• Due to the importance of gene regulation

  2022-01-12

  

  Due to the importance of gene regulation in cancers, HDAC inhibitors have been studied extensively in cancer biology and are in current clinical use as anti-tumor therapies [17]. The HDAC inhibitors vorinostat, romidepsin, and belinostat have been approved for certain T-cell lymphomas, and panobinos

• As a result of the

  2022-01-12

  

  As a result of the capability of modulating the dynamic changes and rearrangement of cytoskeletons, the Rho GTPases, in which RhoA, Cdc42 and Rac1 are best-characterized, have been highlighted as significant contributors for orchestrating neuronal development (Duman et al., 2015, Heasman and Ridley,

• In the inhibitory kinetic studies five different concentrati

  2022-01-12

  

  In the inhibitory kinetic studies, five different concentrations of DEL carefully selected from the near-linear region of the dose–response curve (0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM, and 8.0 μM) were used. The Vm values at fixed [CDNB]–varied [GSH] and at fixed [GSH]–varied [CDNB] were 10.4 ± 0.22 U mg−

• Modulation of the cannabinoid system has been

  2022-01-12

  

  Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a

• br TGR Agonists br FXR TGR

  2022-01-12

  

  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 Materials and methods br Acknowledgements The following r

  2022-01-12

  

  Materials and methods Acknowledgements The following reagents were obtained through the NIH AIDS Reagent Program, Division of AIDS, NIAID, NIH: SIVagm155-4 from Dr. Vanessa Hirsch and Dr. Philip Johnson; Anti-SIVmac251 Polyclonal; SIVagm tan-1 infectious molecular RN486 receptor from Drs. Marc

• In parallel we were also preparing and

  2022-01-12

  

  In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora

• Like other RNA viruses HCV also exhibits a high

  2022-01-11

  

  Like other RNA viruses HCV also exhibits a high degree of genetic diversity, creating a major challenge for the development of both HCV vaccines and pan-genotypic therapeutics (Timm and Roggendorf, 2007). The virus has a total of seven genotypes, with >50 subtypes and millions of quasispecies (Cuype

• It is notable that pharmacological or genetic inhibition

  2022-01-11

  

  It is notable that pharmacological or genetic inhibition of GCGR signaling results in the engagement of a number of compensatory mechanisms that potentially impact glucose control. These include alpha-cell hyperplasia [2], [11], [12], [13] and increased beta-cell proliferation under low insulin cond

• Extensive pharmacological and structural analysis

  2022-01-11

  

  Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in NMS-873 14, 17, 20. Functionally identical to REMD-477, REMD2.59 is

• Quercitrin synthesis Emerging evidence has shown that pharma

  2022-01-11

  

  Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici

• Here we investigated on epigenetic regulatory mechanisms of

  2022-01-11

  

  Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me

• The first phase of insulin secretion is

  2022-01-11

  

  The first phase of insulin secretion is due to calcium signaling because of glucose sensing, increased cytoplasmic ATP levels, cellular depolarization, calcium influx and activation of calcium sensing molecules that eventually causes the fusion of the insulin granules to plasma membrane (exocytosis)

• As an inflammatory mediator histamine plays a

  2022-01-11

  

  As an inflammatory mediator, histamine plays a pivotal role in nociceptive processes in both the central and peripheral nervous systems (Gemkow et al., 2009; Hough & Rice, 2011; Tiligada et al., 2009). In this respect, the participation of H3Rs in modulating pain, especially neuropathic pain, has at

• PBIT Yap and Taz may regulate epicardial cell proliferation

  2022-01-11

  

  Yap and Taz may regulate epicardial cell proliferation, EMT, and fate determination via multiple mechanisms. In this study, we provide evidence that Yap/Taz function in part by directly modulating Tbx18 and Wt1 expression. Members of the T-box family of transcription factors regulate a variety of de

15824 records 504/1055 page Previous Next First page 上5页 501502503504505 下5页 Last page