• The inhibition of HDAC increases the level of

  2021-09-11

  

  The inhibition of HDAC increases the level of histone acetylation and consequently turns the chromatin to be loose and active, allowing multiple transcription factors to access to promoters of diverse genes including tumor suppressor genes []. As compound possessed potent HDAC inhibitory activity a

• In conclusion while class I HDAC inhibitors isoform specific

  2021-09-11

  

  In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides

• Under increased drug pressure more protease

  2021-09-11

  

  Under increased drug pressure, more protease variants with more than one substitution will likely become clinically relevant. The accumulation of additional substitutions can allow RAS variants to emerge that alone are not viable, but in combination can rescue the viral fitness. We previously demons

• br Experimental procedures br Results br

  2021-09-11

  

  Experimental procedures Results Discussion Although the presence and localization of the GlyR subunits have been determined in the adult retina, the proportion of each GlyR subunit has not been assessed in the adult or in the developing retina. In the present study, we carried out the absol

• Racemic protein crystallography has been proven

  2021-09-11

  

  Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,

• Overall our results indicated the

  2021-09-11

  

  Overall, our results indicated the involvement of GABAAR in controlling GnRH/LH release through mechanism which included GABA action on molecular processes leading to GnRH biosynthesis. This is consistent with previous in vivo [14,54] and in vitro [55] studies in ewes suggesting that GABA inhibits G

• In contrast to short term effects

  2021-09-11

  

  In contrast to short-term effects, long-term exposure of beta cells to FFAs impairs insulin secretion and triggers apoptosis [13]. The deleterious effects of FFAs have been linked to altered glucose/fatty ccr5 antagonist oxidation cycle [13], decreased NADPH content [14], endoplasmic reticulum (ER)

• bupropion hydrochloride Our study has some limitations that

  2021-09-11

  

  Our study has some limitations that should be considered when the results are interpreted. First, we did not measure the protein levels of Bax and Bcl2, due to time and budget limitations. Although simultaneous measurements of both mRNA and protein levels are complementary for a better understanding

• br Materials and methods br Results br Discussion The previo

  2021-09-11

  

  Materials and methods Results Discussion The previous studies have reported that positive GLUT1 expression had a predictive value for prognosis of lung cancer patients (Younes et al. 1997a; Meijer et al., 2012; Sasaki et al., 2012). Our conclusion was accordant with these studies. Recently,

• br Preclinical development of GIP agonists

  2021-09-11

  

  Preclinical development of GIP agonists Since the action of DPP IV is not limited to GIP, the most specific pharmacological approach for GIP would be modification at the N-terminus to disrupt DPP IV-mediated degradation. Indeed, it has been shown that GIP analogues with N-terminal modifications a

• Despite their undisputed importance however FPR receptors ar

  2021-09-10

  

  Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis

• notch signaling To meet the requirement of ferroptosis based

  2021-09-10

  

  To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous

• br Conclusions and perspectives br Acknowledgements This wor

  2021-09-10

  

  Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025

• br Materials and methods br Results

  2021-09-10

  

  Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either Leupeptin H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the receptor´s res

• The only approved H R antagonist inverse agonist is

  2021-09-10

  

  The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or

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