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In conclusion we have identified ten novel GPCR genes and
2021-10-26
In conclusion, we have identified ten novel GPCR genes and a pseudogene. Transcripts for GPR78, GPR81, GPR94, GPR95, GPR101, GPR103 and P2Y were detected in various CNS and peripheral tissues. Given the high levels of identity observed within paralogous oGPCR gene clusters, future efforts will likel
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The combination of niacin with a
2021-10-26
The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su
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For a long time the mechanism
2021-10-26
For a long time, the mechanism for the TG-lowering effect of nicotinic HJC 0350 synthesis has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested the
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Some studies show that testosterone
2021-10-26
Some studies show that testosterone may be involved in regulating cell proliferation and its stimulating effect has been proved in castrated rats (Wainwright et al., 2011), but not in mice and meadow voles (Ormerod and Galea, 2003; Benice and Raber, 2010). However, the seasonal difference in cell pr
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The unique mechanism of EAAT anion channel gating results in
2021-10-26
The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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Although domain organization had been clearly delineated by
2021-10-26
Although domain organization had been clearly delineated by the 4.3-Å structure of T4-γ-secretase [], atomic modeling of the side chains had to wait for the 3.4-Å structure []. In total, 598 residues in the transmembrane region and 632 residues in the ECD were modeled for the four components of huma
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Recent studies have elucidated a profound role
2021-10-25
Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty TAME or synthetic ligands
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Although pharmacological studies from the end of the th cent
2021-10-25
Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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The Jumonji JmjC domain containing KDM family
2021-10-25
The Jumonji (JmjC) domain-containing KDM family members can be clustered into seven subfamilies (KDM2 – KDM8). The KDM2 cluster catalyzes H3K36me2/me1 demethylation; in addition, KDM2B/JHDM1B/FBXL10 has been suggested to catalyze demethylation of H3K4me3 [3]. Cell culture studies support that KDM2 p
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Electrochemical techniques have attracted broad
2021-10-25
Electrochemical techniques have attracted broad attention for their outstanding advantages, such as satisfactory sensitivity and convenient operation. Nowadays, nucleic Compstatin nanostructures such as DNA tetrahedron structure, nucleic acid-mimicking structure, exhibit noticeable application in t
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JNJ 5207852 dihydrochloride receptor The analytical approach
2021-10-25
The analytical approach for the simultaneous determination of HA and its metabolites is complex. There are commercial kits that allow the determination of HA through ELISA and of its metabolites through radioimmunoassay (RIA) techniques. However, these immunological-based techniques do not allow sim
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Substitutions V L F V
2021-10-25
Substitutions V36L, F43V and Q80H were identified in the present study. RAS V36L is associated with resistance to boceprevir [18]. In 2015, Brazilian clinical practice guidelines on the management of hepatitis C no longer included combined therapies with boceprevir or telaprevir as a treatment optio
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We also noticed that acetic acid by itself
2021-10-25
We also noticed that acetic acid by itself (used to induce pain) increased spinal cord levels of KYNA (see Fig. 5). The most rational explanation of this finding is based on the possibility that acetic acid and KYNA share the same transport systems and the finding is therefore not surprising. Altho
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Cichlasoma dimerus as most teleost fish species present neur
2021-10-25
Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most rxr receptor species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (Gonzál
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br Conclusion In summary a series
2021-10-25
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic SRT2104 motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent ac
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