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In this study we explore different mathematical models for
2022-04-14

In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixe
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In the present study recipient oestradiol serum levels on th
2022-04-14

In the present study, recipient oestradiol serum levels on the day of donor oocyte retrieval or warming were found to be significantly higher in the antagonist group and higher than 100 pg/ml in all cases. Serum oestradiol level has been reported to have no effect on endometrial receptiveness in ooc
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br Conclusion br Conflict of interest
2022-04-14

Conclusion Conflict of interest Acknowledgments This work was supported by an NRF grant (2016R1A2B4011196) from the Korea Research Foundation. Introduction Thymic epithelial tumors are rare, but they are the most common primary neoplasm of the thymus and of the anterosuperior mediastinu
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br Materials and methods br Results br
2022-04-14

Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast Psora 4 by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minutes and w
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In the present study five Glu substituted analogues of GIP
2022-04-14

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Various strategies have been pursued
2022-04-14

Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino flavopiridol substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g.
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br Activators Many compounds are known to influence the
2022-04-14

Activators Many compounds are known to influence the activity of Ca2+-activated K+ channels, and since hIK1 was cloned more insight has been gained on compounds that have the capacity to increase channel activity. Activation by divalent metal cations has been investigated, with Ca2+, Pb2+, Cd2+,
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Many neutral and acidophilic galactosidases have been purifi
2022-04-13

Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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The current gold standard for diagnosing BAM or
2022-04-13

The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) straight from the source (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated tauroch
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CC is a widespread disorder affecting up to
2022-04-13

CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d
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Sensitivity to EphB TKI was also
2022-04-13

Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 rosavin synthesis after transient transfection of pCMV6-AC-GFP/EphB3, and both were demons
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br Discussion The initial reduction and the subsequent incre
2022-04-13

Discussion The initial reduction and the subsequent increase in permeability proposes a regulatory process to control bleeding. However, following repeated injury, or during long-term presence of the inflammatory stimuli, these mechanisms may become defective and even detrimental. The expression
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The progression of HIV varies from patient to patient
2022-04-13

The progression of HIV varies from patient to patient, with some who progress slowly and others who progress much faster. However, CD4+ and CD8+ cell counts are intimately linked in those that are able to suppress the HIV infection (Walker et al., 1986; Saez-Aninon et al., 2007). Depletion of these
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With LML methyl oxo dihydropyridazin yl
2022-04-13

With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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According to the literature HER mutations are present in
2022-04-13

According to the literature, HER2 mutations are present in 2–4% of lung adenocarcinoma (ADC) patients. Most HER2 mutations are in-frame insertional mutations occurring at exon 20 in the protein kinase domain [[2], [3], [4], [5]]. Although several small molecules and HER2 BMS265246 synthesis have be
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