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br A and tau in
2023-11-29
Aβ and tau in Alzheimer's disease The two classical histopathological hallmarks of AD are extracellular insoluble Aβ deposits, known as Aβ plaques, and intracellular accumulations of insoluble microtubule-associated tau protein, known as neurofibrillary tangles [14]. Aβ peptides are produced as a
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The lactam emerged as lead candidate due to
2023-11-29
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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We found evidence of the interaction between AR
2023-11-29
We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th
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corticotropin releasing factor AKT activity is also self lim
2023-11-29
AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa
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ceramide kinase Microbe derived ligands can also
2023-11-29
Microbe-derived ligands can also activate AHR. Malassezia, a commensal yeast in human skin, can metabolize tryptophan into several AHR activating compounds including FICZ and ICZ [59]. Lactobacillus converts tryptophan into indole-3-aldehyde (IAld), which can activate AHR and promote IL-22 productio
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Additionally regulation of GPCR heteromerization by specific
2023-11-29
Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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The role of DHT in early teleost
2023-11-29
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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For the NSCLC patients with EGFR activating mutations EGFR
2023-11-29
For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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Autophagy is a highly conservative intracellular bulk degrad
2023-11-29
Autophagy is a highly conservative intracellular bulk degradation process including three major forms namely microautophagy, chaperone-mediated autophagy and macroautophagy. A large number of evidence has depicted a pivotal role for autophagy in the maintenance of cardiac geometry and contractile fu
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The tumor suppressor function of LOX
2023-11-29
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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Recent retrospective cohort studies have supported
2023-11-28
Recent retrospective cohort studies have supported these preclinical findings in animals indicating the correlation of AR activation with the induction of bibn australia carcinogenesis. First, men with prostate cancer who underwent androgen deprivation therapy were shown to have a significantly low
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Recent work has detailed the impact of genetic deletion of
2023-11-28
Recent work has detailed the impact of genetic Pemetrexed of AMPK in the liver, revealing only minor phenotypes upon removal in mice (Boudaba et al., 2018). However, these studies very elegantly showed the potential for small molecule-mediated activation of AMPK to elicit large changes in lipid met
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An ALK rearrangement was found in all
2023-11-28
An ALK rearrangement was found in all the analyzable ‘truly positive’ IHC+/FISH+ samples, and the proportion of the various transcripts was in accordance with the literature [[26], [46], [47], [48]]. In these samples, the RNA-seq technique was therefore 100% sensitive and specific. Additional non-ta
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In this study using pure enzyme preparations of human placen
2023-11-28
In this study, using pure enzyme preparations of human placental recombinant AR (hAR) and of AR isolated from bovine lens (bAR), which behave as Michaelis Imiquimod with glyceraldehyde as substrate, is shown that an apparent negative cooperativity action for glucose still occurs. We present evidenc
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Besides its multiple peripheral effects adiponectin
2023-11-28
Besides its multiple peripheral effects adiponectin may ameliorate insulin resistance by acting in the brain, and intracerebroventricular administration of adiponectin in rodents decreases body weight by stimulating energy expenditure [13]. Adiponectin most likely crosses the blood-CSF-barrier (BCB)
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