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br Experimental section br Competing interests
2023-09-28
Experimental section Competing interests Author's contributions Acknowledgement This research is partially supported by a seed fund for the Center for Drug Discovery and Translational Research (LS) and a research grant by Fujifilm (VPS and LS). The Sponsors played no roles in study desig
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Although several different membrane estrogen receptors
2023-09-28
Although several different membrane estrogen receptors have been reported (Qiu et al., 2008; Revankar et al., 2005), a large percentage of membrane-initiated steroid hormone signaling appears to be performed by a subpopulation of the same receptors that act in the nucleus. Specifically, estrogen rec
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c1v1 c2v2 In this review we will present the traditional
2023-09-28
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Our previous studies and others have identified that the inh
2023-09-28
Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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The expanding catalog of glutamate
2023-09-28
The expanding catalog of glutamate receptor auxiliary subunits and associated transmembrane proteins underscores the importance and complexity of the receptor complexes. Whereas the interactions described here specifically control AMPARs, distinct auxiliary subunits, Neto-1/2, modulate neuronal kain
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LAP locations in the parasite tissues would
2023-09-28
LAP locations in the parasite tissues would provide clues for the potential physiological roles of it inside the parasite body. To date, tissue localization of LAPs has been carried out in many helminth parasites; however, information regarding LAPs in tapeworm is scarce. It was shown that LAPs were
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Recently two distinct small molecule inhibitors of
2023-09-28
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Fmoc-Cys(Trt)-ol with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the
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The G R mutation is located at the
2023-09-28
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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The ORR obtained with crizotinib on our cohort was low
2023-09-28
The ORR obtained with crizotinib on our cohort was low compared to other studies, such as the prospective studies of A. Shaw et al. (ORR = 65% in second line), B. Solomon et al. (ORR = 74% in first line) and the more comparable large retrospective study of M. Duruisseaux et al. on the French CLINALK
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Most of the identified aldose reductase inhibitors possess u
2023-09-28
Most of the identified aldose reductase inhibitors possess undesirable effects like poor pharmacokinetic properties, hypersensitivity and Steven-Johnson Syndrome [1]. However, the main side effect is the lack of selectivity relative to aldehyde reductase (ALR1, EC 1.1.1.2). ALR1 plays the important
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In this study we demonstrated
2023-09-28
In this study, we demonstrated that DRR1 protein level in GBM tissues was significantly higher compared to normal Biocytin mg tissues. This data suggested that DRR1 might play a role in the tumorigenesis of glioma. To investigate whether DRR1 could accurately predict the outcome in patients with gl
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AdK as an important upstream regulator of adenosine
2023-09-28
AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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br Difference between ACh and ER tests There are few
2023-09-28
Difference between ACh and ER tests There are few reports concerning the provoked spasm between ER and ACh in the same patients [51], [52], [53]. Different mediators may have the potential of different coronary responses. In our experience, spasm provoked by intracoronary injection of ER is focal
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Using our infection assays we also explored whether low
2023-09-27
Using our infection assays, we also explored whether low-pH compartments were required for the entry of ZIKVs in mammalian cells. Lysosomotropic agents such as ammonium chloride, chloroquine and Bafilomycin A1, strongly inhibited the ability of ZIKVs to enter mammalian cells. Our results are in agre
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In addition to the data provided
2023-09-27
In addition to the data provided by the Ki16425 treatment in the K/BxN arthritis model, new findings from the study of two new LPA receptor antagonists confirm the involvement of the LPA pathway in the pathogenesis of experimental arthritis. In the study by Miyabe et al., the authors reported the tr
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