• br TGR Agonists br FXR TGR Dual Agonists In a

  2022-09-20

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• br TGR Agonists br FXR TGR Dual Agonists In a

  2022-09-20

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• br Material and methods br Results br Discussion

  2022-09-19

  

  Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In RGDfK receptor to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]. Thi

• Recently Bristol Myers Squibb and Merck reported their GPR

  2022-09-17

  

  Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic Ramipril derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists w

• Active compounds and were further tested and

  2022-09-17

  

  Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of (E

• A common feature of ferroptosis is

  2022-09-17

  

  A common feature of ferroptosis is the iron-dependent accumulation of lipid-ROS and the subsequent depletion of polyunsaturated fatty thymidylate synthase phospholipids (PUFA-PLs) [118]. The PUFA chains of membrane lipids are more susceptible to both enzymatic and non-enzymatic oxidation, which res

• Nonetheless several questions remain to

  2022-09-17

  

  Nonetheless, several questions remain to be answered about FAAH inhibition to address cannabis use disorder. The trial was of short duration (4 weeks), whereas most clinical trials in this field have been for 8–12 weeks., , , Although motivational deficits are commonly present in cannabis users and

• Several named antagonist ligands have figured noticeably in

  2022-09-17

  

  Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l

• The mode of action of m Tyr has not been

  2022-09-16

  

  The mode of action of m-Tyr has not been fully recognized. The primary/basic mechanism of action of m-Tyr is thought to be associated with the incorporation of this NPAA into the structure of proteins resulting in formation of dysfunctional proteins [11], [12]. m-Tyr is incorporated into proteins in

• In the pathogenesis of insulin resistance chronic activation

  2022-09-16

  

  In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph

• Lactate LA the end product of

  2022-09-16

  

  Lactate (LA), the end product of aerobic glycolysis, has been long neglected and seen as a byproduct until recently the findings for its important role in global gene transcription, cancer progression, functional polarisation of immune dexamethasone acetate receptor and the sustenance of stem cells

• Lonidamine synthesis Finally our data found that the

  2022-09-16

  

  Finally, our data found that the EBV dUTPase protein modulates tryptophan, serotonin, and DA metabolism and use in vitro and in vivo. The EBV dUTPase may alter kynurenine catabolism in microglia in vitro, suggesting that there is an increase synthesis of quinolinic acid. Quinolinic acid, an agonist

• SGCs tightly ensheath the soma of DRG neurons Costa and

  2022-09-16

  

  SGCs tightly ensheath the soma of DRG neurons (Costa and Moreira, 2015, Hanani, 2005, Takeda et al., 2009). Intimate associations between SGCs and neurons facilitate bidirectional regulation of SGC function and neuronal excitability. After nerve injury, neuronal hyperexcitability can result in SGC a

• To maintain low Glu concentrations in the synaptic cleft

  2022-09-16

  

  To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino GDC-0834 is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and in

• br Acknowledgements This work is supported

  2022-09-16

  

  Acknowledgements This work is supported by the Cognitive Sciences and Technologies Council of Iran (CSTC, Grant No. 95P31), the Iran National Science Foundation (INSF) and the Faculty of Medical Sciences, Tarbiat Modares University, Tehran, Iran. The authors wish to thank Dr. Ayat Kaeidi for his

15521 records 359/1035 page Previous Next First page 上5页 356357358359360 下5页 Last page