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Moreover intestinal chronic inflammation is a promoting
2022-03-17

Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic prostaglandin rec
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The mechanisms underlying the inhibitory effects of n FAs
2022-03-17

The mechanisms underlying the inhibitory effects of n-3 FAs on neoplasia have not been completely elucidated. Until recently, the emphasis has been on the ability of n-3 FAs to compete for the pathways that lead to the synthesis of pro-inflammatory eicosanoids from arachidonic acid, an n-6 FA, there
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Recently Bristol Myers Squibb and Merck reported
2022-03-17

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic acetylcholine chloride derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GP
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We identified three genes KEAP
2022-03-17

We identified three genes—KEAP1, NAA38, and ABCC1/MRP1—as negative regulators of glutathione abundance in human cells. Like KEAP1, NAA38 appears to regulate NRF2 stability, as NAA38 deletion increased NRF2 protein levels and the expression of NRF2 target genes. NAA38 is a component of the NatC N-ter
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br Acknowledgements This work was in part supported
2022-03-17

Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese
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In this study according to the critical pharmacophore T Y
2022-03-17

In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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br PEPCK This enzyme decarboxylates
2022-03-17

PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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br Venous thromboembolism VTE is a rare but
2022-03-17

Venous thromboembolism (VTE) is a rare but potentially life-threatening complication of total joint arthroplasty (TJA) . With modern chemoprophylaxis, the incidence of VTE after primary total hip (THA) or total knee (TKA) arthroplasty is commonly estimated between 0.5% and 1%, and VTE is now consi
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The NuB complex interacts with Asf p which plays a
2022-03-17

The NuB4 complex interacts with Asf1p, which plays a central role in controlling the flux of histones to the various chromatin assembly pathways. This interaction is also evolutionarily conserved having been detected in yeast, chicken and human CGS 35066 [27], [61], [104], [105]. Asf1p appears to i
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Conflicting data concerning the involvement of H R
2022-03-17

Conflicting data concerning the involvement of H2R on glycaemia has also arisen. Its antagonism was reported to decrease [35], not affect [36], [37] and increase [38], [39] Gemcitabine levels. In comparison, the clinical experience with antipsychotic drugs generated clearer evidence for the involve
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An important example of a frame is the lattice
2022-03-17

An important example of a frame is the lattice of open subsets of any topological space X. The correspondence is clearly functorial (by taking inverse images), and consequently one has a contravariant functor with the category of topological spaces and continuous maps as domain category. The functor
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The RAS RAF MEK ERK
2022-03-17

The RAS/RAF/MEK/ERK pathway is a central controller of cell proliferation and survival and, consequently, alterations to some of its components lead to hyperactivation of the pathway, an event related to numerous types of cancer [172]. High rates of alterations to this pathway are found in leukemia,
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Evans Blue tetrasodium salt We have previously established t
2022-03-16

We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in Evans Blue tetrasodium salt and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [
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nebivolol hcl synthesis Notably Cu labeled dimeric exendin s
2022-03-16

Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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A linker length of and atoms
2022-03-16

A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and d
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