• Present malarial chemotherapies mainly rely on a very few

  2021-03-30

  

  Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa

• Members of the Nudix family typically contain

  2021-03-30

  

  Members of the Nudix family typically contain a 23-amino-acid sequence (Nudix box) of GxExREUxEExGU, where U is usually Ile, Leu, or Val and x represents any amino acid. The EUxEE core residues serve as anchors for an Mg ligand that associates with a characteristic pyrophosphate linkage that is comm

• The purposes of this study is to develop

  2021-03-30

  

  The purposes of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs using S-hexyl GSH, and to clarify the mechanism underlying response to such trapping using montelukast, a CysLT1 receptor antagonist, BayCysLT2RA, a CysLT2 recepto

• With a favorable spectrum of CRTh dependent in vitro and

  2021-03-30

  

  With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i

• Our study demonstrated that the sequential

  2021-03-30

  

  Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565

• In the intestine absorbed cholesterol can either be esterifi

  2021-03-30

  

  In the intestine, absorbed cholesterol can either be esterified by ACAT2 (Soat2) and packed into chylomicrons, transported back to the intestinal lumen by ABCG5/ABCG8, or it can be transported into HDL by ABCA1. ACAT2 is confined to enterocytes and hepatocytes and esterifies cholesterol for intracel

• Introduction Breast cancer is a highly

  2021-03-30

  

  Introduction Breast cancer is a highly prevalent malignancy. There are some recognized risk factors for breast cancer, like early menarche or late menopause, which increase the length of the exposure to hormones, as a result of a higher number of ovarian cycles [1]. Moreover, there is evidence supp

• br Molecular genetics Based on the genetic mutations associa

  2021-03-30

  

  Molecular genetics Based on the genetic mutations associated with their development, sarcomas are subdivided into two distinct classes. One class is composed of tumors bearing complex karyotypic abnormalities with no particular pattern. The second class, which includes Ewing sarcoma, encompasses

• Little information is available regarding the expression of

  2021-03-30

  

  Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r

• br Oxidoreductase like MEM for

  2021-03-30

  

  Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2

• The imaging and biochemical data presented

  2021-03-30

  

  The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In

• A study profiling chemokine expression

  2021-03-30

  

  A study profiling chemokine expression in LCLs revealed high expression levels of CCR6, CCR7, and CCR10 and low expression of CXCR4 and CXCR5 in EBV immortalized cells. Accordingly, LCLs showed a markedly increase in migration in response to the ligands of CCR6 (CCL20), CC7 (CCL21), and CCR10 (CCL28

• Experimentally measured DGAT activity was first

  2021-03-29

  

  Experimentally measured DGAT activity was first reported by Weiss et al. (1960) and several different types of DGAT enzyme have since been described in plants [12,41,42]. As recently as 2011 there appeared to be just two DGAT enzymes both in plants and in other eukaryotes, namely DGAT1 and DGAT2 [43

• NMR was employed for the determination of

  2021-03-29

  

  NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a

• Our recent discovery M P H R A S of

  2021-03-29

  

  Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w

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