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ANT located in the IMM mediates the exchange
2021-11-16
ANT, located in the IMM, mediates the exchange of ATP/ADP between the mitochondrial matrix and the intermembrane space (IMS) (Brand et al., 2005; Palmieri and Pierri, 2010). Of the 4 known isoforms, ANT1 is the dominant isoform in the heart (Palmieri and Pierri, 2010). Under physiological conditions
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br Conclusion The addition of cellulose to
2021-11-16
Conclusion The addition of Cy5 NHS ester(Et) receptor to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two
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Currently the computational chemical biology has
2021-11-15
Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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br Conclusion The development discovery of compounds targeti
2021-11-15
Conclusion The development/discovery of compounds targeting small GTPases is challenging [43,44]. Our data point to RBC8 being efficient and potent as a Ral inhibitor in human and mouse platelets, but that it exhibits some activity beyond just Rals, particularly in mouse platelets. It is however
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Importantly lactate and H exert some of
2021-11-15
Importantly, lactate and H+ exert some of their biological effects independently of each other, though sometimes through redundant pathways leading to a same biological effect, as for angiogenesis. In other cases, they can have antagonist effects: lactate was shown to stimulate extracellular matrix
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Olanzapine synthesis Adenosine triphosphate ATP is thought
2021-11-15
Adenosine triphosphate (ATP) is thought to be a crucial molecule in acute pain signaling in the DRG, as well as in the development and maintenance of chronic pain (Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). Extracellular ATP activates the ionotropic P2X receptors (Bur
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The ion conduction pathway reported herein
2021-11-15
The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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Nuclear export of GK has been reported
2021-11-15
Nuclear export of GK has been reported to be dependent on a GK nuclear export signal (NES), mapped to residues 300–310 (Shiota et al., 1999). The assignment of a nuclear export signal common to both the liver and pancreatic GK isoform sequence suggests a possible reversible translocation of GK acros
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The HH Gli pathway has been demonstrated to play
2021-11-15
The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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A group of small molecule with
2021-11-15
A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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br Acknowledgement This work was supported by National
2021-11-15
Acknowledgement This work was supported by National Science Foundation (21475047, 21705051, 21874048), the Science and Technology Planning Project of Guangdong Province (2016B030303010), the Program for the Top Young Innovative Talents of Guangdong Province (2016TQ03N305) and the Foundation for H
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The PK profile and tissue distribution of
2021-11-15
The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an
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br Acknowledgments This research was
2021-11-15
Acknowledgments This research was supported in part by National Institutes of Health IDeA Program COBRE grant GM110732; a USDA National Institute of Food and Agriculture Hatch project; and the Montana State University Agricultural Experiment Station. Introduction Propofol (2,6-Diisopropylphen
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br Conclusions GPCRs are versatile signaling molecules regul
2021-11-15
Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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br FAAH regulation of ECB signaling ECBs
2021-11-15
FAAH regulation of ECB signaling ECBs are fatty myc inhibitor amides and monoacylglyerols functioning as neuromodulator lipids that exhibit rapid (within seconds) on-demand biosynthesis in response to neuronal activation, and are subsequently degraded by specialized catabolic enzymes. There are
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