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Compound was docked into the active site of
2023-09-22
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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After infection with Salmonella those
2023-09-22
After infection with Salmonella those bacteria that are not targeted by autophagy of the complete Salmonella-containing phagosome (see above) but are living freely in the cytosol can be eliminated by xenophagy, that is direct targeting of the ‘naked’ bacteria to the autophagic pathway. The type III
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Consistent with a damaging role for
2023-09-22
Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he
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TLX may promote survival and prevent apoptosis in
2023-09-22
TLX may promote survival and prevent apoptosis in NB GSK2118436 [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially activates
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In previous years evidence emerged that inferred
2023-09-22
In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic e 64 (7) and piceatannol (8) (Fig. 3b) on mammalian arginase with IC50s of 10.6
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The accumulation of oxidized low density
2023-09-22
The accumulation of oxidized low-density lipoprotein (oxLDL) is one of the many causes of the initiation and progression of atherosclerosis (Virmani et al., 2002; Pirillo et al., 2013; Sun et al., 2016; Huang et al., 2016; Tabas, 2010). oxLDL-induced apoptosis of macrophages contributes to the forma
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Gratifyingly compound also demonstrated improved physicochem
2023-09-21
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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br HIF HIF signaling in cancer cells contributes
2023-09-21
HIF-1α HIF-1α signaling in cancer cells contributes to tumor progression by promoting angiogenesis, invasion, metastasis, and the recruitment of immunosuppressive cells via secreted modulators 36, 37. One example of a HIF-1α immunosuppressive pathway is through increased expression of inducible n
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KL 001 receptor br Conclusions br Acknowledgments The author
2023-09-21
Conclusions Acknowledgments The authors are thankful to Hugo Santos, Olga Martinez and Ricardo Lacerda for the technical assistance provided in the maintenance of the aquaria. This work was supported by national funds, through FCT and co-funded by the European Regional Development Fund (ERDF)
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The literature suggests that adiponectin has a steroidogenic
2023-09-21
The literature suggests that adiponectin has a steroidogenic effect on ovarian function. In pigs, in vitro studies have shown that adiponectin reduced basal testosterone secretion in internal theca cells; in granulosa cells, it increased secretion of estradiol and, in combination with insulin, incre
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br Conflicts of interest br
2023-09-21
Conflicts of interest Newly Identified Mechanisms of APN Resistance Hold Therapeutic Potential APN, APN Receptors, and APN Cardiovascular Protection APN Resistance in Cardiovascular Disease The Molecular Mechanisms of APN Resistance Concluding Remarks and Future Directions Finally,
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We have previously shown that
2023-09-21
We have previously shown that the human gonadotropins hLH and hCG trigger a partly irreversible stimulation of intracellular cyclic AMP accumulation in mouse Leydig Tumor fiin (MLTC) in contrast to all other tested mammalian LHs and CG (Klett et al., 2016). In order to get a better insight in the m
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In this report the natural compound deguelin
2023-09-21
In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho
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tivozanib In contrast to TPX members of the CPC
2023-09-21
In tivozanib to TPX2, members of the CPC (Figure 1B), such as survivin, borealin, and INCEN-P, which associate with Aurora B/C in animals, do not appear to have obvious homologs in plants. Recently, however, a putative INCEN-P homolog, termed WYRD, has been identified [34]. Sequence comparison betw
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Beside estrogen several classes of compounds have
2023-09-21
Beside estrogen, several Cetrorelix of compounds have shown significant neuroprotective efficacy when administered shortly after the induction of animal models of stroke, including glutamate (NMDA) receptor antagonists and zinc chelators [25], [26], [27]. Effects of these or other neuroprotective a
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