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Here we report discovery of highly selective pan Aurora kina
2024-11-27
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of TPMPA bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To iden
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br Materials and methods br Results br Discussion CUs
2024-11-27
Materials and methods Results Discussion CUs, which have been used as traditional medicine for thousands of years in East Asian countries, have the potential to be used for cancer chemoprevention and chemotherapy [17], [18], [19], [20]. CuB is one of the most promising agents as it is repor
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Therefore the rational design of
2024-11-27
Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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As aforementioned this study aimed
2024-11-27
As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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Additionally we used the predicted Cyp a
2024-11-27
Additionally, we used the predicted Cyp19a1b amino Efaproxiral Sodium synthesis sequence from a number of bony fish species to infer their genetic relatedness and found that R. quelen occupies an ancient position within the Siluriformes group. A phylogenetic tree was constructed and it included bot
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Several strategies have been employed
2024-11-27
Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, ionomycin induces changes in the spectral properties of the fluorophore(s) incorporated into
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Introduction Antimicrobial resistance is a growing health th
2024-11-27
Introduction Antimicrobial resistance is a growing health threat worldwide that has been associated with incorrect prescription and overuse of Silodosin [1]. Considering that physicians play a central role in antibiotic usage, a better understanding of their prescribing behaviours and their knowle
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AMP activated protein kinase AMPK
2024-11-26
AMP-activated protein kinase (AMPK) is a key cellular energy sensor that maintains energy homeostasis at the cellular and whole-organism level (Hardie et al., 2012). Functionally, the AMPK pathway sustains adenosine triphosphate (ATP) production through activation of fatty tgf beta receptor 1 oxida
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br Conflict of interest statement br Acknowledgement br
2024-11-26
Conflict of interest statement Acknowledgement Introduction Lipoxygenases (LOs) are enzymes catalyzing the positional as well as stereo-specific introduction of molecular oxygen into 1,4-pentadiene structures found in unsaturated fatty acids such as arachidonic flag tag dna sequence or lin
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br Introduction There are greater
2024-11-26
Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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Our results add to previously published
2024-11-26
Our results add to previously published data on the contribution of ALDH3A1 to the optical properties of the cornea. Specifically, the study by Nees et al. (2002) was among the first to examine whether ALDH3A1 serves as a structural component in the cornea and similarly to lens crystallins. Their ex
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br Results br Discussion Tapinarof GSK
2024-11-26
Results Discussion Tapinarof (GSK2894512) is a naturally derived investigational topical medicine with demonstrated clinical efficacy for patients with AD and psoriasis (Bissonnette et al., 2010, Bissonnette et al., 2012a). The drug substance is a polyphenol produced by bacteria that is struct
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br HIF HIF signaling in cancer cells contributes to
2024-11-26
HIF-1α HIF-1α signaling in cancer cells contributes to tumor progression by promoting angiogenesis, invasion, metastasis, and the recruitment of immunosuppressive cells via secreted modulators 36, 37. One example of a HIF-1α immunosuppressive pathway is through increased expression of inducible n
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While HTPCs are not immune cells they
2024-11-26
While HTPCs are not immune cells, they produce IL-6, MCP-1 and other immunologically relevant factors (Mayer et al., 2016). Our results demonstrated that epinephrine and phenylephrine increased the mRNA expression levels of COX-2, IL-6 and MCP-1 in HTPCs without affecting the mRNA expression level o
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br Adiponectin in prostate cancer PC was documented as
2024-11-26
Adiponectin in prostate cancer PC was documented as the leading type of malignancy in males in the US with respect to both the estimated number of cases (22,800) and deaths (27,540) (Siegel et al., 2016). Studies have reported an association between low APN levels and the progression of PC (Micha
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