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br Results br Discussion Tapinarof GSK is a naturally derive
2023-02-07
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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Among all the compounds the novel
2023-02-06
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The Miltefosine 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM) and
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In this study an in vitro AChE inhibition
2023-02-06
In this study, an in vitro AChE inhibition assay combined with UF-HPLC-ESI-Q-TOF/MS method was developed for rapid screening and identification of AChEI from the roots of C. chinensis Franch. Five compounds was found with AChE inhibitory activity and identified by the on-line DAD-ESI-Q-TOF/MS compar
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br Results and discussion br
2023-02-06
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic 360A group extending from the C-3 position of the aniline and substituted groups at
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The inhibition of ACLY induces an anticancer effect that
2023-02-06
The inhibition of ACLY induces an anticancer effect that has been reported to be involved in mitochondrial reactive oxygen species (ROS) generation [14], [16], dual blockade of mitogen-activated protein kinase and phosphatidylinositol-3-kinase/AKT pathways [11], and the glycolytic phenotype of tumor
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Arginase deficiency is a rare urea
2023-02-06
Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a
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Additional support for a role of HMGN
2023-02-06
Additional support for a role of HMGN1 in enhancing DNA repair comes from studies of transcription-coupled repair (TCR) in human cells. Lesions in the template strand of DNA induced by UV light stall the movement of RNA polymerase II (RNAPII) and interrupt transcription. Removal of these transcripti
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Although sex hormones activational effects are known to
2023-02-06
Although sex hormones (activational effects) are known to directly interact with RAS (Baiardi et al., 2005, Miller et al., 1999, Silbiger and Neugarten, 1995), the potential contribution of organizational hormonal and SCC effects on physiological sex-based difference in the regulation of the RAS rem
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br Eprosartan The AT R antagonist
2023-02-06
Eprosartan The AT1R antagonist eprosartan is approved for the treatment of essential TMPyP4 tosylate and may be administered using a convenient once-daily regimen. The drug is a well-tolerated and effective antihypertensive agent with benefit in the secondary prevention of cerebrovascular events,
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TCS 2002 Kuda et al reported that the activity of
2023-02-06
Kuda et al. (1997) reported that the activity of aminopeptidase A (ApA) but not aminopeptidase B (ApB) nor aminopeptidase N (ApN) was decreased in plasma from patients with Alzheimer's disease (AD). More recently Puertas et al. (2013) reported that the activities of plasma ApA, ApB, ApN and IRAP wer
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The preferential expression of ALOX
2023-02-06
The preferential expression of ALOX15B in human macrophages may explain why human genetic studies investigating the association of ALOX15 with cardiovascular disease did not show consistent results. Two rare functional polymorphisms have been characterized in the ALOX15 gene, which leads to increase
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SF1670 Actin is capable of polymerizing spontaneously Howeve
2023-02-03
Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of SF1670 dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerization [5], [6]. The shape and th
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In conclusion two novel series of furo pyrimidin amines and
2023-02-03
In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas
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Our data indicate that the D domain only needs to
2023-02-01
Our data indicate that the D1 domain only needs to hydrolyze ATP a few times, or perhaps even just once, during the processing of a given substrate molecule, whereas the D2 domain hydrolyzes ATP many times. Consistent with this model, only D2 contains the canonical aromatic pore loop residues implic
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The ambiguity surrounding the role played by the LOXs
2023-02-01
The ambiguity surrounding the role played by the 15-LOXs in malignant biological processes stems also from the limitations of current animal models, and especially the usage of its 12/15-LOX murine homolog, which can also catalyze the production of 12-HETE. Indeed, the proinflammatory effect of 12-H
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