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An important role for the precursor molecule
2019-09-06

An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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Several main strategies for targeting E s described in
2019-09-06

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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Three dimensional conformational changes in the cargo
2019-09-06

Three-dimensional conformational changes in the cargo protein’s NES, caused by protein phosphorylation, dephosphorylation, or mutation, can regulate CRM1 binding (Craig et al., 2002, Vogt et al., 2005). Additional protein modifications such as sumoylation, ubiquitination, acetylation, and/or the bin
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In a previous study we reported that the systemic administra
2019-09-06

In a previous study we reported that the systemic administration of the α1-adrenergic receptor antagonist prazosin attenuates the deficit in StemRegenin 1 reward function associated with precipitated nicotine withdrawal (Bruijnzeel et al., 2010). One of the aims of the present experiments was to in
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More recently evidence suggests that dysregulation of CRF si
2019-09-06

More recently, evidence suggests that dysregulation of CRF signaling may also be implicated in panic disorder. For instance, polymorphisms in the CRF1, but not CRF2, gene have been associated with susceptibility to panic disorder in German and Japanese population samples (Ishitobi et al., 2012, Keck
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Since its inception ADEPT approach has been widely
2019-09-06

Since its inception, ADEPT approach has been widely reported by many groups using a variety of enzymes and prodrugs (see reviews) [12], [14]. Both mammalian and non-mammalian enzymes have been utilised. Of the mammalian variety, human β-glucuronidase in combination with many prodrugs [17], [18] and
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Poziotinib mass The CPA EoS was presented by Kontogeorgis et
2019-09-06

The CPA EoS was presented by Kontogeorgis et al., in 1996 [23]. The proposed equation is composed of two parts (SRK EOS + association term) such that it can well predict the thermodynamic behavior of hydrogen bonding materials as a result of considering the association term. Yakoumis et al. (1997) e
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It has only recently been appreciated that antigen
2019-09-05

It has only recently been appreciated that antigen-activated SB202190 undertake two additional transient migrations during the early stages of T-dependent antibody responses. In the first of these, antigen-activated B cells migrate rapidly (within 2–3h) to the outer regions of the follicle before t
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br Materials and Methods br Acknowledgements Authors would l
2019-09-05

Materials and Methods Acknowledgements Authors would like to thank Mr. Pritam Naskar and Mr. Dibya Mukherjee for their help. Authors also acknowledge the help of Mr. Barun Mahata and Dr. Kaushik Biswas, Division of Molecular Medicine, Bose Institute, for human cDNA samples. P.A.B. and A.B.D. w
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We neither observed changes in midazolam eCLmet
2019-09-05

We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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The in vitro cytotoxicity of the prodrugs was
2019-09-05

The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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br Acknowledgments This research was financially supported
2019-09-05

Acknowledgments This research was financially supported by National Natural Science Foundation of China, Nos. 31500926 and 81503282, Natural Science Fund of Guangdong Province, No 2014A030310023, Science and Technology Plan of Guangdong Province, Nos. 2014A020212309, 2013B010404044, 2017A01010501
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In all available E E structures the
2019-09-05

In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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br Activatable optical imaging probes Optical fluorescence i
2019-09-05

Activatable optical imaging probes Optical fluorescence imaging, which directly detects photons emitted from fluorescent probes, has become as a powerful analytical method to study biological processes both in vitro and in vivo. It is characterized by high sensitivity, is free of radioactive irra
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CU CPT 22 A decrease in heme levels enables the phosphorylat
2019-09-05

A decrease in heme levels enables the phosphorylation of eIF2α by HRI and thereby inhibition of eIF2α activity. Indeed, the relatively small change in cytosolic heme levels in SZ CU CPT 22 showed downstream functional consequences manifested by almost 50% elevation in the phosphorylation of eIF2α i
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