• Why do glutamate and glycine bind to

  2024-08-08

  

  Why do glutamate and glycine bind to the PKI-402 receptor in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN

• salubrinal Intracellular Signaling Cascades From ligand sens

  2024-08-08

  

  Intracellular Signaling Cascades. From ligand sensitization to translation of genes, all cellular processes are dependent on the intracellular levels and activity of partners involved in the signaling pathway. These signaling events lead to critical post-translational modifications including phospho

• Kim et al found that hydroxydopamine OHDA promoted the

  2024-08-07

  

  Kim et al. (2013) found that 6-hydroxydopamine (6-OHDA) promoted the atrophy of dopaminergic neurons associated with the activation of poly (ADP-ribose) polymerase (PARP), the translocation of apoptosis inductor factor (AIF) and the depletion of ATP. An increase in p-AMPK and pS6K (upstream kinase o

• ERAP has been crystallized in two

  2024-08-07

  

  ERAP1 has been crystallized in two different conformations, wherein the C-terminal domain IV is either closely interacting with domains I/II and enclosing the active site (termed ‘closed’), or is rotated away in a hinge motion which exposes the active site (‘open’). This large motion correlates with

• A unique finding in this study is

  2024-08-07

  

  A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic nitric oxide synthase inhibitor for substrate, can regulate CREB phosphoryation in the c

• The rescue of the behavioral deficit

  2024-08-07

  

  The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the Eribulin of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confirming previ

• We also measured macrophage infiltration

  2024-08-07

  

  We also measured macrophage infiltration and CLS presence in peri-gonadal AT from db/db mice and controls. CLS are morphological features within AT that are accurate indicators of adipocyte death and macrophage infiltration [56]. An earlier study showed that CLS macrophages account for >90% of the t

• Interestingly intermittent high doses of AKT inhibitors have

  2024-08-07

  

  Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula

• Pregnane X receptor PXR is a nuclear

  2024-08-07

  

  Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli

• The obtained results indicate that even when the impairment

  2024-08-07

  

  The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate

• In the vasculature it is known that A

  2024-08-07

  

  In the vasculature, it is known that A2A and A2B adenosine receptors are stimulatory for adenylyl-cyclase, leading to cyclic-AMP (cAMP) production and vasodilation, while the A1 and A3 adenosine receptors are linked to the inhibitory Gi, suppressing adenylyl-cyclase and favoring contraction. However

• br Conflict of interest br Financial

  2024-08-07

  

  Conflict of interest Financial support Acknowledgments This work was supported by the Japanese Millennium project. We thank all members of the Center for Genomic Medicine of RIKEN and Dainippon-Sumitomo Pharma Co., Ltd. for supporting this study. We are also grateful to members of the Hiros

• The SKOV and SKOV TR cells were

  2024-08-07

  

  The SKOV3 and SKOV3TR KW 3902 were exposed to stepwise increased concentration of paclitaxel with or without a different concentration of autophagy inhibitor (3-MA or HCQ) to further evaluate whether suppression of autophagy affected the growth and drug sensitivity of ovarian cancer cells in vitro.

• The allosteric site of class C receptors is

  2024-08-07

  

  The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201

• Previous investigations have established that aromatase acti

  2024-08-06

  

  Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w

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