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The introduction of a pyrazole moiety into
2024-12-09
The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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A variety of quinazoline or fused pyrimidine
2024-12-09
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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br Methods and materials br Results br Discussion GPCR regul
2024-12-07
Methods and materials Results Discussion GPCR regulation in response to agonist stimulation is common to nearly all GPCRs and is essential in physiological systems to limit persistent signalling. In this study we have investigated the [Pyr1]apelin-13-induced trafficking and desensitization
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Prostate cell growth and prostate carcinogenesis are not onl
2024-12-07
Prostate cell growth and prostate carcinogenesis are not only mediated by androgens, they are also dependent on functional insulin receptor (IR) and insulin-like growth factor-1 (IGF-1) receptor (IGF1R) signaling. Previous studies addressed this issue and reported a correlation between high insulin
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Pazopanib As noted above yeasts particularly S cerevisiae
2024-12-07
As noted above, yeasts, particularly S. cerevisiae (Frey and Röhm 1978; Trumbly and Bradley 1983), produce APs, but these are intracellular enzymes located in the vacuolar compartment, with the exception of aminopeptidase II. About 40% of aminopeptidase II activity is detected as external enzyme, li
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Some of the mechanisms that involve LOX as a potential
2024-12-07
Some of the mechanisms that involve 12-LOX as a potential pathogenic enzyme are illustrated in Fig. 2. Direct β cell effects associated with the stimulation of 12-LOX activity include the activation of second messengers c-Jun N-terminal kinase and p38 MAPK, both of which show increased phosphorylati
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In a working group exposed
2024-12-07
In 2008, a working group exposed 12-month-old transgenic mice (mutation for human amyloid precursor protein expression) and their non-transgenic littermates to isoflurane and halothane for 120min per day for five days. It was concluded that in the transgenic mouse there was overload of amyloid prote
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Interest in natural products has led to the study
2024-12-07
Interest in natural products has led to the study of plant extracts as sources of ARIs. However, chemical complexity of natural extracts makes the identification of ARIs challenging and time-consuming. Identification of bioactive compounds with the desired biological effect from natural products, co
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The correlation in the increase
2024-12-07
The correlation in the increase of BADH mRNA, protein levels, and enzyme activity, demonstrate that oxidation of betaine aldehyde by BADH is primordial to regulate the GB accumulation during physiological cardiac hypertrophy induced by pregnancy, this implies a major role because GB levels enhance c
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There are human genes in the
2024-12-07
There are 12 human genes in the SLC5A family, and 6 of these are expressed in human heart (Table 2). Little is known about SGLT proteins in the heart. Zhou et al. [56] reported the presence of SGLT1 mRNA in the human heart. Researchers have found that levels of SGLT1 mRNA in heart are approximately
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Epiberberine br Experimental procedure br Funding The presen
2024-12-07
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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Fluorescent nucleotide incorporation Regenerative mechanisms
2024-12-07
Regenerative mechanisms often require reemployment of pathways used during development in the embryonic and postnatal periods (Waschek, 2002). PACAP has diverse neurodevelopmental and growth factor-like effects (Botia et al., 2007; Vaudry et al., 2009; Waschek, 2002; Watanabe et al., 2016) and it is
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The extent to which GPCR oligomerization is a regulated proc
2024-12-06
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Acknowledgments br P c is expressed in several steroidogenic
2024-12-06
Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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br Materials and methods br Results br
2024-12-06
Materials and methods Results Discussion The success of CAR-T cell therapy is based on two major facts: one is that cancer cells express tumor-associated antigens (TAAs) on their surface that can be detected by the human immune system; the other is that the CAR molecules target these TAAs o
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