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Compounds and with potent ALR inhibitory activity
2022-11-23
Compounds , and with potent ALR2 inhibitory activity were also tested for their inhibition ability against ALR1, as shown in . They all showed low activity with inhibition percentages no more than 45% at the concentration of 10μM, demonstrating good selectivity for ALR2. To evaluate the antioxidant
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Implicit in this concept is the idea that the
2022-11-22
Implicit in this concept is the idea that the β-adrenoceptors in the detrusor would be activated by adrenergic nerves of the sympathetic system: sympathetic activity promoting relaxation and enhancing bladder capacity. However, it has been demonstrated that there is only a sparse adrenergic innervat
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Regarding androgens it is known that they
2022-11-18
Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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Hypotaurine The role of DHT in early teleost embryogenesis i
2022-11-18
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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Demonstration of in vivo efficacy of
2022-11-18
Demonstration of in vivo efficacy of potential chemopreventive agents in animal models is necessary for their clinical development. Our present study provides experimental evidence that CuB 0.1μmol by oral administration (for 2weeks before the cancer cell injection, 5days per week) significantly inh
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Dihydrotestosterone We showed that activation of the
2022-11-18
We showed that activation of the ATM/ATR pathway leads to over-replication through suppression of CDK1 activity, consistent with previous findings that suppression of CDK1 activity is involved in the polyploidization of megakaryocyte and trophoblast cells [36], [37], [38], [39]. Suppression of CDK1
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Cyprodime hydrochloride In addition to calpain I activity
2022-11-18
In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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As a neuropeptide Apelin also
2022-11-18
As a neuropeptide, Apelin also has a critical role in cardiovascular diseases. Systemic administration of Apelin exert vasodilatory and antihypertensive effects [33]. Meanwhile, the apelin-APJ signal transduction pathway is related to age-associated cardiovascular diseases [34]. It has been known th
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We report here the first study on
2022-11-18
We report here the first study on the inhibitory effects of the organic nitrates – on human erythrocyte GR. The previous reports by Becker et al., investigated other nitro derivatives (including arylizoalloxazines) by using Beutler’s method, monitoring GR inhibition. Data of show inhibition of hGR b
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br AR signals and chemosensitivity in urothelial cancer A
2022-11-18
AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance
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br The prevalence of diabetes is increasing globally and the
2022-11-18
The prevalence of diabetes is increasing globally, and the situation is particularly alarming in Asia. The prevalence of diabetes in China has increased dramatically, from around 1% in 1980 to the most recent estimate of 9.7% according to a nationwide survey . Cumulative evidence shows that type 2
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In this report we introduce a new method for identifying
2022-11-18
In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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The relatively high concentration of
2022-11-18
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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The adult muscle type acetylcholine
2022-11-18
The adult muscle-type Pravastatin sodium receptor (AChR), the exemplar pLGIC, is a heteropentamer comprising two α subunits, and one each of the β, δ, and ɛ subunits (Sine, 2012). These five subunits come together in a counterclockwise α-ɛ-α-δ-β arrangement (Figure 1A). Binding of acetylcholine to
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Further evidence for ACh GABA cotransmission had also been o
2022-11-18
Further evidence for ACh/GABA cotransmission had also been observed in the cortex. Extensive axonal arborization from cholinergic BF neurons exists throughout the cortical layers, allowing direct observation of cholinergic synaptic terminals. One study in the visual cortex of cat examined immunolabe
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