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Lastly haspin inhibitor was assessed against a panel of
2022-04-11
Lastly, haspin inhibitor was assessed against a panel of 292 kinases at 10μM. At this high concentration, the WYE-125132 inhibited thirteen kinases, in addition to haspin, ⩾90%., These kinases were CaMK2b, CaMK2d, CDK7-CycH-Mat1, cGK2, CK1d, CLK1, CLK2, DYRK1A, DYRK1B, DYRK3, PASK, PIM1 and PKD3.
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Of special interest is that riociguat
2022-04-11
Of special interest is that riociguat and NO donors decreased the phosphorylation of many proteins in human platelets. This aspect is presently under further investigation but a few comments can be made already here. Of the extensive spectrum and diversity of human protein kinases and protein phosph
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Enzyme parameters obtained for GC E
2022-04-11
Enzyme parameters obtained for GC-E variants can further be introduced in kinetic models of phototransduction using computational approaches. A similar approach has been successfully applied in the investigation of disease causing mutations of GCAP1 to simulate rod and cone photoresponses under dise
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br Acknowledgments This research was partially supported by
2022-04-11
Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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br GPR GPR has been described as a
2022-04-11
GPR55 GPR55 has been described as a type 3 cannabinoid receptor due to its ability to detect endocannabinoids and may play a role in the endocannabinoid lipid sensing system [28]. GPR55 is activated by both cannabinoid endogenous agoinsts (endocannabinoids) and non-cannabinoids fatty acids namely
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br Action of GPR in metabolically active tissues In addition
2022-04-11
Action of GPR55 in metabolically active tissues In addition to being highly expressed by discrete brain regions, as described in Section 2, GPR55 is also expressed in a wide range of peripheral tissues, including spleen, adrenals and bone (Sawzdargo et al., 1999, Ryberg et al., 2007, Whyte et al.
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br Acknowledgments br Introduction Myelin one of the fundame
2022-04-11
Acknowledgments Introduction Myelin, one of the fundamental adaptations of vertebrates, is a multilamellar structure deriving from the spiral wrapping around the MTT of the plasma membrane of myelin forming glia, oligodendrocytes in the central nervous system and Schwann cells (SC) in the per
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Variants of NEIL were also analysed in Primary sclerosing
2022-04-11
Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo
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br Restart of Stalled Replication Forks By preventing
2022-04-11
Restart of Stalled Replication Forks By preventing the replisome from unwinding duplex DNA, ICLs stall progression of the replication fork, which in turn results in genomic instability 41., 42.. As in prokaryotes, the conventional mechanism of ICL repair in eukaryotes involves the combined activi
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P gps expressed in cells and tissues of human
2022-04-11
P-gps, expressed in BMS-911543 and tissues of human and animals, play an active role in cellular protection against multiple toxicants by transporting them out of a cell. Thus, improving transport activity of P-gp may contribute to removing Cd from living oysters. Cd accumulation in the cultured ce
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br Conclusion Membrane transporters remain relatively
2022-04-11
Conclusion Membrane transporters remain relatively understudied in human disease, especially TBI (Cesar-Razquin et al., 2015), and considerably less is known in terms of expression, function and substrates of membrane transporters in pediatric patients. However, their importance in maintaining XI
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br Funding sources This work was supported in part
2022-04-09
Funding sources This work was supported, in part, by NIH GM115388 to BGM. Acknowledgements Introduction Glucokinase (GCK) plays a central role in the regulation of glucose metabolism. Its activity is restricted to Phenyl sulfate with important roles in whole-body glucose homeostasis [1]. I
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In this study we describe the expression of galr
2022-04-09
In this study, we describe the expression of galr2a and galr2b in zebrafish embryos using whole-mount in situ RNA hybridization. To further analyze the distribution of GALR2b and its interactions with galanin, we generated Tg(galr2b:egfp) zebrafish, which express EGFP under the control of a galr2b p
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All data were analyzed using
2022-04-09
All data were analyzed using SAS software (version 9.3, SAS Institute Inc., Cary, NC). Because of very low FFAR1 protein detection (at the detection limit or no signal) in 3 H-BHB cows, quantification was not possible within a linear range and therefore these animals were omitted from the statistica
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The pharmacokinetic properties of were amenable to oral dosi
2022-04-09
The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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