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Camptothecin is a type of topo I inhibitor
2021-09-23
Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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In summary we propose a
2021-09-23
In summary, we propose a model that explains the possible mechanism the HULC mediates activation of HBV in liver cancer Sorbitol sale (Fig. 8). In the model, HULC promotes the expression of miR-539 by stimulating HBx-co-activated STAT3. Then, miR-539 down-regulates APOBEC3B, leading to an increase
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The CNP pGC B cGMP pathway has been
2021-09-23
The CNP/pGC-B/cGMP pathway has been reported to be potent inhibitor of fibrosis, from an intrinsic compensatory protective response as well as a therapeutic in cardiorenal injury and disease states [6,12,13,22,30]. Indeed, fibrosis is a progressive process leading to increased risk for morbidity and
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CaCl was from the Radiochemical
2021-09-23
45CaCl2 was from the Radiochemical Centre (Amersham, UK), NaVO3 was from Reachim (Moscow, Russia). Tetrodotoxin was purchased from Calbiochem, DTNB from Merck, Darmstadt, Germany. Nifedipine was synthesized in the Institute of Drug Research, Modra, Slovakia and was kindly provided by Dr. Zdeno Mahrl
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VS strategies have been building momentum in G
2021-09-23
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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br Acknowledgements We apologize to our distinguished
2021-09-23
Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri
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We also intended to determine
2021-09-22
We also intended to determine the possible mechanism underlying EZH2 upregulation in the PC. Although no recurrent mutations of EZH2 have been described in CLL [27, 28, 29], we aimed to rule out the possibility of activating mutations in the background of EZH2 overexpression. We detected no mutation
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Electrostatic potential along with measurement and modeling
2021-09-22
Electrostatic potential along with measurement and modeling of corresponding energies is vital for inferring protein properties, lone or complexed with ligands. DelPhi was used for solving Poisson Boltzmann equation, obtaining grid, total reaction and coulombic energies after solvating the proteins
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We first set out to identify the minimum
2021-09-22
We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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br Introduction The amino acid
2021-09-22
Introduction The amino BTL-104 glycine functions as a neurotransmitter in the vertebrate central nervous system: as an inhibitory neurotransmitter and as a co-agonist of the NMDA-subtype of excitatory glutamatergic receptors (Eulenburg et al., 2005). Under a current hypothesis that schizophrenia
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C http www apexbt com media
2021-09-22
C136 is present in the joining region of two domains of NEIL1 and plays a critical role in the stability and dynamics of enzyme (Roy et al., 2007, Prakash et al., 2014). E181 resides in the conserved H2TH motif that binds to DNA and is very essential for enzyme activity. C136 is present in the near
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Crystal structure of CD LEL have revealed
2021-09-22
Crystal structure of CD81-LEL have revealed the head sub-domain to be implicated in binding to HCV (Kitadokoro et al., 2001). In a study using African green monkey CD81, T163A, F186 L, E188K and D196E mutations disrupted HCV E2 binding (Higginbottom et al., 2000). In our docking studies, T163 and D1
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Importance of glucokinase in glucose homeostasis and a
2021-09-22
Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of g
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Over decades a deeper understanding
2021-09-18
Over decades, a deeper understanding of terpene synthases has also permitted enzyme engineering for unnatural substrate acceptance. Novel terpenoids have been successfully synthesized from substrate analogues as by-products from mechanistic investigation (Faraldos et al., 2012; Miller, Yu, & Alleman
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br Ethical standards br Conflicts of
2021-09-18
Ethical standards Conflicts of interest Funding This study was funded by the National Natural Science Foundation of China (grant numbers 81560146, 81660148 and 81760151), Gansu Province health industry research project (grant number GSWSKY-2015-10) and Lanzhou Chengguan District Science and
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