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Molecular modelling studies were performed on
2019-09-24
Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h
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Several research groups have disclosed potent and
2019-09-23
Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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Flexible alignment of isopropylphenylaminobenzimidazole with
2019-09-23
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead GSK 4112 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the other key funct
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Furthermore software engineering practices are important for
2019-09-23
Furthermore, software engineering practices are important for addressing productivity problems in scientific software. Even though the speed of the hardware is rapidly increasing, the additional complexity makes it more difficult for scientists to be productive developers. According to Faulk et al.,
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br Conflicts of interest br Acknowledgments This research wa
2019-09-23
Conflicts of interest Acknowledgments This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Science, ICT and Future Planning (NRF-2015R1A2A2A01004593). Introduction Resistance to Inhibitors of Cholinest
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The potential existence of ER stress was first
2019-09-23
The potential existence of ER stress was first examined in EVTs in placental bed biopsy specimens obtained from pregnancies complicated by early-onset preeclampsia. It was then tested whether ER stress can modulate MMP-2 activity before elucidating the role of proinflammatory cytokines in the induct
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Paclitaxel br A brief history of RBR E s RBR
2019-09-23
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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The first example of a broadly acting antiviral
2019-09-23
The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anot
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br NADH and NADPH Turnover and the
2019-09-23
NADH and NADPH Turnover and the Putative Role of Alternative NAD(P)H Dehydrogenases Still very little is known about the metabolic function of external and internal alternative NADH:UQ oxidoreductases, and almost nothing is known about the mechanisms underlying their metabolic regulation, especia
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An increasing body of evidence demonstrates that MXC can cau
2019-09-23
An increasing body of evidence demonstrates that MXC can cause neurobehavioral and neuropathological alterations [7]. In the brain, there are several steroidogenic enzymes, which are responsible for neurosteroid production. Neurosteroids are subsets of steroids that rapidly change neuronal excitabil
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CYP A is involved in the
2019-09-23
CYP3A is involved in the enzymatic Cy3 TSA clinical of many therapeutic agents [29]. The activity of BFCOD has been used to monitor CYP3A activity in humans [30], pigs [31], mice [32], and fish [23]. The predominant isoform expressed in the human liver is CYP3A4 [33]. In pigs, CYP3A29 contributes mo
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NADP/NADPH Quantitation Colorimetric Kit kinase The X ray cr
2019-09-23
The X-ray crystal structure of palbociclib bound to CDK6 without a NADP/NADPH Quantitation Colorimetric Kit kinase (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conforma
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Acknowledgements This work was supported in
2019-09-23
Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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Moreover a ligand for fusin has recently been found
2019-09-23
Moreover, a ligand for fusin has recently been found: the lymphocyte chemoattractant stromal-derived factor-1 (SDF-1) binds to CHO new transfected with fusin and promotes secondary messenger production (Bleul et al., 1996; Oberlin et al., 1996). A new name, CXCR-4, has been proposed for the receptor
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Our study demonstrated that the sequential
2019-09-23
Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565
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