• The identification of CRF receptor subtypes has led to a

  2021-01-04

  

  The identification of CRF ack1 inhibitor subtypes has led to a number of studies addressing its functional properties. This paper examines the evidence for CRF1 and CRF2 mediation of fear and anxiety. Recent reviews discussing specific CRF receptor functions associated with other conditions includi

• Dipraglurant br Material and methods br Results Diagrammatic

  2021-01-04

  

  Material and methods Results Diagrammatic representations showing the bilateral injection sites in the BNST of all animals used in the present study are presented in Fig. 1. Discussion The present results provide the first evidence that both CRF1 and CRF2 receptors in the BSNT are involved

• Animal studies investigating the role

  2021-01-04

  

  Animal studies investigating the role of D1 dopamine receptors in the PFC have focused on delayed response tasks, which require online maintenance of a previously presented stimulus. Striatal dopamine is thought to be important for flexibility and updating goal representations when new information i

• cytoskeleton Several cholinesterase inhibitors have also

  2021-01-04

  

  Several cholinesterase inhibitors have also been radiolabelled with 11C as potential cholinesterase imaging agents. These include 11C-donepezil, 11C-methyltacrine, and 11C-physostigmine, which also have had limited success in demonstrating the known histochemically defined cholinesterase distributio

• PF-03084014 synthesis Although the analysis described above

  2021-01-04

  

  Although the analysis described above goes far to explain the mechanism of PF-03084014 synthesis perturbations through CHK1 inhibition, it raises important questions about the mechanism by which WT RAS isoforms promote CHK1 S280 phosphorylation. Previous reports have shown that both the MAPK-RSK and

• Our previous high throughput screening HTS

  2021-01-04

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based FITC, Fluorescein isothiocyanate assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimization

• Our previous high throughput screening HTS

  2021-01-04

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based pcpt assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23], [2

• br Materials and methods br

  2021-01-04

  

  Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th

• br Rationale and hypothesis To discover an allosteric inhibi

  2021-01-04

  

  Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be

• Ligand independent constitutively active variants have also

  2020-12-31

  

  Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o

• p kip is a member of the cyclin dependent kinase

  2020-12-31

  

  p27kip1 is a member of the cyclin-dependent kinase (CDK) inhibitor family that acts as a potent tumor suppressor in a variety of human cancers and negatively regulates the transition of cells from the G1 to S phase of the cell cycle, protects against inflammatory injury and promotes epithelial diffe

• Sensory gating describes a filter mechanism protecting the c

  2020-12-31

  

  ‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits opioid receptors to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al., 2003). Au

• Our recent QTL mapping study revealed that the adaptor

  2020-12-31

  

  Our recent QTL mapping study revealed that the adaptor genes, including the NCK genes and the ABI genes, are located within the genomic regions harboring the most significant QTL (Zhou et al., 2017), suggesting that these genes could be involved in the determination of resistance, and possibly throu

• br Transparency document br Introduction The

  2020-12-31

  

  Transparency document Introduction The cyclic nucleotide adenosine 3′,5′-cyclic monophosphate (cAMP) exerts both an endothelium-dependent and an endothelium independent vasorelaxant action in rat SLIGKV-NH2 synthesis [1]. cAMP direct, endothelium-independent vasorelaxant effects have been attr

• Since OH PGE is a moderately selective EP agonist which

  2020-12-31

  

  Since 1-OH-PGE2 is a moderately selective EP4 agonist which could bind to mouse EP3 and EP4 with a relatively similar affinity (Kiriyama et al., 1997), we have used a highly selective EP4 agonist CAY10580 to evaluate the involvement of EP4 activation in PGE2-facilitated EP4 internalization and recyc

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