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It is currently believed that acute morphine administration
2021-07-29
It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ
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We examined the function of immobilised
2021-07-29
We examined the function of immobilised THPs by seeding cells transfected with DDR2-Flag on derivatised crosslinked collagen films, then detecting the phosphorylation of tyrosine 740 (Y740) on the intracellular domain of DDR2 [50]. This regulatory residue is a target for the intracellular tyrosine k
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br Fragment based drug discovery FBDD
2021-07-29
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical Amikacin sale space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency.
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On the other hand p responds to environmental stress includi
2021-07-29
On the other hand, p38 responds to environmental stress, including ultraviolet light, heat, osmotic shock, and inflammatory cytokines (Pearson et al., 2001, Kumar et al., 2003), and is activated in astrocytes after ischemia-like injury (Yung and Tolkovsky, 2003, Niu et al., 2009). Moreover, p38 acti
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In the pleural exudates which reflect
2021-07-29
In the pleural exudates, which reflect the in vivo conditions, the concentrations of CysLTs and PGE2 were quite similar. However, when cancer 5-alpha reductase inhibitors were cultured for 24 h, both analyses of cell culture medium and cell incubations with Ca2+ ionophore showed low levels of CysLT
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Introduction Cytochrome P CYP A is
2021-07-29
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The Zileuton receptor level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxic
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It is important to note that CRF may be activated
2021-07-29
It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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Based on the finding described above the present study
2021-07-29
Based on the finding described above, the present study was designed to investigate the effects of specific CRF receptors, CRF1 and CRF2, in the BLA and CeA on the duration of TI in guinea pigs (Cavia porcellus). To this end, we evaluated whether administration of the CRF1 Fmoc-Lys(Boc)-OH antagonis
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CPG a metalloenzyme derived from sp was
2021-07-29
CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic rta 3 sale prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2 is essen
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Studies of nuclear transplantation of diploid imprint free P
2021-07-28
Studies of nuclear transplantation of diploid imprint-free PGCs have shown that the reconstituted oocytes developed to day 9.5 of gestation, with severely retarded embryos and abnormal placentae (Kato et al., 1999). We also reported that MII oocyte injection of imprint-free phESCs without imprinted
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The AURA trial was a phase
2021-07-28
The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,
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chenodeoxycholic acid br Results br Discussion The
2021-07-28
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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The structure of the HOIP RBR LDD module
2021-07-28
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In th
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The majority of APC C subunits form a giant scaffold
2021-07-28
The majority of APC/C subunits form a giant scaffold, which was originally named the arc lamp, based on its shape when viewing APC/C from one side (Figure 1 and Box 1) [24]. The scaffold consists of two modules: the TPR lobe resembles the curved post and lamp, and the platform resembles the levosime
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A second advance came with the discovery
2021-07-28
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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