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Resistance to epidermal growth factor receptor inhibition in non-small cell lung cancer

Cancer Drug Resistance 2018年第4期1卷 230-249页

作者： Nele Van Der Steen Elisa Giovannetti daniela carbone Alessandro Leonetti Christian D.Rolfo Godefridus J.Peters Department of Medical Oncology VU University Medical CenterAmsterdam 1081 HVthe Netherlands Department of Pathology Antwerp University HospitalAntwerp 2650Belgium Center for Oncological Research University of AntwerpAntwerp 2610Belgium Cancer Pharmacology Lab AIRC Start-Up UnitUniversity of PisaPisa 56124Italy Medical Oncology Unit University Hospital of ParmaParma 43126Italy University of Maryland Greenebaum Comprehensive Cancer Center Baltimore21220 MDUSA

Aberrant activation of the epidermal growth factor receptor(EGFR)is a driving force for cancer growth in a subgroup of non-small cell lung cancer *** patients can be identified by the presence of activating EGFR *** three generations of EGFR-tyrosine kinase inhibitors(TKIs)have been approved by the Food and Drug Administration and European Medicine *** paper reviews the structure of EGFR and the downstream signaling pathways of EGFR and describes the mechanisms of intrinsic and acquired resistance against *** mechanisms include secondary or tertiary mutations in EGFR,the activation of bypassing signaling pathways or a histological transformation to small cell lung ***,drug efflux transporters will affect the cellular accumulation of EGFR-TKIs and penetration of the first generation of EGFR-TKI into the *** sequestration of some EGFR-TKIs may also prevent the drugs to reach their *** conclusion,resistance to EGFR-TKIs is multifactorial,including primary and acquired mutations in the EGFR gene,activation of bypassing pathways and limited uptake of drugs in the cells or target *** pharmacological studies are needed in order to develop new specific compounds targeted to overcome new resistance mechanisms in order to enable a personalized treatment approach.

关键词： Epidermal growth factor receptor non-small cell lung cancer resistance EGFR-tyrosine kinase inhibitors erlotinib gefitinib afatinib osimertinib rociletinib

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SF3B1 modulators affect key genes in metastasis and drug influx: a new approach to fight pancreatic cancer chemoresistance

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Cancer Drug Resistance 2021年第4期4卷 904-922页

作者： Ornella Randazzo Stella M.Cascioferro Camilla Pecoraro Widad Ait Iddouch Amir Avan Barbara Parrino daniela carbone Ugo Perricone Godefridus J.Peters Patrizia Diana Elisa Giovannetti Department of Medical Oncology Cancer Center AmsterdamAmsterdam UMCVU University Medical CenterAmsterdam 1081 HVThe Netherlands Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche(STEBICEF) Universitàdegli Studi di PalermoPalermo 90133Italy Metabolic Syndrome Research Center Mashhad University of Medical SciencesMashhad 91886-17871Iran Cancer Research Center Mashhad University of Medical SciencesMashhad 91886-17871Iran Student Research Committee School of MedicineMashhad University of Medical SciencesMashhad 91886-17871Iran Drug Discovery Unit Fondazione Ri.MEDPalermo 90128Italy Department of Biochemistry Medical University of GdanskGdansk 80-210Poland Cancer Pharmacology Lab AIRC Start Up UnitFondazione Pisana per la ScienzaPisa 56124Italy.

Aim:Because mutations of splicing factor 3B subunit-1(SF3B1)have been identified in 4%of pancreatic ductal adenocarcinoma(PDAC)patients,we investigated the activity of new potential inhibitors of SF3B1 in combination with gemcitabine,one of the standard drugs,in PDAC cell ***:One imidazo[2,1-b][1,3,4]thiadiazole derivative(IS1)and three indole derivatives(IS2,IS3 and IS4),selected by virtual screening from an in-house library,were evaluated by the sulforhodamine-B and wound healing assay for their cytotoxic and antimigratory activity in the PDAC cells SUIT-2,Hs766t and Panc05.04,the latter harbouring the SF3B1 *** effects on the splicing pattern of proto-oncogene recepteur d’origine nantais(RON)and the gemcitabine transporter human equilibrative nucleoside transporter-1(hENT1)were assessed by PCR,while the ability to reduce tumour volume was tested in spheroids of primary PDAC ***:The potential SF3B1 modulators inhibited PDAC cell proliferation and prompted induction of cell *** compounds showed an interesting anti-migratory ability,associated with splicing RON/ΔRON shift in SUIT-2 cells after 24 h ***,IS1 and IS4 potentiated the sensitivity to gemcitabine in both conventional 2D monolayer and 3D spheroid cultures,and these results might be explained by the statistically significant increase in hENT1 expression(P<0.05 *** control cells),potentially reversing PDAC ***:These results support further studies on new SF3B1 inhibitors and the role of RON/hENT1 modulation to develop effective drug combinations against PDAC.

关键词： Pancreatic ductal adenocarcinoma gemcitabine indole derivatives anti-proliferative activity anti-migratory activity SF3B1 RON hENT1

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