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br Introduction br Mitochondrial dysfunction
2022-01-03
Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu
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Little is known about the
2022-01-03
Little is known about the role of GPR35 in physiology and pathology. Using GPR35 knockout and wild-type mice showed that GPR35 activation by KYNA improves energy metabolism and inflammation, while demonstrated that GPR35 plays an important role in the development of angiotensin II-induced hyperten
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br Concluding Remarks br Outstanding Questions br
2022-01-03
Concluding Remarks Outstanding Questions Acknowledgments Research on DNA glycosylases in our laboratory is supported by the National Science Foundation (MCB-1517695). A.A.R. and N.P.B. are supported by the National Science Foundation Graduate Research Fellowship Program (DGE-1445197). In
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There are two ways to transport FFAs into
2022-01-03
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty Macitentan transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsible
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Analogous to all GPCRs the
2022-01-03
Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva
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These data suggest that the dehydration of
2022-01-03
These data suggest that the dehydration of the SSRBCs induced by RANTES might result of an activation of the Gardos channel mediated by the chemokine receptor DARC. However, direct evidence of Gardos channel activation by chemokines in Duffy-positive SSRBCs leading to cell dehydration has not been e
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In fish little information about Gpr
2022-01-03
In fish, little information about Gpr84 is available. We have revealed that lipopolysaccharide (LPS) induces significantly up-regulation of zebrafish , and zebrafish overexpression markedly increased the LPS-stimulated production of the cytokine []. Here we expanded on these studies to further inves
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So what makes a FFAR agonist different and
2022-01-03
So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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The ability of GPX and other selenoproteins to be selectivel
2022-01-03
The ability of GPX4 and other selenoproteins to be selectively induced by ferroptotic stimuli suggests that the stress-induced increase in the transcription of a number of putative, “antioxidant” selenoproteins is an adaptive homeostatic, but insufficient response to prevent cell death in the face o
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Over decades a deeper understanding of terpene synthases has
2022-01-03
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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In tumor cells HK II induction is mediated
2022-01-03
In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [
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encorafenib Sonidegib is currently under investigation for t
2022-01-03
Sonidegib is currently under investigation for the treatment of relapsed/refractory acute leukemia (NCT01826214) [76]. All patients experienced at least 1 AE, including anemia, diarrhea, fatigue, nausea, muscle spasms, decreased appetite, and blood creatine phosphokinase increased. The ongoing pha
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Introduction In the s nitric
2021-12-31
Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P
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br Next we explored the SAR around
2021-12-31
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic mmp inhibitor sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did no
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Rifampicin that is methyl piperazinyl imino methyl rifamycin
2021-12-31
Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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