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Covalent inhibitors are well suited for
2021-04-25
Covalent inhibitors are well suited for targeting the E1 cystamine mg of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in ci
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Recoverin is a kDa retinal protein that binds to calcium
2021-04-25
Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the 5104 of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, characterized b
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Herbal products may alter the metabolism of certain drugs an
2021-04-25
Herbal products may alter the metabolism of certain drugs and, likewise, the metabolism of components of herbal products may be altered by some drugs, specifically those that affect cytochrome P450 SynaptoRedTM C2 (CYP). These can bring about an alteration of the pharmacokinetics and pharmacologica
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Based on the SUMO SIM interaction involved in SUMOD
2021-04-25
Based on the SUMO–SIM interaction involved in SUMOD positioning, a SUMO2ΔSBD (SIM-binding domain; Q30A, F31A, I33A) mutant can be investigated that disrupts this important binding interface (Eisenhardt et al., 2015; Meulmeester, Kunze, Hsiao, Urlaub, & Melchior, 2008). In Fig. 4A, multiturnover assa
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After incorporation of random nucleotides by TdT during heav
2021-04-25
After incorporation of random sik inhibitor by TdT during heavy-chain rearrangements, both TdT and pol λ may perform in trans polymerase activity (in unknown proportions), whereas synthesis of the complementary strand can only be achieved by pol λ using its gap-filling activity, which TdT lacks bec
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The only reported synthesis of
2021-04-23
The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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In addition to an action via P Y receptors extracellular
2021-04-23
In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se
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chem 8 br Conclusion In vivo pharmacokinetic
2021-04-23
Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokinet
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br Materials and methods br
2021-04-23
Materials and methods Results and discussion Conclusions Conflict of interest Acknowledgments This work was financially supported by the National Natural Science Foundation of China (31302162, 31171762), National High Technology Research and Development Program of China (863 Program,
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We thank Dr Hongqiang Qin at Dalian Institute
2021-04-23
We thank Dr. Hongqiang Qin at Dalian Institute of Chemical Physics, Chinese Academy of Sciences for technical assistance in mass-spectrometric analysis. We thank Prof. Quentin Liu at Dalian Medical University and Prof. Qiang Shen at M.D. Anderson Cancer Center for helpful discussion and comments. Dr
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br Acknowledgements br Introduction Anxiety and depression a
2021-04-23
Acknowledgements Introduction Anxiety and depression are major components of maintaining the cycle of addiction, and are responsible for the negative reinforcement of drug seeking behaviors (Sarnyai et al., 1995, Koob and Le Moal, 2008). Both rats and humans exhibit increased anxiety states du
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The detection of galactomannan GM a polysaccharide that is
2021-04-23
The detection of galactomannan (GM), a polysaccharide that is released during Aspergillus growth, is a useful and reliable non-invasive diagnostic test for screening and management of aspergillosis and is often more sensitive than culture (Schelenz et al., 2015, Fisher et al., 2013). The level of ga
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br Conclusion br Acknowledgements br Introduction
2021-04-23
Conclusion Acknowledgements Introduction In recent years, fast progress has been made toward using the supercritical technology in industrial separation processes. Apart from a green extraction process that replaces organic solvents, applications involving supercritical fluids include super
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br Acknowledgments br Significance The mechanisms underlying
2021-04-23
Acknowledgments Significance The mechanisms underlying the adverse effects of Epo-stimulating agents on the reduced survival of cancer patients are not well understood. Here, we identified EphB4 as an alternative Epo receptor, which triggers Src/Stat3 signaling via EphB4. We also showed that r
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VX-702 br Enzyme activations Activated proteinases
2021-04-23
Enzyme activations Activated proteinases can unleash a deluge of tissue damage (Zucker et al., 2009). Once activated, the essential enzymes such as serine proteases and cysteine proteases cannot discriminate between self and non-self, burning away self-tissues (Chien et al., 2009, Laskar et al.,
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