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br Introduction Cardiovascular disease continues to be the
2021-02-24
Introduction Cardiovascular disease continues to be the leading cause of death in developed countries. Atherosclerosis, a chronic inflammatory cardiovascular disease, is characterized by the progressive buildup of oxidized low density lipoproteins in the arterial walls (Ross, 1999). In the develo
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br Materials and methods Male
2021-02-24
Materials and methods Male Hartley guinea pigs (300–350g) were obtained from National Laboratory Animal Center, Taiwan. LTD4, LTC4, LTE4, LTB4, montelukast and BAY u9773 were purchased from Cayman Chemical, Ann Arbor, Michigan; Carbachol, atropine, l-serine, boric acid, l-cysteine and all buffer
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The small molecule d mannuronic acid
2021-02-24
The small molecule β-d-mannuronic Sulindac sulfide (M2000), patented (DE-102016113018.4), has been tested as an anti-inflammatory and a novel immunosuppressive agent in various experimental models such as animal models of immune complex glomerulonephritis, nephrotic syndrome, multiple sclerosis and
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br In patients with type
2021-02-24
In patients with type I diabetes mellitus poor management causes/INS; a drastic rise in glucose levels resulting in diabetic ketoacidosis (DKA). About 1% of DKA episodes can be complicated by cerebral edema. ET and its receptors are involved in the regulation of /INS;cerebral blood flow. We studie
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Two isoforms of intracellular ER ER and ER after binding
2021-02-24
Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of
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Prenylation may turn a flavonoid
2021-02-24
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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Progesterone s metabolite THP may also be
2021-02-24
Progesterone's metabolite, 3α,5α-THP, may also be mediating burying and freezing responses. Results show female Long–Evans rats in behavioral estrous have higher P4 levels in serum, voltage gated potassium channel and hippocampus compared to diestrous female Long–Evans rats. Additionally, ovx femal
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crth2 receptor It has been reported that Eph Ephrin are
2021-02-24
It has been reported that Eph/Ephrin are involved in the regulation of the tumor angiogenesis [10], [11], [12]. The distinct and specific involvement of crth2 receptor and veins in tumor angiogenesis is unclear. EphrinB2 is expressed in arteries and its receptor EphB4 is expressed in veins; these m
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6-Aminonicotinamide sale EPAC induces SOCS gene expression i
2021-02-24
EPAC1 induces SOCS3 gene expression in VECs, resulting in suppression of the JAK–STAT activation initiated by the sIL-6Rα/IL-6 trans-signalling complex [67]. EPAC1 regulates SOCS3 gene induction through the activation of C/EBP and c-Jun transcription factors, which interact directly with the SOCS3 p
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Given the molecular pharmacology and in vitro metabolism dat
2021-02-24
Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma
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br Acknowledgements We thank Joseph Granger
2021-02-24
Acknowledgements We thank Joseph Granger and Bryan Neumann for careful reading of this manuscript. This work is supported by NIH grants AG37609 and HL 60306 to TYC and CCYC. Introduction Eleven million tonnes of waste are produced yearly by the European pulp and paper industry (Monte et al.,
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We should also note that although AOAA is not
2021-02-24
We should also note that, although AOAA is not a specific H2S inhibitor, its inhibitory effect on l-cysteine-induced relaxations are related to H2S since addition of AOAA to another H2S inhibitor PAG did not provide a further inhibition of these relaxations in penile tissue [37]. In our study, the c
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br EBI structure and expression The gene encoding EBI was
2021-02-24
EBI2 structure and expression The gene encoding EBI2 was originally identified together with EBI1 (CCR7) as the most highly upregulated gene in Epstein–Barr virus-infected Burkitt's lymphoma cells [18]. EBI2 belongs to the rhodopsin-like subfamily of seven transmembrane GPCRs [19]. Although it is
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br Conclusions Overexpression of DDR might contribute to tum
2021-02-23
Conclusions Overexpression of DDR2 might contribute to tumor progression in lung SQCC, and the T681I mutation we found in this work is an inactivating mutation. There is a possibility that not only activating mutation but also overexpression of DDR2 might be a molecular target for treatment of lu
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During the course of our research
2021-02-23
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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