is a mammalian ortholog of yeast Vps38 and a promoter of autophagy [51,60,61]. It forms distinct complexes with BECN1 (mammalian ortholog of yeast Vps30/Atg6) and the class III phosphatidylinositol 3-kinase (whose catalytic subunit [PIK3C3] is the mammalian ortholog of yeast Vps34) and contrib
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br Acknowledgements Professor Olli A J nne is warmly
2020-06-03
Acknowledgements Professor Olli A. Jänne is warmly thanked for support and for providing excellent research facilities. Professor Patrik Finne is acknowledged for his help with statistical analyses. Drs Ronald Evans, Vincent Giguère, Jorma Palvimo, Malcolm Parker, and Anastasia Kralli are acknowl
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Although it was shown that IL signaling
2020-06-03
Although it was shown that IL-23 signaling induces expression of T17 pathogenic signature genes through activation of STAT3,, transcription factors other than STAT3 are also implicated for induction of pathogenic T17 cells because IL-6, which activates STAT3 similarly to IL-23, cannot induce IL-23R
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Despite the fact that the
2020-06-03
Despite the fact that the precise relevance of Ube2E self-ubiquitination in vivo is still elusive, findings of Sarkari et al. do establish Ube2E1 ubiquitination in 740 Y-P [36]. In vivo self-ubiquitination of Ube2E1 is further supported by the high-throughput study aimed to identify all ubiquitinate
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br Conflicts of interest br Introduction
2020-06-03
Conflicts of interest Introduction G protein-coupled receptors (GPCRs), form the largest human membrane protein family, with 800 members overall. Many druggable targets for treatment of common diseases involve GPCRs that mediate therapeutic effects of 34% of all marketed drugs (Hauser, Attwood
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br Mammalian DGKs current knowledge Despite our understandin
2020-06-03
Mammalian DGKs: current knowledge Despite our understanding of prokaryotic DGKs, our limited understanding of the structure of mammalian DGKs is a major gap in our knowledge. Importantly, major differences exist between prokaryotic and mammalian enzymes often revealing the fact that structural fe
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br Enzymes involved in microbial steroid degradation
2020-06-03
Enzymes involved in microbial steroid degradation are generally not expressed constitutively, but they are upregulated depending on which steroid substrates are present [17,81]. Thus, a cell-free extract prepared from testosterone-adapted C. testosteroni ATCC 11996 cells displayed a 1(2)-dehydroge
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As illustrated in Table monocyclic acid
2020-06-02
As illustrated in Table 3, monocyclic SCH772984 TFA analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9 exhibited nearly
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