• Theoretically the majority of resistance mechanisms identifi

  2021-10-19

  

  Theoretically, the majority of resistance mechanisms identified so far could be targeted by compounds that are already available, such as inhibitors of ER, PIK3CA/mTOR or FGFR1. However, the potential therapeutic advantage of combining these agents with standard HER2-targeting treatments must be wei

• Pharmacologic approaches of inhibiting GSNOR

  2021-10-19

  

  Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications

• Several studies have found that GPR possesses a distinct pha

  2021-10-19

  

  Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected bms 5 45 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rim

• Little is known about the role

  2021-10-19

  

  Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hypertensi

• br Acknowledgement This work was supported in part

  2021-10-19

  

  Acknowledgement This work was supported in part by grants from the Ministerio de Economía y Competitividad from Spain (BFU2011-23034). Introduction The glutamate hypothesis of schizophrenia emerged from observations in the 1960s that phencyclidine and similar psychotomimetic agents produce sc

• It is well known that GPCR

  2021-10-19

  

  It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling

• Ethanol decreased the value of desensitization for GluR Di C

  2021-10-19

  

  Ethanol decreased the τ-value of desensitization for GluR-Di. Coexpression of stargazin or γ4 further increased the effect of ethanol on desensitization (Fig. 3A, B). The highest ethanol concentration tested (200mM) reduced the τ-value by 16.5±4.9% (n=5) in the control receptors and by 29.3±9.3% (n=

• Unlike our present results in week

  2021-10-19

  

  Unlike our present results in 4–12-week-old (~1–3 months) females, where a high-fat-diet-induced increase in body weight was evident, Schmidt et al. exposed male glut3 mice to a similar high-fat diet (60% kilocalories from fat) and observed no change in body weight, plasma glucose or insulin concent

• br Presenilins and apoptosis Apoptosis also known as program

  2021-10-18

  

  Presenilins and apoptosis Apoptosis, also known as programmed cell death, has a critically important role in tissue homeostasis, development, normal ageing and the pathogenesis of several diseases, including cancer and neurological disorders. The presenilins were first linked to apoptosis when ce

• The Ala to Leu substitution

  2021-10-18

  

  The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several

• br Materials and methods br Results and

  2021-10-18

  

  Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka

• The molecular mechanism of gliotransmitter release is

  2021-10-18

  

  The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular Z-Ligustilide synthesis of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in gl

• br Future perspectives sGC signaling is important in the mai

  2021-10-18

  

  Future perspectives sGC signaling is important in the maintenance of multiple physiological functions. sGC is localized to cell membranes with both sGC Cys modifications and heme regulation identified as the crucial components in regulating sGC activity. Specifically, S-nitrosation of several com

• The fact that GSK recognition of its substrate

  2021-10-18

  

  The fact that GSK-3 recognition of its substrate involves pre-phosphorylation supports the rational for using synthetic phosphorylated peptides as substrate competitive inhibitors [57]. Phosphorylated peptides derived from the N-terminal pseudosubstrate sequence of GSK-3β were very weak inhibitors o

• Introduction Although G protein coupled receptor GPR was

  2021-10-18

  

  Introduction Although G-protein-coupled receptor 55 (GPR55) was considered a cannabinoid receptor, it differs phylogenetically from cannabinoid type 1 (CB1) and type 2 (CB2) receptors as it lacks the classic cannabinoid-binding pocket (Baker et al., 2006). GPR55 is sensitive to an array of cannabin

15668 records 538/1045 page Previous Next First page 上5页 536537538539540 下5页 Last page