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Through the analysis of various
2022-01-04

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic (±)-Anatoxin A fumarate motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of d
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br Sodium glucose co transporter inhibitors SGLT i are
2022-01-04

Sodium-glucose co-transporter-2 inhibitors (SGLT2i) are the latest class of non-insulin glucose-lowering agents that facilitate glycaemic control by inhibiting renal glucose reabsorption, thus promoting glycosuria. Canagliflozin, dapagliflozin, and empagliflozin are the three commonly used agents
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In the present study five Glu substituted analogues
2022-01-04

In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Growth hormone secretagogue receptor GHSR is a member of
2022-01-04

Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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Having shown that some of substitutions Cl CF
2022-01-04

Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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Similar to in vitro data in
2022-01-04

Similar to in vitro data, in vivo studies have also revealed modulation of TLR4-induced inflammatory responses by AEA. The proposed AEA reuptake inhibitor AM404 has been shown to attenuate TLR4-induced increases in plasma levels of IL-6 and IL-1β, the latter effect mediated by CB1 receptor activatio
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Aberrant activity of PRC as a result
2022-01-04

Aberrant activity of PRC2 as a result of over expressed EZH2, has been frequently seen in a wide range of human cancers including breast and prostate tumors [10]. However, leukemia-associated epigenetic aberrations are not fully understood [7]. Herein, we will overview the current knowledge of epige
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br Discussion This study dedicated
2022-01-03

Discussion This study, dedicated to Ro 31-8220 synthesis H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition o
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br S proteins and HBV induced
2022-01-03

S proteins and HBV-induced autophagy HBV surface proteins (S proteins or HBs) are reported to trigger HBV-induced autophagy by inducing ER stress and UPR in host Bacitracin [22]. HBx and HBV-induced autophagy HBx is a multifunctional viral protein. It can regulate virus replication, promote
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A repertoire of cytotoxic payloads is
2022-01-03

A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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In the brain hydrolysis of
2022-01-03

In the brain, hydrolysis of 2-AG by MGL is the primary source of AA for conversion to PGs by cyclooxygenase (Nomura et al., 2011). PGE2 production is required for IL-1β-evoked synapse loss (Mishra et al., 2012). Here, we tested whether decreased PG levels contributed to the synapse protective effect
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br Results and discussion br Conclusions br
2022-01-03

Results and discussion Conclusions Introduction There is no effective treatment for HIV-associated neurocognitive disorder (HAND) which affects about half of the over 36 million people infected (Saylor et al., 2016). HIV can remain in the MDL800 during combination antiretroviral therapy (E
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br The presence of an active glyoxalase
2022-01-03

The presence of an active glyoxalase pathway in an apicomplexan parasite was first reported in Plasmodium falciparum-infected erythrocytes (Vander Jagt et al., 1990). Some years later, glyoxalase I and both glyoxalase II enzymes were characterized in this parasite (Akoachere et al., 2005, Iozef et
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The vast majority of clinical studies have shown that
2022-01-03

The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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br Conflict of interest statement br Acknowledgements This w
2022-01-03

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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