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One may carefully evaluate the concept pancreas derived GLP
2022-04-15
One may carefully evaluate the concept ‘pancreas derived GLP-1′ as this may dependent on the specificity of the BI-9564 used in immunohistochemistry or radiommunoassays. If either a side-viewing antibody or a C-terminal wrapping antibody raised against GLP-1 is applied one may also identify N-termi
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br Voltage dependent anion channel
2022-04-15
Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially
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There are multiple docking platforms suitable for use with n
2022-04-15
There are multiple docking platforms suitable for use with nucleic Dehydroepiandrosterone receptors. These include: DOCK v4-6 (UCSF) [[68], [69], [70]], AutoDock (Scripps) [71], AutoDock Vina (Scripps) [72], GOLD (Cambridge Crystallographic Data Centre) [73], Surflex-DOCK (BioPharmics) [74], Glide (
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The results obtained here in int Gr
2022-04-15
The results obtained here in int-Gr+/+ and int-Gr−/− mice suggested that Gr is required to maintain basal level of Fgf15 expression in the ileum, whereas DEX treatment is able to reduce Fgf15 mRNA in a Gr-independent manner. In previous in vitro studies we have already shown that GC are able to affe
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One effective approach to fine tuning
2022-04-15
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Dabrafenib receptor scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as we
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Taken together our studies uncovered that
2022-04-15
Taken together, our studies uncovered that the RP215 antibody recognize a novel CIgG molecule N-glycan modification at a non-consensus site within the CH1 domain expressed in LSCC tumors. RP215-CIgG interacts with the integrin α6β4 complex and the unique N-glycan epitope mediates the activation of d
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EZH interaction with HADC and HDAC through the
2022-04-15
EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic Roflumi
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Receptor guanylyl cyclases play essential roles in cardiovas
2022-04-14
Receptor guanylyl cyclases play essential roles in cardiovascular and gastrointestinal (patho-)physiology, reproduction biology, cell proliferation, bone growth and sensory signal transduction and, therefore, are important pharmacological targets. Accordingly, the receptor guanylyl cyclase agonists
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Although some PAHs that are human carcinogens have been foun
2022-04-14
Although some PAHs that are human carcinogens have been found in the sugarcane soot (Zamperlini et al., 1997), there are no data about cancer incidence among sugarcane workers. To the best of our knowledge, this is the first report of an evaluation of internal exposure, comparing the harvesting (whe
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To further investigate the relationship between the pro
2022-04-14
To further investigate the relationship between the pro-neurogenic and therapeutic actions, we analyzed the effect of VP2.51 in the presence of the antimitotic agent TMZ. No overt side effects were found at the time of testing as assessed by direct observation of the behavior of the animals in their
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GPR shares a amino acid sequence identity in humans
2022-04-14
GPR81 shares a 52% amino AS1842856 sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capable o
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Overall this study provides compelling evidence that overexp
2022-04-14
Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i
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The compounds described in this paper were prepared
2022-04-14
The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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A-317491 Because of its excellent GPR potency
2022-04-14
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, A-317491 was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel o
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Disrupting the dialog between microbiota and the host especi
2022-04-14
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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