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Derivatives of M that possess
2023-12-18
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these Alrestatin to maintain 5-HTR antagonist properties as (+)-M100907 was demonstra
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Our studies also reveal the
2023-12-18
Our studies also reveal the normal functional roles of the MIR. Interaction between the MIR loop and the N-terminal α helix nucleates conformational maturation of AChR subunits, thereby promoting assembly of mature AChRs [52], [55]. This interaction in homologous parts of all AChR subunits appears t
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In an insightful essay Heryanto writes
2023-12-18
In an insightful essay, Heryanto (1990, 40) writes that language is “a phenomenon expressing the particular history of a society” that did not exist in many parts of the world. “Language is not a universal category or cultural activity. Though it may sound odd, not all people have a language in the
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Physiological total plasma LPA levels are normally less than
2023-12-18
Physiological total plasma LPA levels are normally less than 1μM in healthy subjects. LPA levels have been reported to be increased in malignant effusions or plasma in cancer patients [20]. In addition, increasing ATX activity detected in healthy pregnant women in the third trimester of pregnancy ex
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br Acknowledgments br Introduction Cancer is the leading cau
2023-12-18
Acknowledgments Introduction Cancer is the leading cause of mortality in the United States for those between the ages of 40–79 years, surpassing heart diseases by more than 100,000 deaths [1]. The cause of most cancer subtypes remains idiopathic and may arise out of ‘bad luck’ among otherwise
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The combination of Aurora kinase inhibitors with standard
2023-12-18
The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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We used the lead compound C
2023-12-18
We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.
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Neuropathic animals display increased sensitivity to the ant
2023-12-18
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB cysteine protease inhibitors in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-reg
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br Acknowledgment Supported in part by NIH R EB
2023-12-18
Acknowledgment Supported in part by NIH1R21EB012707 (Biegon, Anat PI). Introduction Estrogens exert pleiotropic effects on a variety of morphological, physiological and behavioral responses in all vertebrate classes ranging from fishes to mammals. Effects of estrogens in the nonreceptor tyros
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In addition to connecting high
2023-12-18
In addition to connecting high ARG1 levels with DNMT3A/TET2 mutations in MDS/CMML patient biopsies, we also wanted to address the cell type demonstrating elevated ARG1. Following our mouse work, we hypothesized that overexpression of this protein would be found in myelomonocytic Sulfo-NHS-SS-Biotin
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br Introduction O Dowd et
2023-12-18
Introduction O’Dowd et al. identified a gene very similar to angiotensin type-1 receptor in 1993 (O’Dowd et al., 1993). The specific selective ligand of this receptor called APJ receptor was determined by Tatemoto et al. in 1998 as apelin (Tatemoto et al., 1998). The high expression of apelin and
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br Impact of global AHR
2023-12-16
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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CA074 Fig A shows a schematic
2023-12-16
Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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Given the powerful and ubiquitous
2023-12-16
Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl
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Although our data show that agrin accelerates the innervatio
2023-12-16
Although our data show that agrin accelerates the innervation of engineered muscle tissue following implantation, there are still several issues that need to be considered. First, the use of primary muscle stem or progenitor Kif15-IN-2 (satellite cells) instead of an immortalized muscle cell line (
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