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In order to increase the oral bioavailability abiraterone
2023-08-29
In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral fak inhibitor of abiraterone acetate (156), it is recommended that this drug should be taken on
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Spermine NONOate Introduction The first use of
2023-08-29
Introduction The first use of the term “autophagy” by a French physiologist, M. Anselmier, in a short article describing the effects of fasting in mice published in 1859, took place almost a century before Christian De Duve described it from a mechanistic point of view in a symposium on lysosomes
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Ryoichi et al modified potent clinical candidate VX with cya
2023-08-29
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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The analysis of the profile of protein phosphorylation in
2023-08-29
The analysis of the profile of protein phosphorylation in MMS-treated Mercaptopurine australia confirmed that both the ATM and ATR pathways were activated in S-phase blocked cells. Interestingly, phosphorylation of Chk1 was observed 24h after MMS-treatment both in AT- and ATM-inhibited cells, whils
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PTP Inhibitor IV br Current limitations and future
2023-08-29
Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med
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Therefore a number of homoisoflavonoids may be designed in
2023-08-29
Therefore, a number of homoisoflavonoids may be designed in future that may be effective against angiogenesis for treating ocular neovascularization. As this Canrenone current study deals with robust molecular modeling techniques on SH-11037 (cpd 15) and related homoisoflavonoids and SH-11037 has ga
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However joint reviews and the consensus from
2023-08-29
However, joint reviews and the consensus from experts offer disparate recommendations with regard to their management in the context of anesthesia, whereas some reviews [6], [7] set out certain doubts regarding their use during the perioperative period. On the other hand, the guidelines for the mana
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br Introduction AMP activated protein kinase AMPK has
2023-08-29
Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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br Methods br Results br Discussion
2023-08-29
Methods Results Discussion Chronic stress renders individuals vulnerable to diseases, and this effect might be, at least partially, mediated by stress hormone-induced immunosuppression. Therefore, investigating the effects of catecholamines on immune Deferoxamine mesylate synthesis is of h
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br Materials and methods br Results br
2023-08-28
Materials and methods Results Discussion In the present study, we aimed to elucidate the contribution of adenosine receptors to vascular tone in mice with T1D. We showed that diabetes resulted in decreased A1 adenosine receptor-mediated contraction in the aorta, which was accompanied by inc
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NLX a k a F or befiradol exhibits
2023-08-28
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in β-Pompilidotoxin mg to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additional
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gap junctions Glycosylphosphatidylinositol GPI cell wall anc
2023-08-28
Glycosylphosphatidylinositol (GPI) gap junctions anchor synthesis pathway is another promising antifungal target. Novel inhibitors of Gwt1 and Mcd4, two enzymes in the GPI anchor pathway were identified by the chemical-genomics-based screening platform CaFT (Candida albicans fitness test) [89]. Scre
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This unsuspected antagonistic interaction of androgen with O
2023-08-28
This unsuspected antagonistic interaction of androgen with OXER1 could therefore explain the effect of plant derived compounds with this ligand-receptor system. For example, wedelolactone, a coumestan found in Eclipta alba (false daisy) and in Wedelia calendulacea that is the major component of ecli
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From a clinical utility standpoint this study showed that
2023-08-28
From a clinical utility standpoint, this study showed that AR can be useful in the GATA3-positive tumor of unknown origin setting. Epidemiologically, in this setting, the top 2 diagnoses in the differential diagnosis are metastatic carcinoma of breast origin or urothelial origin [18]. Seven out of
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Liao and van Linden et
2023-08-28
Liao [47] and van Linden et al. [48] divided the gap between the N-terminal and C-terminal lobes into a front cleft or pocket, a gate area, and a back cleft. The back pocket corresponds to the gate area and the back cleft. The front cleft includes the Gly-rich loop, the hinge, the linker connecting
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