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GSTs have been originally named ligandins because of their
2022-01-11

GSTs have been originally named ‘ligandins’ because of their capacity to bind large ligand molecules (of molecular weight >400 Da) (Oakley et al., 1999). At least three separate Caspase-1, human recombinant proteinase have been reported for xenobiotics within the H-site; only one is for CDNB (Ralat
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br The mode of binding of ligands to GPR
2022-01-11

The mode of binding of ligands to GPR35 As noted above, although kynurenic Fmoc-Gly-OPfp receptor is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Impor
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Studies of human and mouse GPR as ascertained by
2022-01-10

Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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The expression and localization of Cx Cx
2022-01-10

The expression and localization of Cx43, Cx46 and Cx50 in the anterior pituitary vary with physiological activities and with various conditions associated with both natural and pathological changes in hormone secretion. Anterior pituitary Cx43 and Cx50 levels increase and exhibit a more widespread d
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reference 4 The current study aimed to understand the roles
2022-01-10

The current study aimed to understand the roles and the underlying mechanisms of XIST in LSCC, by focusing on the regulation by miR-124-3p, which was previously identified as a target of XIST [12]. We found that the XIST expression is positively correlated with the stages of LSCC in patients. Knockd
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JMJD C is another JmjC domain protein
2022-01-10

JMJD1C is another JmjC domain protein discovered as a putative oncogene in shRNA screens in MLL-AF9-, HOXA9-, and AML1-ETO-driven AML 40, 41, 42. Depletion of JMJD1C decreased the frequency of LICs by inducing their differentiation and impaired the growth and establishment of leukemia in serial tran
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The cytotoxicity of these compounds against Hep B cells was
2022-01-10

The cytotoxicity of these compounds against Hep3B cells was assessed using the MTT assay. As shown in , compounds in series and (except ), which retained the carboxyl at C-17, showed no appreciable cytotoxic activity (IC > 100 μM), whereas compounds in series (except ,) were modestly cytotoxic, i
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serine threonine protein kinase In addition to acting as the
2022-01-10

In addition to acting as the gatekeeper for the metabolic and antioxidant roles of glucose, HKs have also been found to regulate mPTP opening directly. First described in the cancer field, the high-affinity HK isoforms HK1 and HK2 are strongly anti-apoptotic when bound to the outer mitochondrial mem
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According to literature RASs V
2022-01-10

According to literature, RASs V36M, T54S, Q80K and R155K are considered primary resistance mutations to different PIs. RASs V36M and R155K can reduce susceptibility to recently approved PIs simeprevir, paritaprevir and grazoprevir [18], [31], [32]. T54S is associated to resistance for first-wave tel
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Introduction Hepatocellular carcinoma HCC is the fifth
2022-01-10

Introduction Hepatocellular carcinoma (HCC) is the fifth most lethal malignant tumor worldwide and is the second leading cause of cancer-related death [1]. For HCC patients, NG,NG-dimethyl-L-Arginine hydrochloride australia virus (HBV) infection is the important causative risk factor in Asia-Pacif
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br Chemistry The methylsulfanyl dihydro H thieno g isothiadi
2022-01-10

Chemistry The 8-methylsulfanyl-4,5-dihydro-1H-thieno[3,4-g]isothiadizaole scaffold was synthesized from commercially available 1,3-dioxolane-2,1′-cyclohexane-4-one 17 (Scheme 1). The isothiadizaole ring was formed with SOCl2 from N-carboxamide hydrazine imine 19, which was prepared from 17 and hy
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br Conclusion B esterases and reproductive parameters can
2022-01-10

Conclusion B-esterases and reproductive parameters can be used as effect biomarkers of the aquatic contamination with chlorpyrifos. In P. corneus exposed for 14 days to the insecticide, the carboxylesterases determined with p-NFB proved to be the most sensitive biomarker. However, exposure to env
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Studies of human and mouse GPR as ascertained by mRNA
2022-01-10

Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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br Materials and methods br Results br Discussion and conclu
2022-01-10

Materials and methods Results Discussion and conclusions Our data demonstrate that native and 2-OMe-LPC analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells. LPC 18:1 was the first proposed endogenous ligand for GPR119 [1], however natural LPC has limited
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br FXR Agonists Azepinol b indole
2022-01-10

FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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