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br Conclusion The development discovery of compounds targeti
2022-05-24
Conclusion The development/discovery of compounds targeting small GTPases is challenging [43,44]. Our data point to RBC8 being efficient and potent as a Ral inhibitor in human and mouse platelets, but that it exhibits some activity beyond just Rals, particularly in mouse platelets. It is however
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On the basis of the structure of
2022-05-24
On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a cyproheptadine hcl with Asp756 in ACAP2, while the methyl group is
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br Introduction Atherosclerosis is a chronic inflammatory di
2022-05-24
Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino Bedaquiline derivative derived from the metabolism of dietary methionine. Epidemiological studies have shown t
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With able to modulate inflammation and effect
2022-05-24
With ω3 able to modulate inflammation and effect obesity-related outcomes, it is of interested that two G-protein coupled receptors (GPCR), GPR120 and GPR40, were recently deorphanized and shown to recognize ω3 acids (docosahexaenoic, C22:6; eicosapentaenoic, C20:4; and α-linolenic, C18:3), as well
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LPCs have been previously described as potential anti
2022-05-23
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et a
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In this study we investigated the
2022-05-23
In this study, we investigated the contribution of GCK, G6PC, and PCK expression to glycemia in diabetes. We examined liver tissue from 40 obese subjects: 12 had normal glucose tolerance (NGT) and 28 had type 2 diabetes. Materials and methods Results Discussion This study aimed to investig
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The findings in mice were echoed in
2022-05-23
The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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br Material and methods br Results
2022-05-23
Material and methods Results and discussion Discussion It is well established that the guanosine-rich DNA sequences within telomeric DNA repeats, and in the promoter regions of a number of oncogenes or proto-oncogenes such as c-myc [20,23], VEGF [28,48,49] and Bcl-2 [21,50], can readily ass
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Also a large number of small
2022-05-23
Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [
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Occupying at least of brain volume astroglial cells not only
2022-05-23
Occupying at least 50% of K02288 receptor volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of synapses
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br Problem of cellular retention not
2022-05-23
Problem of cellular retention not only affects the cellular activity of the nanoparticles and nanocomplexes but can also have ramifications in their in vivo applications. While inorganic nanoparticles are being developed extensively for detection as well as treatment of different human diseases, i
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ampar Based on the inhibitory potency of C for HDAC
2022-05-23
Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o
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The H R antagonist JNJ developed by Johnson Johnson
2022-05-23
The H3R antagonist JNJ-17216498, developed by Johnson & Johnson, has entered clinical trial studies, but no information regarding its structure has been publicized to date. A phase II study of JNJ-17216498 monotherapy has been completed for patients with narcolepsy, but the results are not publicall
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To promote biomimetic growth of
2022-05-23
To promote biomimetic growth of HAp, Li et al. [20] developed a technique to modify cellulose nanofibers using P2O5. It was ascertained that the negative phosphate groups bonded with Ca2+ through coordination bonds and subsequently guided the growth of the Ca–P crystals throughout the scaffolds. Sim
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In the previous study concerning
2022-05-23
In the previous study concerning HO-1-mediated inhibtion of HCV replication, the mechanism underlying IFN-α/β indcuction by HO-1 involved in HO-1-catalyzed heme metabolic product, biliverdin (Zhu et al., 2010; Lehmann et al., 2010). However, in the present study SnPP, an inhibitor of HO-1 enzymatic
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