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In conclusion our study would seem
2022-11-07
In conclusion, our study would seem to indicate that a hydrophilic microenvironment, which is suitable to accommodate highly hydrophilic molecules with steric hindrance such as aldose hemiacetals, allows the enzyme modulation by one of its most important physiopathological substrates. It is difficul
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br Results br Discussion Tapinarof GSK is a
2022-11-07
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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The excellent potencies selectivities and improved PK
2022-11-07
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
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2-D08 synthesis Our studies also reveal the normal functiona
2022-11-07
Our studies also reveal the normal functional roles of the MIR. Interaction between the MIR loop and the N-terminal α helix nucleates conformational maturation of AChR subunits, thereby promoting assembly of mature AChRs [52], [55]. This interaction in homologous parts of all AChR subunits appears t
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Using constant potential amperometry and electrochemical enz
2022-11-07
Using constant potential amperometry and electrochemical enzyme-based biosensors selective for choline—and, therefore, an accurate readout of ambroxol hydrochloride release (Baker et al., 2015; Bruno et al., 2006a; Parikh et al., 2004, 2007)—tonic and phasic release of acetylcholine were measured s
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br COX and LOX in post mortem AD brain Minghetti
2022-11-07
COX and 5-LOX in post-mortem AD brain Minghetti (2004) reviewed the findings on COX-2 mRNA levels in AD brains, pointing out that the available evidence demonstrated either decreased or increased levels, possibly because of the short half-life of COX-2 transcripts or individual variability. Histo
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Thus one possible target for CRPC
2022-11-07
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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br The Molecular Machinery of
2022-11-07
The Molecular Machinery of Autophagy and Regulation by Sphingolipids Sphingolipid-Mediated Autophagy in Cancer: Dr. Jekyll and Mr. Hyde Autophagy is an evolutionarily conserved stress response that typically promotes survival and antagonizes apoptosis. However, excessive autophagy was found to
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Cerebral ischemia occurs following the occlusion
2022-11-07
Cerebral ischemia occurs following the occlusion of a cerebral artery by a thrombus and causes cell swelling due to cytotoxic edema and BBB disruption with vasogenic edema (Loreto and Reggio, 2010, Nakaji et al., 2006, Shibata et al., 2004). Vasogenic edema is directly linked to alteration of the BB
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blue nitro mg Introduction The corpus luteum CL is a transie
2022-11-07
Introduction The corpus luteum (CL) is a transient endocrine gland that differentiates from the thecal and granulosal cells of the ovarian follicle after ovulation. Its formation and limited lifespan in the mammalian ovary is important for fertility, as the CL produces progesterone (P4), the essent
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br AR signals and chemosensitivity in urothelial cancer A si
2022-11-05
AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance
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Due to metabolic variations it is important to consider argi
2022-11-05
Due to metabolic variations, it is important to consider arginine metabolism and dependency in specific contexts to identify precise patterns. This is best illustrated for ASS: while ASS deficiency correlates with worse prognosis in sarcomas, ASS levels positively correlate with a poor prognosis in
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Liver plays a pivotal role in metabolism of
2022-11-05
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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br Mechanisms for regulation of intracellular cholesterol ho
2022-11-05
Mechanisms for regulation of intracellular cholesterol homeostasis Cells maintain intracellular free cholesterol levels and distribution within stringent tolerances by several mechanisms [55]: (1) uptake of native LDL (the major extracellular carrier of cholesterol) by LDL receptors and modified
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br Hypoadiponectinemia in metabolic syndrome APN belongs
2022-11-05
Hypoadiponectinemia in metabolic syndrome APN belongs structurally to the complement 1q family and is found at high concentrations (>0.01% of total protein) in the serum of healthy individuals [6]. Given the abundance of APN in plasma, it is assumed that alterations in plasma levels of APN might
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