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In our previous study we designed and
2022-06-18
In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic Quizartinib (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro antitum
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According to literature RASs V M T S
2022-06-18
According to literature, RASs V36M, T54S, Q80K and R155K are considered primary resistance mutations to different PIs. RASs V36M and R155K can reduce susceptibility to recently approved PIs simeprevir, paritaprevir and grazoprevir [18], [31], [32]. T54S is associated to resistance for first-wave tel
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Immunohistochemical analysis of sheep skin sections showed t
2022-06-18
Immunohistochemical analysis of sheep skin sections showed that sGC prtotein is expressed in the hair follicles with different location and abundance between white and black sheep skin (Fig. 6). In white sheep skin, Strong sGC positive signal was detected in the upper hair dermal papilla but no posi
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Indeed GSTP mRNA appears to be already highly stable
2022-06-18
Indeed GSTP1-1 mRNA appears to be already highly stable in K562 leukemia SB431542 mg with a half-live of more then 40h which is even further increasing to 92h after hemin treatment and erythroid differentiation. Previous reports quantified GST mRNA half-lives which depend on the cellular model and t
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Although some PAHs that are human carcinogens have been
2022-06-18
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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It appears that not all
2022-06-17
It appears that not all GPR119 agonists require a high dose to elicit acceptable AZD0156 control. According to preclinical data presented at the GTCbio Diabetes Summit, a 3mg/kg dose of AR-7947 was enough to induce similar blood glucose-lowering effects compared to those achieved by 30mg/kg sitagli
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br Clinical development of anti NASH drug therapies The curr
2022-06-17
Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fie
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Based on work from our labs with mGlu NAMs
2022-06-17
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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lactacystin Previous reports have showed that the expression
2022-06-17
Previous reports have showed that the expression and localization of GLUT8 in mouse (Gómez et al., 2006; Kim and Moley, 2007), rat (Ibberson et al., 2002) and human (Schürmann et al., 2002). In this study, GLUT8 protein mainly localized in the spermatocytes, elongated and round spermatids in the adu
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The expression of GLUT receptors throughout the
2022-06-17
The expression of GLUT receptors throughout the body could be considered a potential source for off-target effects even for engineered glucose-conjugated nanomedicines, as there are at least 12 types of GLUT transporters in the body, including GLUT1 in erythrocytes and the blood-brain barrier, as we
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br Conflicts of interests br Acknowledgements We thank
2022-06-17
Conflicts of interests Acknowledgements We thank Drs. T. Tomita and T. Iwatsubo (Tokyo University, Tokyo, Japan) for anti-presenilin 1-CTF antiserum, Dr. A. Takashima (Gakushuin University, Tokyo, Japan) for anti-Pen-2 antiserum and the laboratory members for helpful comments and discussion. M
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br Experimental Procedures Information on the materials
2022-06-17
Experimental Procedures Information on the materials used in this study and the details of how the in vivo and in vitro assays were performed are provided in Supplemental Information. Acknowledgments This research was supported by the National Research Foundation of Korea (NRF) grant funded b
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br FPRs regulate anti microbial responses
2022-06-17
FPRs regulate anti-microbial responses The classic evidence supporting FPR as an anti-microbial receptor is that bacteria are the major biological source of chemotactic formyl peptides, fMLF binds to FPR and fMLF activates chemotactic and anti-microbial responses in neutrophils 2., 3.. Recently,
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Herein we report the discovery
2022-06-17
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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The RAS RAF MEK ERK pathway also known as the
2022-06-17
The RAS/RAF/MEK/ERK pathway (also known as the MAPK/ERK pathway) is one of the most important signaling pathways in PDAC. Activation of the MAPK/ERK pathway promotes PDAC growth and apoptosis resistance in response to gemcitabine [43,44]. We previously demonstrated that inhibition of GPX4 can overco
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