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nampt inhibitor Several CHK inhibitors have been
2020-05-28
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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br The modulation of ER from SERMs to TSECs
2020-05-28
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective SMI-4a receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, despite l
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Introduction Penetrator with Enhanced Lateral Effect
2020-05-28
Introduction Penetrator with Enhanced Lateral Effect (PELE) is a kind of ammunition which consists of a low-density material as the filling and a high-density material as the jacket [1,2]. When PELE impact target, the jacket is radially accelerated, expanded and fractured because of distinctive lat
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br Experimental procedures br Results Fluorescence attributa
2020-05-28
Experimental procedures Results Fluorescence attributable to GnRH-eGFP neurons was observed through the diagonal band of Broca, to the POA of the hypothalamus in GnRH-eGFP transgenic rats for all groups as described previously (Kato et al., 2003, Tada et al., 2013). Discussion The mEPSCs w
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Upon further evaluation of the phage obtained from phage dis
2020-05-28
Upon further evaluation of the phage obtained from phage display, we compared the capture of each of the 4th round phage to a phage possessing the wild-type arylsulfatase A sequence (LCTPSR) using ELISA. Each phage was equivalently exposed to FGE and to the beads for capture; however, we found that
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ACE also known as Kininase II is an important enzyme
2020-05-28
ACE also known as Kininase II is an important enzyme of the Renin angiotensin pyruvate dehydrogenase kinase system (RAAS) (Novo et al., 1987), it is believed to be a potent blood pressure regulator and also plays a crucial role in activation of the bradykinin receptor via inactivation of bradykinin
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As proof of principle the effect of selective blockade
2020-05-28
As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration
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br Conclusions br Acknowledgements This work
2020-05-28
Conclusions Acknowledgements This work was supported by the Science and Technology Planning Projects of Guangdong Province (2014A020210027); the Major Scientific Research Projects of Universities in Guangdong Province (2016KZDXM042); the Natural Science Foundation of Guangdong Province (2015A0
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Breast cancer is the most common neoplasm in
2020-05-28
Breast cancer is the most common neoplasm in women, with approximately 231,840 new cases of invasive breast cancer, 60,290 additional cases of in situ breast cancer and 40,290 deaths occurring in 2015 in the United States. Meanwhile, about 2350 men will be diagnosed with breast cancer, and 440 men w
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br Results br Discussion Many assays in
2020-05-28
Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of
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Here we explored the relative contribution
2020-05-28
Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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br Conclusions There is significant interest in understandin
2020-05-28
Conclusions There is significant interest in understanding the contribution of biological mechanisms to the non-linear/bilinear dose–response curves for DNA-reactive agents. Model monofunctional alkylating agents have datasets amenable to PoD determination for genotoxic effects in both in vitro
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teniposide CaneCPI showed strong inhibitory activity against
2020-05-27
CaneCPI-4 showed strong inhibitory activity against recombinant falcipain-2 and falcipain-3, with IC values of 11.9±0.4nM and 42.3±0.8nM, respectively (Table 1, Supplementary material). Falcipains are involved in hemoglobin cleavage, with generation of two fractions: the heme and the globin. The hem
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We propose two hypotheses to interpret our
2020-05-27
We propose two hypotheses to interpret our findings. The first, ELR (+) CXC chemokines stimulate both CXCR-1 and CXCR-2 chemokine receptor while activating neutrophils; however CXCR-1 chemokine receptor seems to play more active role in the process of neutrophil migration as shown in previous studie
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Nucleophosmin NPM which also plays a role on the
2020-05-27
Nucleophosmin (NPM1), which also plays a role on the nuclear export of ribosomal proteins and subunits (Maggi et al., 2008), is also a relevant MYC target, presumably through an interaction with CRM1. Conversely, it has been recently reported that specific SINE compounds reduce the levels of MYC in
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