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In earlier experiments on snails a
2023-12-11

In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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Steroidal CYP inhibitors can further be classified based
2023-12-11

Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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Our sample is representative of mRCC treated
2023-12-11

Our sample is representative of mRCC treated with sunitinib. However, the results from CCC setting have limited inference due to small exploratory sample (n = 51). Additionally, the significance of survival differences in CCC according to AXL staining is tangential. Unfortunately, we were unable to
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Among the AXL positive tumors that we screened the TNBC
2023-12-11

Among the AXL-positive tumors that we screened, the TNBC cell line MDA-MB-231 showed the highest AXL expression level. Additionally, AXL protein levels were higher in TNBC patient samples than in other breast cancers. Considering the difficulty of, and the urgent need for, effective treatments of TN
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AZ505 synthesis Fig summarizes the oxidative metabolism of a
2023-12-11

Fig. 1 summarizes the oxidative metabolism of arachidonic AZ505 synthesis by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosinophi
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Previous investigations have established that
2023-12-11

Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w
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br Conflict of interest br
2023-12-11

Conflict of interest Acknowledgments This work was financially supported by the Fund Project of Sichuan Provincial Department of Education (16ZB0053), the Scientific Research Foundation of Sichuan Agricultural University (No. 06021400) and the China Postdoctoral Science Foundation (No. 2015M58
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The AT hook motif is highly conserved in
2023-12-11

The AT-hook motif is highly conserved in evolution from bacteria to humans and is found in one or more copies in a large number of other, non-HMGA, proteins, many of which are transcription factors or are involved in chromatin remodeling [8]. For example, AT-hook peptide motifs are essential compone
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br Materials and methods br Results br
2023-12-11

Materials and methods Results Discussion The transcriptional activity of PGC-1α is regulated by a number of stimuli, exemplifying the range of settings in which mitochondrial biogenesis is induced. The mechanisms governing this regulation have been extensively studied and have been determin
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Several enzymes in serine and glycine metabolism
2023-12-11

Several enzymes in serine and glycine metabolism have been proposed as biomarkers for cancer stage and prognosis. Phosphoglycerate dehydrogenase (PHGDH), phosphoserine phosphatase (PSPH), and serine hydroxymethyltransferase (SHMT) levels are high in TNBC and low in luminal-A breast cancers (Kim et a
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The lactam emerged as lead candidate due to
2023-12-11

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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AhR was proven to participate in carcinogenesis Its
2023-12-11

AhR was proven to participate in carcinogenesis. Its high expression was demonstrated in a variety of tumors, i.e. pancreatic, prostate, urinary tract, lung and papillary thyroid carcinoma (Safe et al., 2013, Mian et al., 2014). However, cell line studies showed variable AhR levels/responses. AhR kn
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The excellent potencies selectivities and improved
2023-12-11

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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We have previously shown that
2023-12-11

We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific Purvalanol B blockade or activation (Rojas-Corrales et al., 2000). Moreover
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Pituitary adenylate cyclase activating polypeptide PACAP is
2023-12-08

Pituitary adenylate cyclase-activating polypeptide (PACAP) is a member of the secretin/growth hormone-releasing hormone (GHRH)/vasoactive intestinal peptide (VIP) family, with potent anti-inflammatory and potent cytoprotective properties [[6], [7], [8], [9], [10], [11], [12], [13]]. PACAP exists as
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