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Inhibitors of the G rdos
2022-05-21
Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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br FXR FGF in the
2022-05-21
FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, Pam2CSK4 and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synthesiz
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Albumin is the major carrier of free fatty acids
2022-05-21
Albumin is the major carrier of free fatty acids (FFAs) in plasma [59], and harbours seven binding sites that are common to FFAs with a range of chain-lengths (C10-C18) across its three domains (Fig. 1a) [60,61]. In vitro, saturated, mono- and poly-unsaturated FFAs, with chain lengths ranging from C
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Recently they reported an enyne chemotype agonist Fig with l
2022-05-21
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral PR-619 (tmax=15min) and a decent pharmacokinetic profile, a sati
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The product chain length determination mechanism of prenyltr
2022-05-20
The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino ON123300 residues in each subfamily of -prenyltransferases have enabled the understanding of the basic catalytic
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It is well known that
2022-05-20
It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the
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Case report A yr old Caucasian female presented
2022-05-20
Case report A 66-yr-old Caucasian female presented to Raigmore Hospital in Inverness, Scotland for orthopaedic surgery, specifically a trapeziectomy with ligament reconstruction and tendon interposition and extensor pollicis longus realignment after a diagnosis of bilateral pantrapezial osteoarthri
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br Conclusions and perspectives br Acknowledgements This
2022-05-20
Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025
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The most abundant form of Hat p in
2022-05-20
The most abundant form of Hat1p in the nucleus is apt to be in the form of the NuB4 complex [96]. In the context of Cinacalcet HCl assembly, the function of the NuB4 complex may be similar to that ascribed for the cytoplasmic HAT1 complex. That is, the NuB4 complex may be involved in directing newly
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In mammalian cells Motins have been identified as a key
2022-05-20
In mammalian cells, Motins have been identified as a key link between F-actin and Hippo pathway regulation, as knockdown of all three Motins increased Yap activity even in the presence of cytoskeletal disruption [105]. Motins can physically associate with F-actin but this association is blocked by p
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G P also plays a critical
2022-05-20
G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon
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In conclusion studies of the regulation of the HO BVR
2022-05-20
In conclusion, studies of the regulation of the HO-1/BVR/CO pathway by selective pharmacological approaches may lead to the discovery of novel compounds for the treatment of diverse diseases. Recent results validate the use of advances in targeting HO-1 in various vascular diseases. However, there a
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We are pursuing a hit to
2022-05-20
We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result
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Beckman Coulter s DxN VERIS Molecular Diagnostics System
2022-05-20
Beckman Coulter’s DxN VERIS Molecular Diagnostics System (DxN VERIS System) is a fully automated system for the quantitative analysis of molecular targets, integrating sample introduction, nucleic Desformylflustrabromine hydrochloride synthesis extraction, reaction set-up, real-time PCR amplificati
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We report herein an electrochemical analysis of the
2022-05-20
We report herein an electrochemical analysis of the interaction between L1 and sGC, where conventional solution phase voltammetry is combined with a novel technique, the voltammetry of microparticles (VMP), in order to obtain mechanistic information on the deactivation of sGC by L1. The VMP is a sol
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