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Phylogenetic analysis of the secretin like hormones yields p
2022-06-14
Phylogenetic analysis of the secretin-like hormones yields poorly supported trees due to the short length of their peptide sequences (Dores et al., 1996). However, phylogenetic analyses typically show that the secretin-like peptides encoded by the proglucagon (glucagon, GLP-1 and GLP-2) and GIP Pert
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In summary this study shows that compound d has strong
2022-06-14
In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st
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Azaperone synthesis C steroids and their glycosylation produ
2022-06-14
C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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Endoxifen CaCl was from the Radiochemical Centre Amersham UK
2022-06-14
45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl
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D appears to be important
2022-06-14
D83 appears to be important for receptor function as a mutation to an alanine produced a non-functional channel. Interestingly, maintaining the charge as in D83E produced only a small reduction in GABA sensitivity. Other mutations at this position which included residues capable of hydrogen bonding
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br Competing interests br Authors contributions br Transpare
2022-06-14
Competing interests Authors contributions Transparency document Introduction Non-alcoholic fatty liver disease (NAFLD) is a spectrum of liver diseases ranging from simple steatosis to non-alcoholic steatohepatitis (NASH), which may further progress to liver cirrhosis and liver carcinoma
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The highest metabolic stability observed for compound k EC
2022-06-14
The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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In addition we assessed the viability of tetrahydroquinoline
2022-06-14
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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br Declarations of interest br Founding information
2022-06-14
Declarations of interest Founding information This work was partially supported by the New Energy and Industrial Technology Development Organization (NEDO) Japan [grant number P03043]; and Grants-in-Aid for Scientific Research [grant number 16H00738 to H.M.] from the Japan Society for the Prom
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Consistent with our gene profiling analyses showing
2022-06-14
Consistent with our gene-profiling analyses showing that genes involved in mutual compensation of EGFR or integrin/FAK were significantly downregulated by Tinagl1 overexpression, treatment with r-Tinagl1 inhibited the activation of EGFR and FAK in vitro, and phenocopied the combined inhibition of in
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br Conclusions Symptoms from bilateral
2022-06-14
Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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br Results br Discussion In this study six new
2022-06-13
Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of 133 2 synthesis unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in th
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MST are involved in signalling pathways following along the
2022-06-13
MST1/2 are involved in signalling pathways following along the canonical and noncanonical Hippo pathway. The canonical pathway is highly conserved between D. melanogaster and mammals and a master regulator of tissue growth. During development and within the canonical pathway, MST1/2 seem to have red
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br Concluding Remarks and Future Perspectives Our understand
2022-06-13
Concluding Remarks and Future Perspectives Our understanding of substrate targeting mechanisms utilized by kinases has grown tremendously in the past few years, but challenges still remain in relating these mechanisms to the organization of complex signaling networks. Substrate prediction based o
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Toxoplasma gondii is an exceptionally tractable apicomplexan
2022-06-13
Toxoplasma gondii is an exceptionally tractable apicomplexan parasite that expresses a limited yet representative subset of apicomplexan cyclase orthologs, making it an ideal model for investigating cyclic nucleotide signaling in Apicomplexa. Of the five putative nucleotide cyclases, only TgACα1 and
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