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Etoposide VP a semisynthetic podophyllotoxin
2022-06-13

Etoposide (VP-16), a semisynthetic podophyllotoxin derivative agent, is widely used as a chemotherapic treatment for many cancers (Hande, 1998). VP-16 has been known that its activity is mediated by the interaction with topoisomerase II (an ATP-dependent nuclear enzyme) which regulates DNA topology
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br GPR GPR has been described as a
2022-06-13

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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To assess the roles of GPR
2022-06-13

To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) ci-1033 synthesis from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh120
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Ubiquitination of GlyRs subunit on plasma
2022-06-13

Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor Meropenem synthesis and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also, the functional co
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Sulfo-NHS-SS-Biotin receptor br Conflict of interest stateme
2022-06-13

Conflict of interest statement Acknowledgements This work was supported by the National Health and Medical Research Council of Australia (NHMRC) (project grants [1061044], [1065410] and [1126857], and NHMRC program grant [1055134]); P.M.S. and A.C. are NHMRC Principal and Senior Principal Rese
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Clinical trials of all GSIs have ended prematurely
2022-06-10

Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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In summary this study demonstrated
2022-06-10

In summary, this study demonstrated the cDNA cloning and characterization of the galanin type II receptor (GalR2) and a novel GalR2-like receptor (GalR2-L) in chickens, in which these two receptors are possibly originated from a gene Phenyl sulfate event that occurred in the early vertebrate lineag
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The current gold standard for diagnosing
2022-06-10

The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) BMS-303141 (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid and
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We tested formyl MYVKWPWYVWL which we had previously
2022-06-10

We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi
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With the identification of small nonpolar substituents at
2022-06-10

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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In the FARM motifs of GGPPSs
2022-06-10

In the FARM motifs of GGPPSs, hydrophobic Isoniazid australia are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP syntha
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The molecular target of N BPs is
2022-06-10

The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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Our data show that oxidative stress high
2022-06-10

Our data show that oxidative stress (high levels of ROS) suppresses the process of lysosomal exocytosis, which would be predicted to impair the expulsion of toxic compounds from cells. Therefore, we propose that ROS have a biphasic effect on the lysosomal clearance: consistent with their role as a s
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In contrast to RhoA Rac and Rap which are
2022-06-10

In contrast to RhoA, Rac1 and Rap1 which are stimulated by platelet activators and inhibited by NO/PKG, the GTPase ADP-ribosylation factor 6 (Arf6) is regulated in the reverse way. Platelet agonists like thrombin, collagen, or ADP, reduce Arf6-GTP levels, whereas NO and PGI2 oppose this reduction [1
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Furthermore the role of GSK in the pathogenesis of inflammat
2022-06-10

Furthermore, the role of GSK-3 in the pathogenesis of inflammation has been widely documented as it accompanies inflammatory conditions such as diabetes mellitus, mood disorders, Alzheimer’s disease, cancer (Jope et al., 2007), and has been associated with atherothrombotic CVD events. However, anoth
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