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An alternative to the agonist or antagonist potential
2023-10-17
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Conclusion Twenty compounds with dinitrobenzoate scaffold
2023-10-17
Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5
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br Cytochrome b br Cytochrome P hydroxylase lyase
2023-10-17
Cytochrome b5 Cytochrome P450 17α-hydroxylase/17,20-lyase (P450 17A1) A number of P450s involved in steroid biosynthesis are multifunctional as they carry out two or more sequential hydroxylation reactions on the same substrate(s). P450 17A1 is a dual function endoplasmic reticulum enzyme enco
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LPA binds to six specific
2023-10-17
LPA binds to six specific cell surface GPCR receptors. The receptors LPA1 (lysophosphatidic receptor 1, formerly, Edg2), LPA2 (Edg4) and LPA3 (Edg7) belong to the endothelial differentiation gene family (EDG) and share sequence homology (50–60% amino Betamethasone Dipropionate receptor homology) An
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Previous studies have demonstrated ATR
2023-10-17
Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Liproxstatin-1 to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]
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Cerebral ischemia occurs following the occlusion of a
2023-10-17
Cerebral ischemia occurs following the occlusion of a cerebral artery by a thrombus and causes cell swelling due to cytotoxic edema and BBB disruption with vasogenic edema (Loreto and Reggio, 2010, Nakaji et al., 2006, Shibata et al., 2004). Vasogenic edema is directly linked to alteration of the BB
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That increased longevity was not the exclusive
2023-10-16
That increased longevity was not the exclusive result of blood pressure reduction. This was demonstrated by analysis of life-long, whole body deletion of AT1A receptors in normotensive mice. These animals exhibited a very significant increase in lifespan when compared to wild- type mice [159], [160]
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Introduction Cardiovascular disease is the
2023-10-16
Introduction Cardiovascular disease is the principal cause of morbidity and mortality in patients with Bax inhibitor peptide V5 (1). Comprehensive management of these patients includes not only adequate glycemic control but also attention to additional recognized risk factors. Hypertension is a car
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Interestingly ZIP expression was decreased in dog testes aft
2023-10-16
Interestingly, ZIP9 expression was decreased in dog testes after they were implanted with gonadotropin releasing hormone (GnRH) which the authors proposed was due to androgen ablation (Bulldan et al., 2016a). The expression of other members of the ZIP (SLC39A) family has also been shown to be regula
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br AR expression in breast tissue Although androgenic
2023-10-16
AR expression in breast tissue Although androgenic signalling is chiefly associated with the development and maintenance of primary and secondary male characteristics, especially during puberty when the testes are by far the major source of testosterone, the AR also plays important functions in f
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Amyloid fibrils are insoluble high molecular
2023-10-16
Amyloid fibrils are insoluble, high-molecular-weight, non-crystalline aggregates and traditional experimental techniques for structure determination such as X-ray and solution NMR cannot resolve their high resolution structures [64], [68]. However, amyloid fibrils exhibit various advantageous featur
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br Material and methods br Results br Discussion Nimodipine
2023-10-16
Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic Cy3 azide to support cellular growth and survival. CCH influences the oxygen and glucose s
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br Introduction AMP activated protein kinase AMPK has
2023-10-16
Introduction AMP-activated protein kinase (AMPK) has been found to be a key character against cardiovascular diseases and cellular stress. When activated by certain stress, AMPK regulates sugars and fatty acids that are good or detrimental to the heart. For example, targeting AMPK phosphorylation
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Critically we found that pre treatment with A monomer prepar
2023-10-16
Critically we found that pre-treatment with Aβ monomer preparations prevented the Aβ oligomer-induced aggregation of PrPC. These preparations contain a mixture of Aβ species and consequently it was not possible to identify the precise form of Aβ that is responsible for this effect. It is possible th
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In conclusion we demonstrated that
2023-10-16
In conclusion, we demonstrated that, in the skeletal muscle of rats with T1DM, CRBN levels increased and AMPK, Akt, GLUT4, PGC-1α, and FNDC5 levels decreased, resulting in increased fasting glucose levels. Aerobic exercise training decreased levels of CRBN, which was possibly mediated by AMPK, Akt,
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