• Introduction Glucose dependent insulinotropic polypeptide GI

  2022-05-04

  

  Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G

• Until recently the mechanism of

  2022-05-04

  

  Until recently the mechanism of how GSMs shifted γ-secretase cleavage was poorly understood. Today, building on the sequential cleavage model developed by Ihara and colleagues [14], there is evidence that GSMs act as processivity enhancers, and iGSMs as inhibitors of processivity [120]. At least for

• Mouse Angiopoietin-2 / ANG2 / ANGPT2 Protein (His Tag) A gr

  2022-04-29

  

  A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous

• UNC0638 br Rationale The present study

  2022-04-29

  

  Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym

• br Materials and methods br Results br Conclusions In

  2022-04-29

  

  Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str

• As for hMOF inhibitor s study Dekker and Zheng et

  2022-04-29

  

  As for hMOF inhibitor's study, Dekker and Zheng et al. synthesized MG149 (Fig. 1) as an inhibitor of Tip60 and MOF which has an IC50 value of 74 ± 20 μM and 47 ± 14 μM [31]. However, MG149 has no experimental data on hMOF in cell or in vivo. The lack of hMOF inhibitor limits the function study of hM

• NVP DPP 728 dihydrochloride Based on the aforementioned find

  2022-04-29

  

  Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated

• br Materials and methods br

  2022-04-29

  

  Materials and methods Results Discussion An HMC is a blinding type of cataract frequently observed in Asian countries due to the appallingly high incidence of high myopia in those areas [4], [5] and typically features earlier onset and more rapid progression of nuclear cataract [1], [2]. Th

• Thus one of the aim of the work was

  2022-04-29

  

  Thus, one of the aim of the work was to link the phytotoxic effect of m-Tyr on root growth of tomato seedlings to modification of RNS level and tissue distribution accompanied by determination of 3-NT content. Due to the role of GSNOR, which is suggested to be a key element in the interplay between

• In three independent groups identified GPR

  2022-04-26

  

  In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac

• Indeed it was shown further in VSV G

  2022-04-26

  

  Indeed, it was shown further in VSV G that the H80A mutation, and the E123L and D121L double mutation, which both abolish VSV G fusion properties, were rescued by the same compensatory Q112P mutation. In a single FD, residue 112 is located on the opposite side of the three-stranded β-sheet and is fa

• Methoxyflavone and methoxyflavanone Fig both act as

  2022-04-25

  

  6-Methoxyflavone and 6-methoxyflavanone (Fig. 2) both act as flumazenil-insensitive positive allosteric modulators of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. Both fl

• Homeobox genes can promote oncogenesis through multiple mech

  2022-04-25

  

  Homeobox genes can promote oncogenesis through multiple mechanisms, including gene translocation, loss of heterozygosity, gene amplification, DNA methylation, enkephalin mg remodeling, etc. For instance, translocation-mediated fusion of HOXA9 or HOXA13 on chromosome 7p15 with the nucleoporin gene NU

• Compared to a large database of NSCLC

  2022-04-25

  

  Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi

• ursolic acid australia The H R antagonist cimetidine Tagamet

  2022-04-22

  

  The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1

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