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In conclusion two novel series of furo pyrimidin
2024-09-18
In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas
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Our initial approach to identify hits was
2024-09-18
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI BAN ORL 24 sale library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility
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br LOX in pancreatic cancer LOX
2024-09-18
5-LOX in pancreatic cancer 5-LOX is a key player in pancreatic cancer (PC) progression. The upregulation of 5-LOX mRNA has been observed in pancreatic adenocarcinoma (PDAC) and also in neoplastic pancreatic tissues (Kennedy et al., 2003). Higher levels of 5-LOX transcripts (messengers) are presen
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br Introduction Human esophageal carcinoma is one of
2024-09-18
Introduction Human esophageal carcinoma is one of the most frequently diagnosed cancers, ranked as the eighth leading causes of cancer-related mortality worldwide. Esophagus squamous cell carcinoma (ESCC) is the most common histological type of esophageal carcinomas, especially with a higher inci
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ATM is required for the proper
2024-09-18
ATM is required for the proper function of the DNA-repair pathway in response to bleomycin-induced DNA damage in mammalian cells [55], [56]. Recent reports suggest that ATM activation by double-strand breaks leads to the subsequent ATR activation [57], [58], [59]. The recruitment of ATR to double-st
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br Ataxia telangiectasia and Rad related as a therapeutic ta
2024-09-18
Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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br Results br Discussion ER and GR
2024-09-18
Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in
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Then Autodock was employed for site directed docking
2024-09-18
Then, Autodock4.2 was employed for site directed docking on AD with the ligands of the cluster(s) having high binding affinities in VS II experiment (Morris et al., 2009). Docking protocols were followed as per our earlier report with 200 GA (genetic algorithm) run (Kalani et al., 2015). Likewise, l
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Arginase deficiency is a rare urea cycle disorder
2024-09-14
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 Materials and methods br Results
2024-09-14
Materials and methods Results Discussion Fluoride can readily penetrate cellular membranes and seriously damage the structure and physiological function of cells (Zhou et al., 2015). Several studies have shown that excessive fluoride can decrease the viability of cells and that the growth o
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br Methodology br Antibiotics in lakes br Antibiotic resista
2024-09-14
Methodology Antibiotics in lakes Antibiotic resistance genes in lakes Perspectives of study on JP 1302 dihydrochloride and ARGs in lakes Conclusion This paper systematically reviewed the distribution of antibiotics and ARGs in global lakes. A total of 57 antibiotics reported at least
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How do increased levels of
2024-09-14
How do increased levels of ammonia as observed in clinical HE constrain synaptic plasticity? Numerous studies have investigated the modulation of signal transduction pathways activated in LTP or LTD irrespective of being necessary or sufficient for changes in synaptic efficacy (Wen et al., 2013). Ye
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Therefore to better understand the functional properties of
2024-09-14
Therefore, to better understand the functional properties of Peruvian infusion tea plants and provide evidence for the development of functional food supplements containing the Peruvian infusion tea plant, the aldose reductase inhibition together with the antioxidant activities of 24 selected Peruvi
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shows the synthesis of imidazole intermediates
2024-09-14
shows the synthesis of imidazole intermediates , , and . The key precursor keto aldehyde – was prepared in situ by SeO mediated oxidation of corresponding carbonyl compounds and or hydrolysis of dibromo ketone . Subsequent treatment with -Boc piperidine-4-carbaldehyde in the presence of aqueous
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APPL was the first adaptor protein identified that
2024-09-14
APPL1 was the first adaptor protein identified that interacts directly with adiponectin receptors [18]. A two-hybrid study by Dong and colleagues revealed that the C-terminal extracellular domain of AdipoR1 interacts with adiponectin, whereas the N-terminal cytoplasmic domain of AdipoR1 interacts wi
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