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A novel series of DHODH inhibitors
2019-07-18
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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Till date several predictive models have
2019-07-18
Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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The effect of NAT deletion on mitochondrial function in MDA
2019-07-18
The effect of NAT1 deletion on mitochondrial function in MDA-MB-231 neuropeptide receptors has been reported elsewhere (Carlisle et al., 2018). However, unlike the data presented here, increases in reserve capacity and glycolytic reserve were seen. The reasons for this variance between our study an
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br Materials and Methods br Acknowledgements br Introduction
2019-07-18
Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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Our data indicate that the ability of
2019-07-18
Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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It is interesting to note that oligomerization of recombinan
2019-07-18
It is interesting to note that oligomerization of recombinant DDR1 ECD primarily occurred when the protein was incubated with collagen in solution and to a much lesser extent when collagen was pre-immobilized on a surface as reported in our earlier studies (Agarwal et al., 2007). We believe that pre
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Eukaryotic cell cycle machinery is
2019-07-18
Eukaryotic cell cycle machinery is thought to appropriately modulate cell proliferation and cell expansion in various developmental stages and environmental conditions. The core feature of cell-cycle control is the fluctuation of CDK activity, which is regulated by three interactive and conserved me
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Significantly elevated levels of DNA damage
2019-07-18
Significantly elevated levels of DNA damage observed in peripheral blood of tea garden women workers indicate the occupational exposure. The same was observed in cholinesterase activities, which detected lower activity in the exposed group compared to non-exposed. Large volumes of pesticides are use
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Alisol B 23-acetate Consistent with a clear separation of bi
2019-07-18
Consistent with a clear separation of biological function between ARISC and BRISC in cells, mutations in BRCC36 and Abraxas are prevalent in cancer genomes whereas mutations in KIAA0157 are rare. A survey of the Catalogue of Somatic Mutations in Cancer (COSMIC) consortium, revealed that to date, 37
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N acetylation by N acetyltransferase NAT is an important met
2019-07-18
N-acetylation by N-acetyltransferase (NAT) is an important metabolic pathway for some substances, and there are 2 functional NAT isoforms in humans—NAT1 and NAT2. Studies of etamicastat in healthy subjects showed an extensive N-acetylation of etamicastat to the inactive metabolite BIA 5-961, and a l
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Introduction Angiotensin II Ang II and
2019-07-18
Introduction Angiotensin II (Ang II) and Endothelin 1 (ET-1) are potent vasoconstrictive peptides recognized as key players in many cardiovascular diseases [1]. Cardiac hypertrophy, ischemic arrhythmia, and stroke have been associated to an overstimulation of the angiotensin II type 1 (AT1) recepto
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br Discussion Variable estradiol effects on cell
2019-07-18
Discussion Variable estradiol effects on cell proliferation have been reported according to animal species, tissues, and type of estrogen receptor [16,21,22,[29], [30], [31]]. In the kidney, 17βE was found to increase [3H]-thymidine incorporation in primary rabbit kidney proximal tubule Palifosfa
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Finally naringin and hesperidin have different
2019-07-18
Finally, naringin and hesperidin have different glycosidic moieties (neohesperidose α-1,2 and rutinose α-1,6 respectively), bound in the same C7 position on the A ring of the flavonoid. The higher value of k/KM of RHA-Phis towards the former substrate suggests that the enzyme shows a preferential hy
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Despite many studies having demonstrated the importance of c
2019-07-18
Despite many studies having demonstrated the importance of connexin43 (Cx43), the most abundant connexin in bone cells, for bone development and turnover during the last decade [27], little is currently known about GJIC and Cx43 in primary bone tumors. In this report, we analyzed the specific role o
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Several reasons may explain that
2019-07-17
Several reasons may explain that other studies using PDE-5-Is yielded negative or contradictory results [30], [31], [32]. Lee [30] applied 50mg sildenafil to seven patients with liver cirrhosis. NO and cGMP in the hepatic CEP-18770 significantly increased, hepatic and pulmonary resistance decreased
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