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The cavity volume of the binding pocket may differ not
2024-05-14
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino Cy3 azide substitution within a binding pocket may result in a change in the cavity volume. This, in turn, may affe
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Does dietary caffeine interfere with
2024-05-14
(8) Does dietary caffeine interfere with antinociception by other modalities that alter pain (TENS, exercise, joint mobilization, water immersion therapy)? Caffeine and/or A1R antagonists inhibit antinociception by each of these modalities in preclinical studies, such that there is potential for int
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br ACK inhibitors Since ACK activation
2024-05-14
ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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Despite these conflicting data about COX
2024-05-14
Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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What are the in situ
2024-05-13
What are the in-situ effects of multi-site CaM associations with AT1R? Kai et al. showed that synthetic peptides corresponding to residues 125–137 (rat sequence) in SMD2, 217–227 in the N-terminal side of SMD3, and 304–316 in SMD4JM inhibit to various degrees AngII-induced GTPase activity of isolate
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orthopoxvirus variola Androgen receptor translocates from th
2024-05-13
Androgen receptor translocates from the cytoplasm to the nucleus after binding to its ligands (Quigley et al., 1995). In the current study, although propofol did not significantly affect total androgen receptor protein levels, it significantly decreased nuclear androgen receptor levels. These findin
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br Results The newly synthesized leucine ureido derivatives
2024-05-13
Results The newly synthesized leucine ureido derivatives were firstly evaluated for their enzymatic inhibition using porcine kidney APN (Microsomal, Biocol) with bestatin as the positive control (Table 1). One isoleucine ureido derivative 14 and phenylglycine ureido derivative 15 were also synthe
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In conclusion we identify in this report the molecular natur
2024-05-13
In conclusion, we identify in this report the molecular nature of the 12- and 15-lipoxygenases in M. mulatta and P. pygmaeus and also that the expression of the rhesus enzyme in lung epithelial cells is regulated by interleukin-4. The switch from a mainly 12-LO enzyme to a mainly 15-LO enzyme during
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As one of emerging high
2024-05-13
As one of emerging high-throughout methods, metabolomics detects metabolites which are ultimate response of biological systems to environmental changes [14]. Metabolomics uncovers metabolic alteration at the systems level. Comparison of global metabolic profiling reflects some unidentified biologica
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Liver plays a pivotal role in metabolism of xenobiotic
2024-05-13
Liver plays a pivotal role in metabolism of xenobiotic compounds, such as environmental contaminants and drugs. Some of these compounds generate hepatic damage and impair its function. It was well-known that 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) could induce pathological changes in mouse and ra
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There is a growing literature
2024-05-13
There is a growing literature on ABCA2 expression in human biopsies, where it has been described as a potential biomarker of leukemias. In childhood T-cell acute lymphoblastic leukemia, ABCA2 and ABCA3 were expressed at high levels, which upon treatment with methotrexate, vinblastine and doxorubicin
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This study was funded and supported by Tehran
2024-05-13
This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet
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vistusertib A weakness of our technique is that during
2024-05-13
A weakness of our technique is that during the early post-operative period without the scaffold of an enteric channel patients can be at risk for traumatic or difficult catheterization, with 3 of 6 requiring a visit. This appeared to be offset by having skilled and educated housestaff capable of rec
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Many metalloenzyme inhibitors consist of two chemical compon
2024-05-13
Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino BMS-509744 residues that form the substrate-binding site of the metalloenzyme. The MGB is ofte
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The Kelch like ECH associated protein Keap Nrf
2024-05-13
The Kelch-like ECH-associated protein 1 (Keap1)-Nrf2 signaling pathway functions as one of the key regulator of the cellular defense system against oxidative stress [26]. Nrf2 is a redox-sensitive transcription factor, that is sequestered in the cytoplam by binding to Keap1; however, under oxidativ
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