0000000000606920

AUTHOR

Pavlo Holenya

showing 2 related works from this author

Severe metabolic alterations in liver cancer lead to ERK pathway activation and drug resistance

2020

Background: The extracellular signal-regulated kinase (ERK) pathway regulates cell growth, and is hyper-activated and associated with drug resistance in hepatocellular carcinoma (HCC). Metabolic pathways are profoundly dysregulated in HCC. Whether an altered metabolic state is linked to activated ERK pathway and drug response in HCC is unaddressed. Methods: We deprived HCC cells of glutamine to induce metabolic alterations and performed various assays, including metabolomics (with 13C-glucose isotope tracing), microarray analysis, and cell proliferation assays. Glutamine-deprived cells were also treated with kinase inhibitors (e.g. Sorafenib, Erlotinib, U0126 amongst other MEK inhibitors). …

Life sciences; biology0301 basic medicineSorafenibMAPK/ERK pathwayCarcinoma HepatocellularResearch paperMAP Kinase Signaling SystemGlutamineProliferationlcsh:MedicineAntineoplastic AgentsGeneral Biochemistry Genetics and Molecular Biology03 medical and health sciences0302 clinical medicineDownregulation and upregulationddc:570medicineSerineHumansHCCProtein Kinase InhibitorsCell Proliferationlcsh:R5-920Cell growthChemistryKinaseMicroarray analysis techniquesLiver Neoplasmslcsh:RGeneral MedicineHep G2 Cellsdigestive system diseasesMetabolic pathway030104 developmental biologyAnaerobic glycolysisDrug Resistance NeoplasmKinase inhibitors030220 oncology & carcinogenesisCancer researchMetabolomeMetabolic stateAerobic glycolysisTranscriptomelcsh:Medicine (General)medicine.drugEBioMedicine
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Design of novel artemisinin-like derivatives with cytotoxic and anti-angiogenic properties

2010

Abstract Artemisinins are plant products with a wide range of medicinal applications. Most prominently, artesunate is a well tolerated and effective drug for treating malaria, but is also active against several protozoal and schistosomal infections, and additionally exhibits anti-angiogenic, anti-tumorigenic and anti-viral properties. The array of activities of the artemisinins, and the recent emergence of malaria resistance to artesunate, prompted us to synthesize and evaluate several novel artemisinin-like derivatives. Sixteen distinct derivatives were therefore synthesized and the in vitro cytotoxic effects of each were tested with different cell lines. The in vivo anti-angiogenic proper…

DrugArtemisininsSwinemedia_common.quotation_subjectmalariaArtemisia annuaAngiogenesis InhibitorsDrug resistanceArtemisia annuaP-glycoproteinPharmacologychemotherapyStructure-Activity Relationshipchemistry.chemical_compoundIn vivoparasitic diseasesmedicineAnimalscancerArtemisininCells CulturedZebrafishCell Proliferationmedia_commondrug resistancebiologyPlant ExtractsArticlesCell BiologyFlow Cytometrybiology.organism_classificationArtemisininsIn vitrochemistryArtesunateMolecular Medicinemedicine.drugJournal of Cellular and Molecular Medicine
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