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(+)-Usniacin Growth inhibition assays are the
2024-03-29
Growth-inhibition assays are the most commonly used to identify antifungal small molecules. However, they have several facts that limit their use since many pathogenic fungi grow as filaments making difficult a correlation between growth and OD (optical density). They are not useful for identifying
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Breast Cancer Although androgens have been considered to be
2024-03-29
Breast Cancer: Although androgens have been considered to be a risk factor in prostate cancer they have been recommended to treat breast cancers. Even before the discovery of SERMs and aromatase inhibitors, steroidal androgens such as medroxyprogesterone and fluoxymesterone were used to treat breast
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PF-04691502 br Conclusions br Introduction During numerous p
2024-03-29
Conclusions Introduction During numerous physiological processes, aldehydes are generated from a variety of endogenous and exogenous precursors including amino acids, carbohydrates, and lipids [1]. Most aldehydes are highly reactive and cytotoxic due to the strong electrophilic nature of the t
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br Results br Discussion Tapinarof GSK
2024-03-29
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 Impact of global AHR deficiency on diet
2024-03-29
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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br Expression of ADK in the normal brain In adult
2024-03-28
Expression of ADK in the normal brain In adult brain, ADK is primarily expressed in astrocytes. Immunocytochemical analysis of adult rat and mouse nk1 antagonist revealed predominant astrocytic expression throughout the hippocampus and cortex. Two isoforms of ADK have been identified in mammals,
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br Acknowledgments This work was supported by
2024-03-28
Acknowledgments This work was supported by the R&D Program of the Institutional Research Program of KRICT (SI1701-02), and by the Next generation carbon upcycling project of Ministry of Science and ICT. JSC is kindly grateful to the National Research Council of Science and Technology (NST) for fi
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Molecular docking simulations were carried
2024-03-28
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic Ti
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endothelin receptor The first rationally designed dual mPGES
2024-03-28
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic endothelin receptor - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been
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While the yeasts and see Glossary each
2024-03-28
While the yeasts and (see Glossary) each contain only one Aurora homolog, Ipl1p (increase in ploidy 1) and Ark1 (Aurora-related kinase 1), respectively 5, 6, , and Xenopus laevis contain two Aurora kinases: Aurora A and Aurora B [4]. Mammals have three Aurora kinases, A, B, and C (Figure 1). In an
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Recruitment of the Rad BP mediator to chromatin involves
2024-03-28
Recruitment of the Rad9/53BP1 mediator to Sorafenib synthesis involves multiple pathways (Fig. 2). In unperturbed conditions, Rad9 is already bound to chromatin via interaction between its Tudor domain and methylated histone H3 at lysine 79 [82], [83], [84], [85]. This constitutive Rad9 recruitment
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Thus phosphorylation of p was used to measure the
2024-03-28
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc a83 expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Results an
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Songbirds are outstanding models in
2024-03-28
Songbirds are outstanding models in the study of vocal communication (Maney and Pinaud, 2011). Following the pioneering studies of William H. Thorpe and Peter Marler on the development of song in chaffinches (Fringilla coelebs) and white-crowned sparrows (Zonotrichia leucophrys) (Marler, 2004; Thorp
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Plant defensins Vriens et al
2024-03-28
Plant defensins (Vriens et al., 2014) and linear AMPs (Domingues et al., 2015, Liu et al., 2008) have been shown to present several modes of action. Among these different mechanisms, permeabilization of the fungal membrane has been described as a secondary effect of plant defensin action (Vriens et
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Tetracyclines constitute one of the most important antibioti
2024-03-28
Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200
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