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Acknowledgments The authors would like to thank members
2021-12-21

Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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br Acknowledgments This study was financially supported
2021-12-21

Acknowledgments This study was financially supported by National Science Center Poland grant No DEC-2011/02/A/NZ4/00031 (KKK), Jagiellonian University Medical College (Poland) grants: K/ZDS/007130 (SM) and K/ZDS/007131 (SM), COST Action CA15135 (DŁ, HS, KKK) and DFG INST 208/664-1 FUGG (HS). Than
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We also examined possible involvement
2021-12-21

We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p
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Several studies have found that GPR
2021-12-21

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected 1400W dihydrochloride expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, S
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br Pharmacology br Background to GPR function br
2021-12-21

Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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In addition to the increase of extracellular glutamate ICH c
2021-12-21

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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Glucagon regulates the transition from hepatic
2021-12-21

Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2
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Analysis of the GHSR screening data for inactive library
2021-12-21

Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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Inhibitors against the proteasome a component of the ubiquit
2021-12-21

Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor MK1775 and were shown to induce apop
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There are additional implications of subunit alterations in
2021-12-21

There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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br Introduction Currently HIV infection
2021-12-20

Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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br Materials and methods br Results br Discussion Reduced gl
2021-12-20

Materials and methods Results Discussion Reduced glutathione is considered to be one of the important regulators of REDOX balance in the biological system. The cellular concentration of 4-HNE under physiological conditions ranges from 0.1 to 3μM and has no detrimental effect in the biologic
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ap5 The manuscript provides mechanistic insights into the su
2021-12-20

The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 ap5 with MNF [
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In the present study we conducted a search
2021-12-20

In the present study, we conducted a search for other possible endogenous ligands for GPR35. We focused on lysophospholipids because of the homology (30%) between GPR35 and GPR55 whose endogenous ligand is lysophosphatidylinositol (LPI) [9], especially 2-arachidonoyl LPI [10]. Notably, the GPR35 gen
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To overcome these limitations investigators have
2021-12-20

To overcome these limitations, investigators have developed novel strategies for identifying and purifying gonadotropes from transgenic mouse models. For example, FSH-producing gonadotropes have been tagged in vivo with a transgenic cell surface antigen (H-2Kk) so that they can be purified in vitro
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