• Following activation of mGluRs GRIP stabilized AMPARs appear

  2024-12-07

  

  Following activation of mGluRs, GRIP-stabilized AMPARs appear to be the primary target for endocytosis. Consistent with this model, we find that using siRNA to reduce GRIP1/2 expression blocks the AMPAR internalization and the synaptic depression mediated by mGluRs. Reductions in GRIP1/2 expression,

• The first identified auxiliary subunit stargazin is essentia

  2024-12-07

  

  The first identified auxiliary subunit, stargazin, is essential for AMPAR function in cerebellar granule neurons (Hashimoto et al., 1999). Subsequently, a family of six transmembrane AMPAR regulatory proteins (TARPs) were defined that modify channel trafficking, gating, and pharmacology (Kato and Br

• A central question that arises

  2024-12-07

  

  A central question that arises in this discussion is whether enhanced neurobehavioral responses to food cues emerge as a consequence of weight gain, or whether there are intrinsic differences in the motivational responses to food cues that precede weight gain. In support of pre-existing differences,

• In pancreatic islets we found an

  2024-12-07

  

  In pancreatic islets we found an increase in protein expression of leukocyte 12/15-LO that paralleled the metabolic decline characterized by severe hyperglycemia and reduced islet numbers. Similar increase in 12/15-LO expression by Western blot was found in the control mice, which have a normal meta

• Targeted disruption of the Akt gene in mice induces

  2024-12-07

  

  Targeted disruption of the Akt1 gene in mice induces a growth retardation phenotype [4,19]. Akt2 KO mice reveal mild growth retardation and insulin resistance [4,20,21]. Akt1/2 double KO (DKO) mice display severe growth deficiency and die shortly after birth. These mice exhibit impaired bone and ski

• Nrf br AhR br Nrf and AhR friends or

  2024-12-07

  

  Nrf2 AhR Nrf2 and AhR: friends or foes for energetic metabolism? Perspectives in carcinogenesis upon xenobiotic exposure Acknowledgements Introduction Integration of endogenous and exogenous signals via appropriate receptors is at the core of biological differentiation and adaptive r

• br Theoretical mechanism of ABCA activity in

  2024-12-07

  

  Theoretical mechanism of ABCA2 activity in LE/LY in modulation of cholesterol trafficking It is important to confirm that ABCA2 is a lipid transporter and identify the substrates that are mechanistic in its cholesterol sequestering activity. We hypothesize that ABCA2 modulates cholesterol sequest

• Previous studies suggest that TGF contributes to

  2024-12-07

  

  Previous studies suggest that TGF-β contributes to the pathogenesis of diabetic renal injury [47]. TGF-β stimulates matrix production and prevents matrix degradation, which leads to increase collagen deposition and glomerulosclerosis [48]. In the current study ABT702 significantly reduced renal coll

• alverine br Introduction Epilepsy is characterized by

  2024-12-07

  

  Introduction Epilepsy is characterized by spontaneous recurrent seizures and represents one of the most frequent neurological diseases affecting about 60 million people worldwide (McNamara, 1999). It is estimated that up to 50% of all cases are triggered by “initial precipitating injuries”, such

• Application of the broad acting

  2024-12-06

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• br Acknowledgements We thank Dr Stefan Schulte

  2024-12-06

  

  Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific

• The combination of Aurora kinase inhibitors with standard

  2024-12-06

  

  The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the

• Aurora A overexpression is also

  2024-12-06

  

  Aurora-A overexpression is also related to the activation of NF-κB, a potent anti-apoptotic effector that may play a role in preventing apoptosis in cancer Annexin V-Cy3 Apoptosis Kit Plus [18]. These data show that we are still at the beginning of unraveling the complex mechanism by which these g

• Ryoichi et al modified potent clinical candidate VX

  2024-12-06

  

  Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos

• In PMCA Mg favors the conversion E P E P

  2024-12-06

  

  In PMCA, Mg2+ favors the conversion E1P → E2P [13] and, as in SERCA [11], it accelerates the phosphorylation displacing the E1–E2 equilibrium towards E1. In SERCA, Sørensen et al. [41], proposed that ATP reacts by an associative mechanism mediated by two Mg2+ ions to form an aspartyl-phosphorylated

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