• Whereas allostery in the cell is relatively understudied sig

  2024-04-12

  

  Whereas allostery in the β cell is relatively understudied, significant progress has been made in understanding the physiology and mechanistic biology of how AMPK and its upstream kinases govern β cell function. LKB1 phosphorylates AMPKα at Thr172 [21], and loss of LKB1 in β cells abolishes phosphor

• br Experimental methods br Acknowledgments br Introduction L

  2024-04-12

  

  Experimental methods Acknowledgments Introduction Long-term potentiation (LTP) and long-term depression (LTD) at excitatory synapses are thought to underlie experience-dependent learning and memory. These synaptic plasticity mechanisms are best characterized at hippocampal CA1 synapses, whe

• In order to postulate its binding mode in APN compound

  2024-04-12

  

  In order to postulate its binding mode in APN, Phentolamine Mesylate 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occ

• ACh induced changes in respiratory frequency could be

  2024-04-12

  

  ACh-induced changes in respiratory frequency could be of interest. They may reveal an important mechanism of respiratory modulation at the caudal NTS level. ACh-induced increases in respiratory frequency within this region have been also reported by Furuya et al. (2014). Changes in respiratory timin

• Regarding brain tumors AXL has been implicated in gliomagene

  2024-04-11

  

  Regarding CH 223191 tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochemical analysis of AXL and G

• AT signaling is distinct to that of

  2024-04-11

  

  AT2 signaling is distinct to that of AT1 (Kaschina and Unger, 2003). As shown here, opposite to the stimulating effect of AT1 signaling, it inhibits apelin secretion. Activation of AT2 receptor, which is also G-protein coupled, is known to decrease cAMP and cGMP levels by inhibiting adenylyl cyclase

• br Under normal physiological conditions the agonist binds t

  2024-04-11

  

  Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G

• Recent studies revealed that certain plant derived compounds

  2024-04-11

  

  Recent studies revealed that certain plant-derived compounds can also interfere with AR function. One way of such an interference is by modulating its expression levels. This is the case for the two flavonoids quercetin and luteolin that have been reported to repress the function of AR by inhibiting

• br Results and discussion In order to

  2024-04-11

  

  Results and discussion In order to investigate the assembly dynamics and aggregate structures of Aβ16-22, twelve molecular systems with the number of peptides varying from 1 to 12 were studied. In all simulations, the same peptide concentration (~15 mM) was maintained by adjusting the dimensions

• br AMPK as a druggable target AMPK signaling

  2024-04-11

  

  AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in

• The lactam emerged as lead candidate due to its high

  2024-04-11

  

  The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok

• Through systematic deletion of AhR in specific cell

  2024-04-11

  

  Through systematic ryanodine of AhR in specific cell types, Di Meglio et al. (2014) revealed that AhR in keratinocytes and fibroblasts are key to the exacerbated psoriatic phenotype induced by IMQ in AhR-deficient mice. This emphasizes the crosstalk between keratinocytes and the immune system to re

• Lee et al have demonstrated that APPL associates with

  2024-04-10

  

  Lee et al. have demonstrated that APPL1 associates with AdipoR1 in Hek293 CID 755673 where both proteins have been overexpressed with suitable tags [16]. In contrast to recent data the formation of this complex is not enhanced by exogenous adiponectin [16], [33]. Knock-down of APPL1 reduces the lev

• KX2-391 dihydrochloride br Conclusion The HT receptor family

  2024-04-10

  

  Conclusion The 5-HT receptor family is complex, and one may ask as does Bryan Roth et al. [205] whether this is useless KX2-391 dihydrochloride (i.e. too much redundancy) or an embarrassment of the riches (i.e. many potential targets to choose from to affect normal or pathological function); mole

• A selected set of these new derivatives

  2024-04-10

  

  A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil

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