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Imatinib STI is a first line tyrosine
2019-08-26

Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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11-dUTP In the context of E ligase drug discovery it is
2019-08-26

In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 11-
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br Materials and methods br Results br
2019-08-26

Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and w
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Sp family protein has been regarded as the
2019-08-26

Sp family protein has been regarded as the housekeeping gene and is ubiquitously expressed. Although Sp family expression is regulated with some stimuli [17], [20], the total Sp family protein levels are not changed in most cases, as observed in our present study (Fig. 4). Constitutive binding of th
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br Materials and methods br Author contributions br Acknowle
2019-08-26

Materials and methods Author contributions Acknowledgements Supported by grants from the Zhejiang Provincial Natural Science Foundation (LY16H030016, LY17H030012), and the Zhejiang Science and Technology Public Welfare Project (2015C33279), Anesthesiology Center in North of Zhejiang Provinc
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Some of the psychoactive actions of
2019-08-26

Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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Both anxiogenic and antinociceptive effects produced by CRF
2019-08-24

Both anxiogenic and antinociceptive effects produced by CRF seem to be selective for the CRF1 receptor, since intra-dPAG microinjection of ASV 30, a CRF2 receptor antagonist, altered neither the anxiety nor the antinociception response. Intra-dPAG ASV 30 was also unable to prevent the anxiogenic (ob
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This review focuses on the atomic basis of CRM
2019-08-24

This review focuses on the atomic basis of CRM1-mediated nuclear export. There are now 27 crystal structures of CRM1 in the Protein Data Bank (PDB) (www.rcsb.org) [64]. Collectively, this large body of work explains various aspects of CRM1 function. Here we summarize the structure–function studies t
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br Materials and methods br Acknowledgements We thank Drs Na
2019-08-24

Materials and methods Acknowledgements We thank Drs. Nathan Sherer (University of Wisconsin-Madison) and Bryan Cullen (Duke University) for generous reagent gifts. The following reagent was obtained through the NIH AIDS Reagent Program, Division of AIDS, NIAID, NIH: HIV-2ROD phage from Dr. Ron
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Stress is usually comprehended as an event
2019-08-24

Stress is usually comprehended as an event affecting mainly the HPA axis and initiating the alarm reaction represented by activation of the adrenal medulla. This means that the levels of related hormones and neurotransmitters are significantly elevated during and after the stress. CRF, following its
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peptide receptors To develop antagonists selective for
2019-08-24

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic peptide receptors () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable al
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Several of the keloid like lesions seen in
2019-08-24

Several of the keloid-like lesions seen in these individuals were pigmented. It is of potential relevance that genetic variants in DDR1 [MIM: 600408] have been associated with vitiligo, and DDR1 activation is involved when cyclin dependent kinase are attached to collagen-IV fibers. Because DDR1 and
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Central to the mechanism of cold I R associated
2019-08-24

Central to the mechanism of cold I/R-associated liver injury is the activation of the pro-inflammatory cascade resulting in the release of pro-inflammatory cytokines. In agreement with the present study, serum and hepatic mRNA levels of TNF-α, IL-6, and ICAM-1 were all significantly up-regulated ear
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Why are Tfh cell dynamics so fundamentally different in
2019-08-24

Why are Tfh cell dynamics so fundamentally different in naive and immune animals? Initially, GC BAMB-4 must pass stringent affinity and specificity checkpoints to ensure only high-affinity non-self-reactive cells are selected. Therefore, restricting primary Tfh cells with the greatest helper capacit
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Muscle Ring Fingers MuRFs comprising TRIM MuRF TRIM MuRF
2019-08-24

Muscle Ring Fingers (MuRFs) comprising TRIM63 (MuRF1), TRIM55 (MuRF2) and TRIM54 (MuRF3) are the most studied TRIMs in the heart. However, with increasing knowledge of E3 ligases and recent advancements in the field, many other TRIMs such as TRIM8, TRIM21, TRIM24, TRIM32, TRIM45, TRIM69 and TRIM72 w
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