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With rare exceptions the biological role of secretase
2021-09-02
With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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carboxypeptidase a br Acknowledgments The research leading
2021-09-02
Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/
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Several classes of small molecule inhibitors of FBPase
2021-09-02
Several PHA 543613 hydrochloride of small-molecule inhibitors of FBPase have been reported. These inhibitors can be structurally classified into two groups; non-phosphorus-based inhibitors and phosphorus-based inhibitors. In the former group, several chemotypes including anilinoquinazoline, indole d
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NMR analyses support the above statement
2021-09-02
NMR analyses support the above statement. Compound 32 is an interesting example of an isosteric analog of compounds 12–14. It has been demonstrated that 32 forms a rather stable six-membered ring via a hydrogen bond based on the chemical shift of the phosphorus chir99021 at the C-3 position as illu
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A key inciting event in atherosclerosis is
2021-09-02
A key inciting event in atherosclerosis is the deposition of circulating low-density lipoprotein (LDL) in the subendothelial space of major arteries. In the subendothelium, native LDL is no longer protected by circulating antioxidants and is oxidatively modified to oxidized LDL (OxLDL) [5]. OxLDL is
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br Author contribution br Acknowledgements We want to thank
2021-09-02
Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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br General Characteristics of the Type II Dehydrogenases Alt
2021-09-01
General Characteristics of the Type II Dehydrogenases Alternative NAD(P)H dehydrogenases conduct the reaction of the rotenone-insensitive oxidation of cytosolic and mitochondrial matrix NADH and/or NADPH (Fig. 1) (Melo et al., 2004, Rasmusson et al., 2004, Rasmusson et al., 2008). They catalyze t
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nicotinic receptor agonist We also determined the uracil con
2021-09-01
We also determined the uracil content of CJ236 DNA by thin-layer chromatography of in vivo32P- or [6-3H]uracil-labeled CJ236 2′-deoxyribose 5′-monophosphates as well as by LC/MS of deoxyuridine and thymidine 2′-deoxynucleosides (Table 1, Table 2, Table 3). Examination of the 32P data showed that, ba
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SB 415286 In summary A is a potent orally available
2021-09-01
In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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Renal injury by cisplatin has been
2021-09-01
Renal injury by cisplatin has been associated with oxidative stress, inflammation, and apoptosis (Francescato et al., 2007, Iseri et al., 2007, Kiymaz et al., 2008, Ueki et al., 2012). Specifically, apoptosis is an important mode of cell death in cisplatin nephrotoxicity, and many studies including
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Milrinone Introduction Primitive neuroectodermal tumors PNET
2021-09-01
Introduction Primitive neuroectodermal tumors (PNETs) are malignant, small round cell tumors of neural crest origin which typically arises from bone or soft tissue in the trunk/axial skeleton/paraspinal regions in adolescents and young adults and comprises of and prostate is extremely rare.1, 2 Th
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Little information is available regarding the expression
2021-09-01
Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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Plasminogen is composed of five N
2021-09-01
Plasminogen is composed of five N-terminal kringle domains and a C-terminal serine protease domain. The kringle domains have an affinity to lysine and binding of plasminogen with its receptors is dependent on its lysine interacting kringle domains [10], [28]. In the current report, we show that enol
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The endothelin receptor type B
2021-09-01
The endothelin receptor type B (EDNRB) belongs to the family of G protein-coupled receptors, which functions as a vital regulatory factor in signal transduction in cells, locating on human chromosome 13q22.3 (Ayala-Valdovinos et al., 2016; Bregar et al., 2018; Morimoto et al., 2018; Widowati et al.,
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Intriguingly one E residue may
2021-09-01
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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