Hyperoside exhibits anticancer activity in non ‑small cell lung cancer cells with T790M mutations by upregulating FoxO1 via CCAT1.

In conclusion, hyperoside inhibited proliferation and induced apoptosis by upregulating FoxO1 via CCAT1 in T790M‑positive NSCLC both in vitro and in vivo, suggesting that hyperoside is a novel candidate for T790M‑positive NSCLC treatment. PMID: 31894285 [PubMed - as supplied by publisher]
Source: Oncology Reports - Category: Cancer & Oncology Tags: Oncol Rep Source Type: research

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Abstract Ruthenium compounds have shown to be promising alternatives to platinum(II) drugs. However, their clinical success depends on achieving mechanisms of action that overcome Pt-resistance mechanisms. Electron-deficient organoruthenium complexes are an understudied class of compounds which exhibit unusual reactivity in solution and may offer novel anticancer mechanisms of action. Here, we evaluate the in vitro and in vivo anticancer properties of the electron-deficient organoruthenium complex [(p-cymene)Ru(maleonitriledithiolate)]. This compound is found to be highly cytotoxic: 5 to 60 times more potent than ...
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research
Abstract Eleven novel acridone derivatives were synthesized and evaluated for their anticancer activity against 60 human cancer cell lines. Five compounds 8b, 8d, 8g, 8h, and 8k displayed very good in vitro antiproliferative activities well over 95% of the panels. The most active compound is 8k (5, 7-dibromo-3-phenyl-3,4-dihydroacridin-1 (2H)-one). In addition, 8k was the most sensitive agent in all 9 panels starting with prostate (0.075 µm), leukemia (0.116 µm), non-small cell lung cancer (0.164 µm), colon cancer (0.193 µm), CNS cancer (0.264 µm), melanoma (0...
Source: Bioorganic and Medicinal Chemistry - Category: Chemistry Authors: Tags: Bioorg Med Chem Source Type: research
Immune-checkpoint inhibitors (ICIs) have emerged relatively recently as a new therapeutic option for advanced non-small –cell lung cancer (NSCLC): as second-line therapy after chemotherapy [1], first-line monotherapy for patients with>50% programed cell-death –protein-1 ligand-1 (PD-L1) expression on tumor cells [2] or in combination with chemotherapy for any PD-L1–expression level [3]. However, ICIs can cause immune-related adverse events (irAEs) affecting any organ but, most frequently, skin, colon, endocrine organs, liver and lungs [4].
Source: Lung Cancer - Category: Cancer & Oncology Authors: Source Type: research
In this study, circCCDC66 in NSCLC cells was highly expressed. Downregulation of circCCDC66 impaired cell proliferation, migration and invasion whereas boosted cell apoptosis in NSCLC. Data from molecular mechanism assays testified that circCCDC66 bound with miR-33a-5p in NSCLC cells. And miR-33a-5p inhibition could rescue the suppressive effect of circCCDC66 knockdown on NSCLC progression. In addition, karyopherin subunit alpha 4 (KPNA4) in NSCLC cells was proofed to be directly targeted by miR-33a-5p. Moreover, through rescued-function assays, we observed that upregulating KPNA4 expression could countervail the restraini...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - Category: Drugs & Pharmacology Authors: Tags: Biomed Pharmacother Source Type: research
CONCLUSIONS: These preliminary results demonstrate the success of a Military Treatment Facility (MTF)-based LCS Program in the detection of early stage lung cancer. Earlier stage detection may result in better health outcomes for affected patients. In the population studied, duration of smoking proved to be more significant than pack-years in predicting lung cancer risk. These results validate the newly dedicated resources and continued efforts to strengthen the LCS program at NMCSD and across MTFs. PMID: 31925432 [PubMed - as supplied by publisher]
Source: Military Medicine - Category: International Medicine & Public Health Tags: Mil Med Source Type: research
Synlett DOI: 10.1055/s-0039-1690781 In this work, 21 novel (1,4-disubstituted 1,2,3-triazole)-dihydropyrimidinone (1,2,3-trzl-DHPM) type hybrids were synthesized and characterized. These were divided into two types: hybrids A (5 in total) containing the dihydropyrimidinone heterocyclic ring decorated with a 1,4-disubstituted 1,2,3-triazole in the C-5 position [these compounds were accessed by a multicomponent copper(I)-catalyzed azide alkyne cycloaddition (CuAAC) (or click)–Biginelli reactions with satisfactory yields (39–57%)] and hybrids B (16 in total) containing two 1,2,3-triazole units in the C-5 and C-6 m...
Source: Synlett - Category: Chemistry Authors: Tags: letter Source Type: research
AbstractDammarenolic acid (DA) is an A-seco-dammarane triterpenoids, isolated fromDipterocarpus alatus resin. DA was modified including reactions of esterification and amination with heterocyclic amines andl-amino acids. The structures of new compounds were confirmed by MS,1H NMR, and13C NMR spectroscopic analyses and their activities againstα-glucosidase and acetylcholinesteras were studied. The cytotoxic activity of DA was screened using a broad panel of 60 human cancer cell lines and it has cytotoxic effect for a variety of human tumor cell lines (leukemia, non-small cell lung cancer, colon cancer, CNS cancer, mel...
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research
This report is the first to elucidate the localization and accumulation of dacomitinib in the rat intestine and skin and should be valuable during efforts to clarify the mechanism dacomitinib-induced diarrhea or skin toxicities. PMID: 32001948 [PubMed]
Source: Acta Histochemica et Cytochemica - Category: Biochemistry Authors: Tags: Acta Histochem Cytochem Source Type: research
Heerlein Hussain :The epidermal growth factor receptor (EGFR) family contains four transmembrane tyrosine kinases (EGFR1/ErbB1, Her2/ErbB2, Her3/ErbB3 and Her4/ErbB4) and 13 secreted polypeptide ligands. EGFRs are overexpressed in many solid tumors, including breast, pancreas, head-and-neck, prostate, ovarian, renal, colon, and non-small-cell lung cancer. Such overexpression produces strong stimulation of downstream signaling pathways, which induce cell growth, cell differentiation, cell cycle progression, angiogenesis, cell motility and blocking of apoptosis.The high expression and/or functional activation of EGF...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Review Source Type: research
ConclusionNSCLC patients represented genetically heterogeneous subgroup with a high frequency of co-occurring mutations in cancer-associated pathways. This diverse mutational profile may have key clinical and research implications for understanding the variability of treatment outcome in pre-TKI-treated NSCLC population. The differences in the MAF ofEGFR T790M may determine different responses to TKI therapy in patients harboring dual mutations.
Source: Journal of Cancer Research and Clinical Oncology - Category: Cancer & Oncology Source Type: research
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