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However although in vitro studies in heterologous systems ha
2024-09-04
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Having established the structural requirements for
2024-09-04
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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br Discussion Herein we demonstrate that
2024-09-04
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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br Synthetic lethal approaches In
2024-09-04
Synthetic lethal approaches In addition to the potential utility of ATM and ATR as chemo- or radiosensitisers, recent studies suggest that such compounds may have single agent activity in certain subsets of patients through induction of synthetic lethality. Two genes are considered synthetically
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br Mechanisms of GPCR internalization Like for
2024-09-04
Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated Carprofen (CME) is the best characterized and arguabl
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In previous years evidence emerged that inferred secondary
2024-09-04
In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic AICAR (7) and piceatannol (8) (Fig. 3b) on mammalian arginase with IC50s of 10.6
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Various antiangiogenic drugs have been
2024-09-04
Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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Abnormalities in placentation in patients with PE appear to
2024-09-04
Abnormalities in placentation in patients with PE appear to be associated with changes in different components of the signaling pathway that mediates cytotrophoblast migration/invasion. Studies have showed that the activation of the Notch signaling pathway is associated with the differentiation and
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With regard to participation of
2024-09-03
With regard to participation of the 12S-lipoxygenase in diabetes mellitus, inconsistent results have been obtained. Earlier studies demonstrated that the leukocyte-type 12S-lipoxygenase is specifically expressed in pancreatic b-cells and is involved in regulating glucose-stimulated insulin secretion
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br Experimental Procedures br Acknowledgments We thank the
2024-09-03
Experimental Procedures Acknowledgments We thank the members of the Qing laboratory for helpful suggestions and Biotree Biotech Co., Ltd. (Shanghai, China) for metabolomics analysis and data interpretation. This study was supported by the National Key Research and Development Program of China
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br Neurological development and BCAAs Glutamate is an import
2024-09-03
Neurological development and BCAAs Glutamate is an important excitatory neurotransmitter in the brain, and BCAAs (especially leucine) function to synthesize glutamate in astrocytes around neurons, since leucine enters the brain from the blood more rapidly than other phospholipase inhibitor and p
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Another issue is that the vast majority of data from
2024-09-03
Another issue is that the vast majority of data from PET and CSF are from selected participants recruited through tertiary care dementia centers [176]. It is widely recognized that clinic-based participants differ from community-based studies, for example, the amount, type, and distribution of neuro
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br Disclosures br Author contributions br
2024-09-03
Disclosures Author contributions Grants This work was supported by National Institutes of Health/National Heart, Lung, and Blood Institute MERIT Award R37 HL040696 to J.A.F. Acknowledgments Introduction The AGC kinases, named after the protein A, G and C kinases, are an evolutionaril
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br Introduction Psychostimulant abuse and addiction remain a
2024-09-03
Introduction Psychostimulant abuse and addiction remain a societal problem in the United States. The latest statistics from the National Survey on Drug Use and Health indicate that slightly less than one million people over the age of 12 report having a cocaine use disorder (NSDUH, 2016). Additio
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Luciferase Immunoprecipitation Systems LIPS which utilizes r
2024-09-03
Luciferase Immunoprecipitation Systems (LIPS), which utilizes recombinant antigens fused to the enzyme reporter Renilla luciferase (Ruc) to detect patient antibodies, provides a unique platform to investigate Amikacin disulfate directed against a variety of antigenic targets [25]. Previously, LIPS
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