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Apoptosis type I programmed cell death is considered to
2021-04-01
Apoptosis, type I programmed cell death, is considered to be involved in the pathogenesis of various liver diseases, such as autoimmune hepatitis [[5], [6], [7], [8], [9], [10]] and hepatocellular carcinoma [11,12]. Apoptosis is activated by a variety of extrinsic or intrinsic pathways factors. Prev
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br Methods br Results br Discussion There are
2021-04-01
Methods Results Discussion There are two particularly important facets of the present ERK findings relevant to drug conditioning. One is the strong ERK signal observed in the medial prefrontal cortex and the nucleus accumbens during the immediate post-trial interval following the final cond
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Further modifications on the position of compound led to com
2021-04-01
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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In conclusion our findings suggested that EP receptor activa
2021-04-01
In conclusion, our findings suggested that EP4 receptor activation triggers apoptosis in B-cell lymphoblasts. Our results also showed that EP4 receptor engagement inactivates NF-κB, which, in turn, sensitizes Ramos Erteberel to apoptosis induced by chemotherapeutic agents. EP4 receptor agonists are
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There are five phosphorylated serines in casein
2021-04-01
There are five phosphorylated serines in β-casein. However, only phosphorylated Ser35 was identified in the samples hydrolysed with GE at 37 and 50 °C, i.e., f32-42 and f32-44 of β-casein. The identification indicates that phosphorylated peptides were less detectable from the non-phosphorylated pept
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Mouse Cyp a is a homologous isoform of
2021-04-01
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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Our study provides proof of
2021-04-01
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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DNMT is the dominating enzyme
2021-04-01
DNMT1is the dominating enzyme responsible for maintenance of the DNA methylation pattern and the primary enzyme responsible for copying methylation patterns following DNA replication (Moore et al., 2013). DNMT1 maintains the mitotic inheritance of the original methylation pattern in a cell lineage d
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We recently reported that the information about the electron
2021-04-01
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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Although many GPCR heteromers have been identified using het
2021-03-29
Although many GPCR heteromers have been identified using heterologous cell lines, only very few fit all three criteria. This is mainly due to the difficulties to study these structures in native tissues because of the lack of sensitive and selective tools, not only capable of detecting in vivo evide
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br Fragment based drug discovery FBDD
2021-03-29
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 2-Phenyl-2-(1-piperidinyl)propane space with libraries which are smaller in size, producing drug leads with high ligand-b
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The mammalian two hybrid results described above
2021-03-29
The mammalian two-hybrid results described above were all obtained in 293T cells, and thus the higher RLU observed specific to the hCrm1 fusion could be consistent with human h2 receptor antagonist having an unknown activator that interacts with hCrm1 HEAT repeat 9A and somehow facilitates Crm1-Rev
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Flexible alignment of isopropylphenylaminobenzimidazole with
2021-03-29
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead selective estrogen receptor modulators 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1
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Furthermore positioning the naphthalene nucleus in d
2021-03-29
Furthermore, positioning the naphthalene nucleus in 3d within the main active site and forming one hydrogen bond with Tyr385 in addition to many hydrophobic interactions with Val349, Leu352, Gly526, Ala527 and Leu531 residues, correlates well with the position and hydrophobic interactions of the tri
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A further quandary concerning rediscoveries arises in habita
2021-03-29
A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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