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br Acknowledgements This work was financed by the
2022-06-06
Acknowledgements This work was financed by the projects “Mejora Genética del Almendro” (MINECO-Spain, AGL2017-85042-R), “The molecular mechanisms to break flower bud dormancy in fruit trees” to RS-P within the Villum Young Investigator Program and by the VILLUM Research Center for Plant Plasticit
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Type diabetes mellitus is characterised by two major
2022-06-06
Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta pdgf receptor [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin resistance i
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AMI-1 The HH signaling has also been implicated in the
2022-06-06
The HH signaling has also been implicated in the regulation of cancer stem AMI-1 (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malignancies, inc
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The usefulness of GIP R
2022-06-06
The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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Comparison of dlGALRs deduced amino acid
2022-06-06
Comparison of dlGALRs deduced amino bimatoprost sequences with that of human GALRs demonstrate that the GALR1 ortholog sequences have diverged less than those of GALR2. Since often duplicate genes undergo divergent evolution through sub-functionalization, loss or gain of new functions (Prince and P
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Recently they reported an enyne
2022-06-06
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral 1027 synthesis (tmax=15min) and a decent pharmacokinetic profile
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Current studies have identified five orphan G protein couple
2022-06-06
Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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SETDB is ubiquitously expressed in mouse tissues and
2022-06-06
SETDB1 is ubiquitously expressed in mouse tissues, and more than 900,000 ERVs are dispersed through the mouse genome. Nevertheless, the repertoire of ERVs under the control of SETDB1 was limited and highly cell-type specific. Only 17,349 ERVs were associated with H3K9me3 domains in Th2 cells. The va
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Losmapimod LSD also contributes to the regulation
2022-06-06
LSD1 also contributes to the regulation of specific programs of gene expression in postmitotic, fate-committed neurons. Perhaps its most specialized role is in the complex series of epigenetic regulatory events that permit each olfactory sensory neuron to express one and only one of the thousands of
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Long term effects of prolonged darkness on specific physiolo
2022-06-06
Long-term effects of prolonged darkness on specific physiological activities were also monitored at different leaf positions. Basically, stomatal conductance and CO2 assimilation were different at various leaf stages and were decreased or inhibited significantly within 24 h in all leaf positions upo
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br General aspects of HDACs br General aspects of
2022-06-05
General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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Solasodine In the H NMR spectrum two
2022-06-05
In the 1H NMR spectrum two pairs of doublet resonances arising from the protons in the aromatic moiety of the two diastereoisomers can be readily observed around 7.5–7.6 ppm. These resonances can be used to detect and quantify the two diastereoisomers. From the results presented in Fig. 1A it can be
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In conclusion GPR inhibits and GPR enhances the cell motile
2022-06-05
In conclusion, GPR120 inhibits and GPR40 enhances the cell motile activity stimulated by TPA in melanoma cells, while MMP-9 activation was reduced by GPR40. In contrast, GPR40 negatively regulated cellular functions of fibrosarcoma TDZD-8 sale [11]. Taken together, it is suggested that opposite effe
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Strengths The primary feature of GPR agonists resides in
2022-06-05
Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L AMG 9810 as well as glucose-dependent insulin secretion and insulin promoter activity enhancement in pancrea
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In addition to their functional activation
2022-06-05
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic SCR7 australia to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas
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