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Recently roflumilast has been approved as the first selectiv
2021-02-23
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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br Conflict of interest br Acknowledgments This
2021-02-23
Conflict of interest Acknowledgments This work was supported in part by grants from the , Spain (INCITE08PXIB203092PR). VGM was supported by a FPU pre-doctoral scholarship from the , Spain. MLR was supported in part by a crowdfunding campaign (PRECIPITA), coordinated by the Spanish Foundation
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Kinetic isotope effects KIEs inform on
2021-02-23
Kinetic isotope effects (KIEs) inform on bond vibrational changes between the ground state (GS) and TS of a chemical reaction and remain one of the most powerful experimental techniques for interrogating TS structure. KIEs on enzyme reactions measured by the internal mitotic inhibitor of labeled su
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Herein we explored by docking studies the effectiveness of
2021-02-23
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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Cultured cells or mouse lung tissues were
2021-02-22
Cultured cells or mouse lung tissues were harvested and lysed in Radio-Immunoprecipitation Assay (RIPA) buffer (0.05 mol/l Tris–HCl pH 7.4, 0.15 mol/l NaCl, 0.25% deoxycholic acid, 1% NP-40, 1 mmol/l ethylenediamine tetraacetic AZD6738 synthesis (EDTA), 1 mmol/l phenylmethylsulfonyl fuoride, 1 μg/
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br Role of cysLT signaling on various neurological complicat
2021-02-22
Role of cysLT signaling on various neurological complications which are associated with Alzheimer’s disease Alzheimer’s disease, first described in 1906 by Alois Alzheimer, is a neurodegenerative disease and a very common cause of dementia progressively leading to death. Even though years of rese
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Considering all these facts in the present study we investig
2021-02-22
Considering all these facts, in the present study, we investigated the effects of two highly selective CRF receptor 2 antagonists (antisavaugine-30, ASV-30; and astressin-2B, AST-2B) on anxiety behavior in rats. The rationale for such an experimental approach was based on the premise that fear and s
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The mechanism by which these HIV PIs impair skeletal
2021-02-22
The mechanism by which these HIV-PIs impair skeletal muscle palmitate transport and oxidation has been partially elucidated. CD36 (also referred to as fatty (3S,5S)-Atorvastatin sodium salt receptor translocase; FAT) is a transmembrane protein involved in the transport of long-chain fatty acids (LC
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In rodents but not humans two splice
2021-02-22
In rodents but not humans, two splice variants of Chk are identified as Ntk and Ctk, which possess and lack the N-terminal unique domain, respectively. While Ctk is abundantly expressed in the brain, Ntk is selectively restricted to myeloid and lymphoid cells, especially megakaryocytes [31]. This ra
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Both receptors belong to the large family of G protein
2021-02-22
Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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13148 synthesis Besides chemopreventive effects against oxid
2021-02-22
Besides chemopreventive effects against oxidative DNA damage we evaluated the protective effects of the three Hypericum sp. and isolated compounds against alkylating DNA damage induced by MMS in HT29 cells. Human exposure to alkylating agents, from different sources, occurs in a continuous way and i
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Interferon IFN induces formation of a heterotetrameric IFN g
2021-02-22
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic Erlotinib Hydrochloride (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial gro
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pramiracetam Our results indicate that C CoA is
2021-02-20
Our results indicate that C75-CoA is formed in the hypothalamus following stereotaxic injection of C75. Inhibition of hypothalamic CPT1 by C75-CoA in vivo, as seen in our experiments, is independent of the putative inhibition by malonyl-CoA, which may be formed after the action of C75 either on FAS
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The detection of galactomannan GM a polysaccharide that is
2021-02-20
The detection of galactomannan (GM), a polysaccharide that is released during Aspergillus growth, is a useful and reliable non-invasive diagnostic test for screening and management of aspergillosis and is often more sensitive than culture (Schelenz et al., 2015, Fisher et al., 2013). The level of ga
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PF-4708671 Kumar et al studied Umbelliferone
2021-02-20
Kumar et al. studied Umbelliferone β-D-galactopyranoside (UFG) (benzopyrone), found in many plants exhibiting numerous pharmacological actions. The results of the study showed that UFG in a dose of 10, 20 or 40mgkg-1 per day, helps to prevent paw edema and arthritic score development for arthritis i
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