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A variety of quinazoline or fused pyrimidine
2024-07-06

A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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The GRAVY value for a protein is calculated
2024-07-06

The GRAVY value for a protein is calculated as the sum of hydropathy values of all the amino acids, divided by the number of residues in the sequence (Kyte and Doolittle, 1982). According to Kyte and Doolittle (1982) integral membrane proteins typically have higher GRAVY scores than do globular prot
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As cytosolic acetyl CoA levels in hepatocytes descend cellul
2024-07-06

As cytosolic acetyl-CoA levels in hepatocytes descend, cellular production and concentration of cholesterol go down, a change that is known to be sensed by the Sterol response element binding protein (SREBP)/Cleavage-Activating Protein system, leading to SREBP escort to the Golgi apparatus, cleavage
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Thirdly and finally multiple studies have
2024-07-06

Thirdly and finally, multiple studies have analyzed the activation of neurons in the auditory telencephalic areas of songbirds in response to various auditory stimuli. Neuronal activation was identified by the increased expression of immediate early genes such as fos or ZENK (also know as zif-268, e
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Arginase deficiency is a rare urea
2024-07-06

Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a
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br Conflict of interest br Introduction Platelets are anucle
2024-07-06

Conflict of interest Introduction Platelets are anucleate blood cells essential for hemostasis and wound healing; tight regulation of platelet numbers is crucial for human health. Platelets are synthesized and released from bone marrow megakaryocytes into the circulation where they remain for
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Aconitase clusters are prone to oxidations and are among the
2024-07-06

Aconitase clusters are prone to oxidations and are among the first to undergo a change in transition state during stages of electrophilic stress rendering them inactive [31]. Aconitase activity in LETO and OLETF did not differ at T0 suggesting that the early onset of insulin resistance may not be at
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This unsuspected antagonistic interaction of androgen
2024-07-06

This unsuspected antagonistic interaction of androgen with OXER1 could therefore explain the effect of plant derived compounds with this ligand-receptor system. For example, wedelolactone, a coumestan found in Eclipta alba (false daisy) and in Wedelia calendulacea that is the major component of ecli
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Synaptic scaling up is induced
2024-07-06

Synaptic scaling up is induced within primary visual 2-Amino-ATP (V1) by brief sensory deprivation (Desai et al., 2002; Lambo and Turrigiano, 2013). Several studies have examined the transcriptional changes within extracts of V1 following visual deprivation protocols (Lachance and Chaudhuri, 2004;
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The synthetic route to M developed by Rice
2024-07-05

The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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Mechanisms implicated in antinociception by
2024-07-05

Mechanisms implicated in antinociception by A3R agonists in neuropathic pain are summarized in Box 3. Cellular transduction mechanisms for A3Rs include inhibition of cyclic AMP, PKA via Gαi, interactions with PLC/IP3/DAG and signaling via Gαi and Gαq, and interactions with PI3K/MEK/ERK via βγ subuni
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br Acknowledgments We thank the anonymous reviewers for
2024-07-05

Acknowledgments We thank the anonymous reviewers for their constructive comments on the manuscript, and also thank Dr. Hans-U. Dahms for his comments on the manuscript. This work was supported by a grant from the National Research Foundation (2009-0071218) funded to Young-Mi Lee. This work was al
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br Funding br Introduction l Dihydroxyphenylalanine l DOPA i
2024-07-05

Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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Matrix metalloprotease inhibitors are increasingly available
2024-07-05

Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi
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yohimbine hydrochloride br Author contributions br Acknowled
2024-07-05

Author contributions Acknowledgments TJC, KW, and VG are supported by awards made to MJN: a Consolidator Grant from the European Research Council under Grant no. 311336; a University Research Fellowship from the Royal Society, and a Career Development Award from the Human Frontiers Science Pro
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