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In contrast exposure of CRF a receptors to h
2020-11-23
In contrast, exposure of CRF2(a) receptors to h/rCRF in living cells produced a strikingly weak translocation of βarrestin2 to the membrane. Specifically, we found a markedly lower magnitude and slower rate of βarrestin2 recruitment to CRF2(a) receptors in response to h/rCRF concentrations as high a
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The synthesis of tricyclic analogs
2020-11-23
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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Finally the recent work to define the microcircuitry of the
2020-11-23
Finally, the recent work to define the microcircuitry of the central amygdala and the role of specific cell populations in fear conditioning can stand as a useful model for advances in preclinical alcohol research. To date, the role of the amygdala in alcohol-related behaviors, and reward-related be
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Peptides undergoing only a single hydroxylation
2020-11-23
Peptides undergoing only a single hydroxylation, i.e. PA-Hyp-KPAPK and PAPK-Hyp-APK, were then used to investigate the kinetics of vCPH co-factor and co-substrate dependences. The values for KMapp for Fe(II) and KM for 2OG for the two peptide substrates were within error (KMapp, Fe(II): 0.9 μM ± 0.1
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Tacalcitol Our results for imidacloprid were
2020-11-23
Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic Tacalcitol receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes in Im concentrations. Ho
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The present study is the first time to investigate the
2020-11-23
The present study is the first time to investigate the effect of piperine on intestinal sterol transporters and enzymes in the small intestine. NPC1L1 is a sterol transporter responsible for taking up cholesterol from the lumen to enterocytes (Davis et al., 2004). ACAT2 is an enzyme, which esterifie
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So what can we glean from this illuminative foray into
2020-11-23
So what can we glean from this illuminative foray into how Chk1 and MK2 participate in checkpoint control? First and foremost, this work reveals that KW-2478 deficient in the tumor suppressor p53 contain two spatially distinct G2/M phase checkpoint control kinase networks. This provides compelling
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Initially studies of GPCRs predominantly assessed
2020-11-23
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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Several studies have already shown that mPR
2020-11-23
Several studies have already shown that mPR activation can significantly reduce intracellular cAMP levels in different kind of cells, such as GT1-7 neuronal cells [32], MDA-MB-468 breast cancer cells [55] and primary vascular endothelial cells [56]. The experiments performed with PTXa and 8-Br-cAMP
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By using live imaging of
2020-11-20
By using live imaging of an ERK fluorescence resonance energy transfer (FRET) sensor, the authors show that ERK activity propagates in a stepwise manner from the center to the periphery of the tracheal placode. This row-by-row propagation of ERK activity fits a relay model in which each row activate
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EP is the major receptor to mediate PGE induced
2020-11-20
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by 98059 receptor in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16], [26]. How
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PGE EP activation has been found to
2020-11-20
PGE2-EP4 activation has been found to attenuate the activation of microglia and to prevent lipid peroxidation and pro-inflammatory gene expression in a murine model of lipopolysaccharide (LPS)-induced thrombin inhibitors inflammation [15]. Moreover, PGE2/EP4 signaling has elicited a protective func
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br Conclusions Nanoparticles can be
2020-11-20
Conclusions Nanoparticles can be used to modulate the catalytic activity of various industrially and clinically useful enzymes, as well as pH, temperature and storage stabilities, which will enable the process to occur more efficiently and less costly. The interaction between an enzyme and nanopa
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While agnathans appear to have reduced their Ednr repertoire
2020-11-20
While agnathans appear to have reduced their Ednr repertoire to the Ednra gene (that may have been amplified in the Arctic lamprey), gnathostomes in general have been relatively inert to Ednr gene loss. Strikingly, the only Ednr gene that has been lost repeatedly is EdnrB2 (lost in therian mammals,
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Ubiquitination can occur on a single monoubiquitination or s
2020-11-20
Ubiquitination can occur on a single (monoubiquitination) or several (multiubiquitination) lysine residues, or the same lysine residue can be subjected to several rounds of Ub conjugation (polyubiquitination). Ub bonds within polyUb chains are formed through 1 of 7 lysine residues in Ub, and the typ
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