• glycine receptors Two major categories of arginase inhibitor

  2022-10-13

  

  Two major categories of arginase inhibitors have been distinguished (Fig. 3): the first category comprises synthetic arginase inhibitors, which have been developed from the substrate l-arginine [35]; and the second category includes inhibitors derived from natural products [36]. The category of synt

• Because of the critical roles

  2022-10-13

  

  Because of the critical roles played by AMPK in energy sensing and cancer cell survival, a huge number of drugs have been proposed to exert their pharmacological effects by means of AMPK activation (Kim and He, 2013). For example, metformin has been shown to activate AMPK in muscle (Sajan et al., 20

• The molecular mechanisms that mediate the plasticity of the

  2022-10-13

  

  The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct

• br Brain cell reactions Brain

  2022-10-13

  

  Brain cell reactions Brain cells in common with all metabolic cells must contain chemically active primary compounds which spontaneously initiate and continue cell reactions under normal conditions of temperature and pressure (NTP). These compounds have been identified as monophosphoric and polyp

• Pranlukast An important observation is that this patient

  2022-10-13

  

  An important observation is that this patient has been on ALK inhibitor for more than 4 years (51 months: 27 months on crizotinib+24 months on alectinib and on-going) and there was no evidence of disease progression in the central nervous system. The other potential driver mutation in this patient’s

• Serum soluble sCD is a shedding product from

  2022-10-13

  

  Serum soluble sCD21 is a shedding product from the ectodomain of membrane CD21 after B cell activation (Masilamani et al., 2003, Masilamani et al., 2004a, Masilamani et al., 2004b, Grottenthaler et al., 2006, Hoefer et al., 2008), which resembles the ligand-binding capacity of intact CD21 (Wu et al.

• br Funding br Introduction l Dihydroxyphenylalanine l DOPA i

  2022-10-13

  

  Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side

• In cancer cells HIF upregulates

  2022-10-12

  

  In cancer cells, HIF-1α upregulates HK-II expression by binding to the hypoxia-responsive element in the HK-II promoter region to adapt to hypoxic conditions [20]. In the present study, we observed that mangiferin transiently increased HIF-1α expression in endothelial cells, suggesting another possi

• There is no doubt that GPR is a

  2022-10-12

  

  There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago

• Rapid action of E on

  2022-10-12

  

  Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor

• br The GLI code The

  2022-10-12

  

  The GLI code The GLI code model [21], [22] considers the total GLI function as a balance of positive activator (GLIA) and negative repressive (GLIR) activities with GLI1 being mostly a positive transcription factor and GLI3 mostly a transcriptional repressor. The GLIA:GLIR ratio is thus critical,

• Another small compound targeting IBAT has been evaluated in

  2022-10-11

  

  Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause

• Natural product based drug discovery can be enhanced with co

  2022-10-11

  

  Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in Natural Product Library binding assays, we used molecular modeling to predict how well thes

• FPR family Human FPR was first

  2022-10-11

  

  FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c

• The typical pharmacophore for GPR agonists contains

  2022-10-11

  

  The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors

13160 records 350/878 page Previous Next First page 上5页 346347348349350 下5页 Last page