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In young animals the HT A receptor antagonist ketanserin at
2023-10-23

In young animals, the 5-HT2A dantrolene sodium sale antagonist ketanserin, at relatively low concentrations, shifted 5-HT concentration-response curves rightward, suggesting a role for 5-HT2A receptors in mediating 5-HT-induced contractions of the ureter. The slopes of the ketanserin Schild plots fo
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br Materials and methods br
2023-10-23

Materials and methods Results Discussion Recent studies have highlighted DBIBB and autophagy as novel targets for the treatment of liver fibrosis [7,14]. In this study, we demonstrated that catalpol protected the rat liver from CCl4-caused injury and fibrogenesis in vivo and in vitro for t
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br The future of cancer therapeutics with Aurora
2023-10-23

The future of cancer therapeutics with Aurora kinase inhibitors Involvement of Aurora kinases in deregulating multiple tumor suppressor and oncogenic pathways together with the preclinical findings on the efficacy of Aurora kinase inhibitors in attenuating growth of tumor tak1 kinase suggests tha
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br Aurora kinases br Wnt signaling pathway The signal
2023-10-23

Aurora kinases Wnt signaling pathway The signal transduction pathway of Wnt/β-catenin signaling pathway plays an important role in embryogenesis to control cell differentiation and tumorigenesis [39]. A recent report indicates that 90% of colorectal cancer occur due to the activation of the Wn
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lxr agonist br Funding This study was supported by Grant
2023-10-23

Funding This study was supported by Grant UM1-CA186690 (NCI-CTEP) and R01CA204173 (CJB). This project used the UPCI Cancer Pharmacokinetics and Pharmacodynamics Facility (CPPF) and was supported in part by award P30-CA47904 and R50CA211241. Introduction Despite the efficacy of platinum based
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Several structural classes of ASK inhibitors mostly
2023-10-23

Several structural nkh of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revealed som
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Previous investigations have established that aromatase acti
2023-10-23

Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w
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Co is an essential element for life in minute
2023-10-23

Co is an essential element for life in minute amounts [5]. The human adult contains about 1.1mg Co with the daily requirement of 0.1μg/day. Co is a component of vitamin B12. Co induces erythropoietin and blocks iodine uptake by the thyroid, controls the transfer of enzymes like homocysteine methyltr
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br Funding This work was supported by the National
2023-10-23

Funding This work was supported by the National Natural Science Foundation of China (grant No. 81573664). Thanks to Jing-xian Yang from the Pharmacology Laboratory of Liaoning University of Traditional Chinese Medicine for support with technology and experimental equipment. Disclosure Confl
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br Conclusion We present here the first comprehensive analys
2023-10-23

Conclusion We present here the first comprehensive analysis of B-Raf-induced transcriptional activation in insulinoma cells. The B-Raf-induced signaling cascade targets the c-Fos and the c-Jun genes. Both gene products are constituents of the AP-1 transcription factor. The phosphatases MKP-1 and
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br Antibiotic drug discovery approaches Traditionally novel
2023-10-23

Antibiotic drug discovery approaches Traditionally, novel Rp-8-Br-PET-cGMPS were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries derived
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br Concluding remarks Enhanced membrane binding
2023-10-23

Concluding remarks Enhanced membrane binding upon calcium stimulation in KNK437 suggests a pre-requisite step that involves a conformational change in LOX. This might facilitate it to tether to the membrane and regulate enzyme activity. The calcium binding loops and the putative active site entr
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An important observation is that this patient
2023-10-23

An important observation is that this patient has been on ALK inhibitor for more than 4 years (51 months: 27 months on crizotinib+24 months on alectinib and on-going) and there was no evidence of disease progression in the central nervous system. The other potential driver mutation in this patient’s
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Curcumol In previous research we determined that blocking mA
2023-10-23

In previous research, we determined that blocking mAC during heparin-induced capacitation result in sperm having a lesser oxygen consumption, suggesting that cAMP produced by this enzyme would be linked to mitochondrial activity and, therefore, with the regulation of sperm metabolism (Fernández and
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br Aberrantly enhanced adenosine signaling in retina of oxyg
2023-10-23

Aberrantly enhanced adenosine signaling in retina of oxygen-induced retinopathy Current therapeutic development of ROP focuses on directly targeting VEGF and HIF-1α signaling pathway (Cavallaro et al., 2014, Penn et al., 2008, Mintz-Hittner et al., 2011, Hartnett and Penn, 2012). However, cellula
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