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The extensive worldwide research efforts
2021-10-11
The extensive worldwide research efforts in the decade following FFA1 de-orphaning aimed at developing clinically useful FFA1 agonists were nearly halted after Takeda’s first-in-class agent fasiglifam (TAK-875) was discontinued in phase III of human trials. On the date of submission of this manuscri
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C prevents the glutamate and erastin induced
2021-10-11
C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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One of the main mechanisms enabling recycling of intracellul
2021-10-11
One of the main mechanisms enabling recycling of intracellular redox-active iron is lysosomal degradation of ferritin in the process of autophagy, often referred to as ‘ferritinophagy’ [128]. Autophagy was suggested to contribute to ferroptotic cell death by promoting the degradation of iron storage
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ionomycin br Conclusions In summary our results demonstrate
2021-10-11
Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical ionomycin have a dual effect, and a decrease of the 5-HT2A ex
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br Positive regulation of gene expression
2021-10-11
Positive regulation of gene SC-9 by Nrf2 Repression of Nrf2 by Keap1 Because many xenobiotic inducers of NQO1 and GST enzyme activities contain a thiol-reactive electrophilic moiety (i.e. are soft electrophiles), Paul Talalay and colleagues predicted in 1988 that they would be recognized with
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Elimination of the Q R bridge significantly affected
2021-10-11
Elimination of the Q234–R244 bridge significantly affected the protein CL 316243 disodium salt but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially retained th
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In the liver ghrelin has opposite effects to insulin
2021-10-11
In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty Cy7 NHS ester (non-sulfonated) mg oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de n
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br Materials and methods br Results br Discussion Nervous
2021-10-11
Materials and methods Results Discussion Nervous system disease is an important signal of AIDS deterioration (Rosca et al., 2012, Yilmaz et al., 2012). It is possible that HIV crosses the blood Folinic acid barrier or blood cerebrospinal fluid barrier into the central nervous system freely
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br Concluding remarks br Introduction
2021-10-11
Concluding remarks Introduction The hair ARRY-142886 of vestibular organs detect linear and rotational head movements, providing sensory information that is essential for normal postural and visual reflexes. Most vestibular hair cells are produced during embryonic development, but they can be
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br Future perspectives A plethora of reports
2021-10-09
Future perspectives A plethora of reports from in vivo and in vitro human and animal studies have demonstrated the potential role of FGFR signalling in human carcinogenesis, whether it be in an oncogenic or tumour suppressive capacity. It is still not well understood how FGFRs can act as tumour s
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In a preliminary communication we showed that AT and
2021-10-09
In a preliminary communication, we showed that AT and ETB receptors colocalize and coimmunoprecipitate in renal proximal tubule cells, and stimulation of the AT receptor increases ETB receptor expression in Wistar-Kyoto (WKY) rats [abstract; Zeng C,, 26:80A, 2003]. We hypothesize that the ETB recept
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Given the overexpression of HO in some tumors such as
2021-10-09
Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho
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PDEs a group of metallophosphohydrolases hydrolyze the cycli
2021-10-09
PDEs, a group of metallophosphohydrolases, hydrolyze the 3′,5′-cyclic phosphate group on cyclic nucleotides to a 5′-monophosphate, thereby blocking cyclic AMP (cAMP) or cGMP signaling [8,9]. There are different types of PDE isozymes, with different substrate specificities. PDE5 (specific to cGMP) an
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br Family A Receptors as Promiscuous Sensors
2021-10-09
Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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KN-92 Compounds and were tested for pharmacodynamic effects
2021-10-09
Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a
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