• On the basis of the structure of the Rab ACAP

  2022-02-12

  

  On the basis of the structure of the Rab35/ACAP2 complex, the authors identified Thr76 in switch II of Rab35 as one key specificity determinant (Lin et al., 2019). The crystal structure shows that the hydroxyl group of Thr76 forms a 5-Methyl-CTP with Asp756 in ACAP2, while the methyl group is a par

• Initially the synthesized compounds from were evaluated

  2022-02-12

  

  Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic 3'-O-(2-nitrobenzyl)-2'-dATP mg

• br Amino acid usage in cancer br Perspective

  2022-02-12

  

  Amino nisin usage in cancer Perspective High glucose consumption is a common feature of several types of tumor cells. Therefore, so far, in vivo positron emission tomography (PET) imaging with the glucose analog 18F-fluorodeoxyglucose (18F-FDG) has been used to detect various tumors. However,

• Interestingly zaprinast administration not only prevents

  2022-02-12

  

  Interestingly, zaprinast administration not only prevents the development of hypersensitivity but also enhances opioid effectiveness. Opioids have long been considered among the most effective drugs used to treat pain (Watkins et al., 2005; Mika et al., 2013; Szczudlik et al., 2014a, Szczudlik et al

• br TGR Agonists br FXR

  2022-02-12

  

  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

• The life cycle of T cruzi requires both

  2022-02-12

  

  The life cycle of T. cruzi requires both vertebrate and invertebrate hosts. In the insect (invertebrate) vector, the protozoan undergoes extracellular replication, whereas in the mammalian (vertebrate) host it replicates by obligate intracellular multiplication (Rodrigues et al., 2014). Hence, the p

• The DNA cleavage activity assay in the

  2022-02-12

  

  The DNA cleavage activity assay in the present study also demonstrated the DNA glycosylase activities of SMUG1, NEIL1, TDG, and NTHL1 for 5OHU paired with A. While our findings on the activities of SMUG1 and NEIL1 were consistent with the results reported from previous studies [25], [50], the activi

• br Membrane transporters as a novel therapeutic target

  2022-02-12

  

  Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS

• Solid tumors usually present insufficient supply

  2022-02-12

  

  Solid tumors usually present insufficient supply of oxygen, activating the hypoxia inducible factor-1 (HIF-1) pathway, which prompts an adaptive response on genes that regulate glycolytic metabolism, promoting glucose uptake through the transcription of GLUTs [54]. Increasing evidence indicates that

• Despite the potential promise of both of these

  2022-02-12

  

  Despite the potential promise of both of these peptides, such compounds are still susceptible to efficient renal filtration (Emmanouel et al., 1978, Holst, 1991, Deacon et al., 1996). However, numerous studies have demonstrated that fatty NVP-AUY922 dervatisation of related regulatory peptides resu

• Interruption of glucagon signaling pathway targeting glucago

  2022-02-12

  

  Interruption of glucagon signaling pathway targeting glucagon receptor (GCGR) by gene knockout, antisense oligonucleotides or specific antagonists induces α-cell hyperplasia and alleviates hyperglycemia and other metabolic symptoms in diabetic animals and patients [[7], [8], [9]]. Here we used a ful

• In the present study five Glu

  2022-02-12

  

  In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pr

• Recently unimolecular multi functional peptides that combine

  2022-02-12

  

  Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with AG-14361 and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weight l

• In a mouse model of hyperhomocysteinemia

  2022-02-12

  

  In a mouse model of hyperhomocysteinemia (a risk factor for the development of vascular dysfunction) it has been shown that myoendothelial communication is enhanced due to increased expression of Cx37 and IK1 Biotin-tyramide synthesis [], allowing the propagation of endothelial signals to VSMC and

• Thus this work aims to evaluate the effect of tannic

  2022-02-12

  

  Thus, this work aims to evaluate the effect of tannic everolimus on β-galactosidase activity, by observing the variations in the molecular interaction kinetic parameters ( and ). Besides, these data were correlated with the modifications that the tannin caused to the enzyme’s secondary structure (C

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