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Screening of the compounds allowed for a number of
2021-09-24
Screening of the compounds allowed for a number of interesting SAR observations. First of all, pyridyl analogue demonstrated that a pyridine ring would be beneficial for both log as well as increasing the potency (entry 2 versus entry 1). Electron-poor aryl groups next to the oxadiazolone were detr
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LPCs have been previously described as potential anti
2021-09-24
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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br Acknowledgement The author expresses her sincere
2021-09-24
Acknowledgement The author expresses her sincere appreciation to Brian P. Kenealy, Ph.D. for his contributions to the series of studies described in this article that were conducted during his tenure in the lab, as a graduate student first and then a postdoctoral research fellow. She also thanks
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Dimesna br Materials and methods br Results br Discussion Th
2021-09-24
Materials and methods Results Discussion The redox domain that spans the region between amino Dimesna positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent crystal structures of
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Tail group SAR of the imidazole
2021-09-24
Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl
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topoisomerase inhibitor Also considered very rare is progres
2021-09-24
Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic topoisomerase inhibitor decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor antibodies
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Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) Gli si
2021-09-24
Gli signaling pathways play critical roles in embryonic and postnatal lung development [22]. Many reports suggest that wound healing and fibrotic diseases involve activation of pathways used during development [23]. In the adult lung, Gli signaling activity measured by Gli1 expression is restricted
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In the past two decades
2021-09-24
In the past two decades, studies of the non-B cell-derived Ig, including cancer cell-derived IgG, have been predominately facilitated by general anti-human Ig antibodies, which do not distinguish the non-B Ig from classical Ig derived from B cells. Due to this caveat, it remains obscure about whethe
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Neither E nor Z FPP synthase catalyzed
2021-09-24
Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase
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Whether histamine receptor distribution is altered in canine
2021-09-24
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist,
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In the present study fasting blood glucose and insulin
2021-09-23
In the present study, fasting blood glucose and insulin levels were not significantly different between GA patients and control cases. Normal mammalian cells typically acquire fatty acids from the circulation owing to insulin, which is the most lipogenic hormone in the subset of adult tissues, inclu
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Mitochondrial binding by HK prevents mortality
2021-09-23
Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,
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br Acknowledgments This research was funded by generous
2021-09-23
Acknowledgments This research was funded by generous grants from the Singapore National Medical Research Council (NMRC CBRG grant NMRC/CBRG12Nov114 (BD)). WJC is supported by NMRC Clinician Scientist Investigator award and partly supported by a Singapore Cancer Syndicate Grant, the National Resea
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One important aspect about GSK inhibitors is their
2021-09-23
One important aspect about GSK-3 inhibitors is their effect on pluripotency of galanin [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of events preserv
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br Funding This work was partially supported
2021-09-23
Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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