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It is now widely known that blockade of CysLT receptors
2019-09-30
It is now widely known that blockade of CysLT1 receptors strongly inhibits antigen-induced bronchial contractions in specimens isolated from non-asthma subjects. However, this blockade is not complete as shown in the present study and in other literature.4, 15, 16 The results of the current study su
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br Benefits and risks of traditional combined oestrogen
2019-09-29
Benefits and risks of traditional combined oestrogen–progestogen HRT regimens Combined oestrogen–progestogen regimens were developed to reproduce the short- and long-term benefits of oestrogen replacement therapy (ERT) and to simultaneously provide appropriate protection against oestrogen-related
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br Materials and methods br Results br Discussion PKA
2019-09-29
Materials and methods Results Discussion PKA and Epac are two principal effector proteins involved in cAMP signaling; they are expressed in a wide range of tissues and control diverse biological functions [10]. The existence of two cAMP effectors provides more precise regulation of cAMP sig
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When six chemical inhibitors were incubated with TRB
2019-09-29
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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MMP-2/MMP-9 Inhibitor I mass br Materials and methods br Res
2019-09-29
Materials and methods Results Discussion DNA-PKcs and the Ku heterodimer (Ku70 and Ku80) constitute the DNA-PK complex, which is a serine/threonine kinase. DNA-PK phosphorylates H2AX and other substrates, such as main NHEJ factors (Artemis, XRCC4, and DNA ligase IV) [4]. Therefore, DNA-PK d
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br Inhibition of DHODH The final
2019-09-29
Inhibition of DHODH The final products 7a–n were assessed for their DHODH inhibitory activity on rat liver mitochondrial/microsomal membranes. A procedure adapted from the literature was employed (see Experimental), in which oxidation of DHO to ORO is monitored by following the concomitant reduct
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Nitric oxide NO is synthesized by conversion of the
2019-09-29
Nitric oxide (NO) is synthesized by conversion of the l-arginine to NO and l-citrulline through reaction which is catalyzed by nitric oxide synthetase (NOS) (Knowles and Moncada, 1994). NO as an important molecule not only play a role as second messenger but also binds to cytochrome c oxidase and de
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br Materials and methods br Results br
2019-09-29
Materials and methods Results Discussion Conclusions First, we replicated the association of DDR1 with SZ in an independent Spanish sample and demonstrated that a SNP-SNP interaction within DDR1 played a role in the association with the disease. Second, we observed that SZ subjects with
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In the present study Asian swamp eel CXCR a
2019-09-29
In the present study, Asian swamp eel CXCR1a (MaCXCR1a), MaCXCR1b, MaCXCR2, MaCXCR3a, MaCXCR3b, and MaCXCR4 were identified from the Asian swamp eel genome. To explore the features and functions of these CXCRs, we focused on the identification and molecular characterization of MaCXCRs, and Liquidamb
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Compounds were prepared via the
2019-09-29
Compounds were prepared via the routes shown in , varying the sequence of reactions to install the thiazole or the phenyl ring at the end of the synthesis (pyridyl examples were prepared using similar chemistry). The aminothiazole building blocks were prepared as shown in . 5-Aminothiazole was prep
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In the intestine absorbed cholesterol can either be esterifi
2019-09-29
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
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As expected the nortestosterone derived progestins tested we
2019-09-29
As expected, the 19-nortestosterone-derived progestins tested were moderate agonists of hAR (C), with EC50s ranging from 2 to 10nM, however all were less potent than the endogenous ligand DHT by at least a factor of 6, with relative potencies ranging from 0.0301 to 0.164. This is in agreement with p
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Brg is a core unit
2019-09-27
Brg1 is a core unit of BAF complex and is required for the self-renewal and pluripotency of ESCs (Ho and Crabtree, 2010). We confirmed the interaction of DPF2 and BRG1 by immunoprecipitation and showed that these proteins extensively co-localize in the genome. Although both Brg1 and Dpf2 positively
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In contrast irinotecan has shown much less myelosuppression
2019-09-27
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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br Halogenases Enzymatic C H activation leading to
2019-09-27
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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