• br Authors contributions br Acknowledgements br Introduction

  2021-01-21

  

  Authors’ contributions Acknowledgements Introduction Retinoic topoisomerase ii is a key signalling molecule in healthy development and in differentiation of stem cells, albeit uncontrolled levels of retinoic acid can lead to mutagenesis [1]. In eukaryotes retinoic acid is made by oxidation

• In vitro work by us and others revealed

  2021-01-21

  

  In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan

• Midazolam oral clearance is used for characterization of bot

  2021-01-21

  

  Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo

• Then the mechanisms responsible for BPA induced

  2021-01-21

  

  Then the mechanisms responsible for BPA induced up regulation of ERRγ were further investigated. Recent studies indicated that Akt and MPAK can modulate the protein levels and transcriptional activities of ERRγ (Heckler et al., 2014, Sun et al., 2014). Previous studies also indicated that BPA can ac

• FG2216 br Assessing DUB activity The Ub field

  2021-01-21

  

  Assessing DUB activity The Ub field has benefited greatly from the past efforts of biochemists and chemical biologists who have reconstituted Ub signals in vitro and generated tools for capturing or measuring DUB activities, many of which can be readily produced or are commercially available (Ekk

• DDR expression is upregulated in the glomeruli and tubules

  2021-01-20

  

  DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident dormin is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favor to t

• A series of monocarboxylated chalcones e g

  2021-01-20

  

  A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 Nogo-66 (1-40) was not se

• br Conflict of interest br

  2021-01-20

  

  Conflict of interest Acknowledgements This study was supported by the National Natural Science Foundation of China (No.31571839), the Chinese Ministry Program for New Century Excellent Talents in University (NCET-12-0865), and Special Fund for Agro-scientific Research in the Public Interest (N

• In this paper we focused on Ewing sarcoma

  2021-01-20

  

  In this paper, we focused on Ewing sarcoma (ES), a rapidly growing, highly malignant bone tumor developing metastases in the vast majority of patients unless multiagent chemotherapy is applied [16]. ES is the second most frequent bone tumor in childhood and adolescence, and is characterized by the p

• cyp3a inhibitors In summary we have identified a series of a

  2021-01-20

  

  In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als

• In normal chow fed mice EP deficiency

  2021-01-20

  

  In normal chow fed mice, EP4 deficiency also decreased the expression of CYP8B1, the downstream target of CYP7A1. Similarly, knockdown of EP4 with small interfering RNA reduced the expression of CYP8B1 in HepG2 cells. Therefore, it was anticipated that there would be an increased expression of CYP8B

• br Mechanisms of acquired resistance

  2021-01-20

  

  Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may

• br Introduction Detection of driver

  2021-01-20

  

  Introduction Detection of driver mutations in patients with advanced non-small cell lung cancer (NSCLC) is critical because they receive great benefit from kinase inhibitors [[1], [2], [3], [4]]. However, it is often difficult to obtain tumor tissue in advanced NSCLC patients. Cell-free DNA (cfDN

• NIBR189 receptor The idea that ASB can

  2021-01-19

  

  The idea that ASB11 can drive compartment expansion in the CNS is further supported by in vitro work in human neuronal precursors. Nerve growth factor (NGF)-induced differentiation of PC12 pheochromocytoma NIBR189 receptor [11] and RA-induced human pluripotent teratocarcinoma carcinoma (NT2) cells

• Several of the plant extracts that showed interaction with

  2021-01-19

  

  Several of the plant extracts that showed interaction with ERα and ERβ have differing reports concerning estrogenicity and receptor binding. Extracts of dong quai stimulated MCF-7 proliferation but failed to increase uterine weight or transactivate either ERα or ERβ in a cell assay (Amato et al., 20

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