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br Acknowledgements This work was
2023-10-18
Acknowledgements This work was supported by the National Key Technology Research and Development Program (2012BAD19B01) and General Financial Grant from the China Postdoctoral Science Foundation (2015M581754). Introduction Cough is one of the most important defensive reflex brought into actio
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The discovery of acetylsalicylic acid aspirin in paved the w
2023-10-18
The discovery of acetylsalicylic neuron specific enolase (aspirin) in 1897 paved the way for the development of classical NSAIDs as first-line therapeutics for anti-inflammatory, anti-pyretic and analgesic therapy. Large efforts have been made in the following decades to improve the efficacy and in
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br Involvement of LPA receptors in
2023-10-18
Involvement of LPA receptors in cancer LPA׳s effects are mediated by at least six different G protein-coupled receptors (LPA1–6). Human gastric and ovarian cancers overexpress the mRNA encoding LPA1 and LPA2 compared to healthy tissues [6], [11], [12]. Papillary and follicular thyroid cancers exh
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The Type A series contains of the confirmed hits making
2023-10-18
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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Although the interactions of PhLP with G and its
2023-10-17
Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls endo-iwr signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its interacting partners i
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Introduction Cardiovascular disease is the
2023-10-17
Introduction Cardiovascular disease is the principal cause of morbidity and mortality in patients with AI-10-49 (1). Comprehensive management of these patients includes not only adequate glycemic control but also attention to additional recognized risk factors. Hypertension is a cardiovascular ris
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mostly The specific functions of ERs and AR underline their
2023-10-17
The specific functions of ERs and AR underline their crucial roles during different phases of spermatogenesis. Their deregulation could affect numerous downstream targets, thereby, disrupting spermatogenesis and male fertility. Various studies have shown that estrogen-like chemicals in the environme
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Cucurbitacin I Cells have developed strategies aiming to enh
2023-10-17
Cells have developed strategies aiming to enhance both the efficiency of proteins with chaperone activity as well as their overall antioxidant capacity to maintain proteostasis under oxidative stress conditions (Miyata et al., 2012). For instance, 2-Cys peroxiredoxin is an abundantly expressed, anti
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Further evidence for action mechanism was provided by assays
2023-10-17
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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Given the powerful and ubiquitous nature of adenosine
2023-10-17
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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Nutritional factors affecting ASD have also
2023-10-17
Nutritional factors affecting ASD have also recently received attention. An increase in postsynaptic zinc (Zn) level induced by clioquinol (a Zn chelator and ionophore), and the subsequent activation of NMDA receptors through the tyrosine kinase Src, rescued social interaction in Shank2−/− mice (Lee
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Our initial approach to identify hits was two pronged
2023-10-17
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI Griseofulvin library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility wa
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The H N mutation in exon
2023-10-17
The H373N mutation in exon 6 has not previously been reported [3], [4], [5], [6]; thus, this mutation appears to be a novel mutation. The functional expression study demonstrated that the H373N mutation results in almost complete loss of enzymatic activity. Thus, it is highly likely that the H373N m
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br Studies in zebrafish vascular and
2023-10-17
Studies in zebrafish: vascular and neural development and the regulation of left–right asymmetry Zebrafish embryos represent an excellent model system to examine vertebrate vascular development. Major advantages of the zebrafish system include its genetic tractability, small size, external fertil
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exemplifies three of the compounds
2023-10-17
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC deoxycorticosterone synthesis as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or de
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