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To test the compounds metabolic stability we measured the
2023-12-11
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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Illustrated in is the protocol we applied for the
2023-12-11
Illustrated in is the protocol we applied for the screens of novel furoic acids as ACL inhibitors. We constructed our furan carboxylate library that contained 1446 2-furoic agomelatine mg derivatives and 501 3-furoic acid derivatives by performing substructural searches of the ZINC database. We l
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The tumor suppressor function of LOX in
2023-12-11
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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ISRIB br HIF Signaling in AA Therapy
2023-12-11
HIF-α Signaling in AA Therapy Resistance An important result emerging from Phase 3 clinical trials testing AA therapies is improvement of progression-free survival (PFS) that is not accompanied by enhanced overall survival (OS) [26]. This dichotomy has been attributed to mechanisms of acquired re
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Several ceritinib resistant mutations following
2023-12-11
Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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A large number of aldose reductase inhibitors have been prep
2023-12-11
A large number of aldose reductase inhibitors have been prepared synthetically, and a limited number of them are therapeutically used. However, none of them is satisfactory. Here, Cannabis extracts with high content of non-psychotropic phytocannabinoids CBD/CBDA or CBG/CBGA showed statistically sign
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br There is evidence to
2023-12-08
There is evidence to suggest that GMF activities are regulated in vivo by post-translational modification. indeed, there is strong precedent for ADF-homology family proteins being regulated in this manner. Cofilin is inhibited by phosphorylation of a serine residue at its N terminus. This residue
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Owing to efficient catalytic character high electrolyte acce
2023-12-08
Owing to efficient catalytic character, high electrolyte accessible area, easy fabrication and many other interesting properties, metal oxide nanoparticles are extensively used in a variety of electro-analytical processes [14]. Metal oxide nanoparticles immobilized over a conductive and large area s
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Defining the multiple roles of autophagy in
2023-12-08
Defining the multiple roles of autophagy in stroke has been a rapidly evolving and exciting venue for translational research, with innovative products being applied from bench to bedside. Spanning pharmacological pathway manipulation and functional experimental validation, altered autophagy activati
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perhexiline Lower LDL C mediated by
2023-12-08
Lower LDL-C mediated by variants in the ACL gene is causally associated with the risk of cardiovascular events. Because, genetic variants that mimic the effect of an ACL inhibitor have the same effect on the risk of cardiovascular events per unit change in LDL-C as variants that mimic the effect of
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The use of FTAI can overcome the negative impact
2023-12-08
The use of FTAI can overcome the negative impact of low estrus detection efficiency, but implies effective synchrony of luteal function as well as synchronous growth and ovulation of a viable autophagy pathway follicle. Pregnancy rates obtained with FTAI may be comparable or better than those obtain
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Here the so called alkali assay
2023-12-08
Here the so-called alkali assay [18] is proposed as a method to be applied directly on the purified recombinant enzyme sharing the same structural and functional features of the wild-type enzyme [19], [20], [21] using its physiological substrate androstenedione. The assay that was already successful
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961 The regulation of gene expression by glucocorticoids
2023-12-08
The regulation of gene expression by glucocorticoids can be mediated either by the canonical mechanism that involves the interaction of the glucocorticoid receptor (GR), a transcription factor activated by the hormone, with glucocorticoid response element (Ye et al., 2007), or by the non-canonical m
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In Pham et al employed
2023-12-08
In 2014, Pham et al. [22] employed the microsphere-based technology to create a Luminex probe-based assay for the rapid identification of single nucleotide polymorphisms that are known to confer resistance to one or more echinocandins in C. glabrata. The targets for the FKS probes were generated usi
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The apocrine sweat glands of the human axilla
2023-12-08
The apocrine sweat glands of the human axilla produce odor substances with pheromone functions whose nature corresponds to volatile steroids (Cowley and Brooksbank, 1991, Grosser et al., 2000, Sobel et al., 1999, Weller, 1998). These functions only begin with puberty, indicating that sex hormones st
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