• br Introduction Type Diabetes mellitus T DM is a

  2021-04-19

  

  Introduction Type 2 Diabetes mellitus (T2DM) is a metabolic disorder that raises blood glucose level for a prolonged time. T2DM is associated with acute complications like ketoacidosis, hyposmolar coma, chronic complications include heart disease, stroke, kidney failure, foot ulcers and damage to

• Dipeptidyl peptidase inhibitors DPP is

  2021-04-19

  

  Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit CZC-25146 secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficacy has

• Proof of concept studies with disulfiram

  2021-04-19

  

  Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d

• Given the widespread occurrence of oncogene induced

  2021-04-19

  

  Given the widespread occurrence of oncogene-induced RS and the increasing clinical interest in small molecule inhibitors that further exacerbate RS in human cancers (such as ATR inhibitors), our findings point to a protective role for RAD52 in the maintenance of cancer cell viability. As such, RAD52

• RN486 br Materials and methods br Results br Discussion GOS

  2021-04-19

  

  Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy

• The molecular formula of was assigned as

  2021-04-19

  

  The molecular formula of 2 was assigned as C12H12N2O2 by the positive HRESIMS at m/z 217.0973 [M+H]+ (calcd for 217.0972), 13C NMR and DEPT spectra, having 8 degrees of unsaturation. The 1H NMR spectrum contains an ABX spin system comprised of resonances at δH 7.47 (d, J=1.9Hz, H-2′), 6.86 (d, J=8.3

• 88 3 sale Pyrazolopyrimidines are bioisostere of purine exhi

  2021-04-17

  

  Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase 88 3 sale [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour and leuka

• Recently we have observed that

  2021-04-17

  

  Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti

• In conclusion this study provides the first investigation

  2021-04-17

  

  In conclusion, this study provides the first investigation of role of ACC receptors in parasitic nematodes. While research using C. elegans to evaluate anthelmintic targets is an excellent tool to provide relevant information, research on similar targets in parasitic nematode can provide key informa

• br Materials and methods br Results br Discussion In

  2021-04-17

  

  Materials and methods Results Discussion In this study, we confirmed the activation of Akt by udenafil in 3T3-L1 cells. To elucidate the underlying mechanism of udenafil, we focused on the mitochondria. Our findings demonstrated that udenafil improved mitochondrial function and expression o

• In the present study we determined concentration

  2021-04-17

  

  In the present study, we determined concentration–response relationships for selected synthetic progestogens using in vitro luciferase transactivation assays driven by PR, ARα and ARβ from Murray–Darling rainbowfish () and compared the profiles with those obtained from similar assays based on human

• In the brain E can modulate

  2021-04-17

  

  In the brain, E2 can modulate the mitogen-activated protein kinases/extracellular signal-regulated kinases (MAPK/ERK) pathway, which is involved in the formation of different memory types (Atkins et al., 1998, Blum et al., 1999, Schafe et al., 2000). When the MAPK/ERK signaling pathway is activated,

• br Materials and methods br Results br Discussion

  2021-04-17

  

  Materials and methods Results Discussion The oestrogen agonist properties and androgen antagonist activities of parabens have been well documented by a variety of in vitro and in vivo assay systems over the past decade (Chen et al., 2007, Darbre and Harvey, 2008, Golden et al., 2005). To th

• Accordingly we prepared three compounds and as shown

  2021-04-17

  

  Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available mk-801 with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced undesired compound rath

• We not only found that the ISR leads to

  2021-04-17

  

  We not only found that the ISR leads to attenuation of conventional cap-dependent translation with no change in RAN translation of the G4C2 expanded repeat, but also that GA translation from the expanded repeat (but not from 5 G4C2 repeats, perhaps because the protein product does not aggregate) is

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