2009
Reductive activation of the prodrug 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) selectively occurs in oxygen-deficient cells and overcomes O6-alkylguanine-DNA alkyltransferase mediated KS119 tumor cell resistance
Baumann RP, Penketh PG, Ishiguro K, Shyam K, Zhu YL, Sartorelli AC. Reductive activation of the prodrug 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-[[1-(4-nitrophenyl)ethoxy]carbonyl]hydrazine (KS119) selectively occurs in oxygen-deficient cells and overcomes O6-alkylguanine-DNA alkyltransferase mediated KS119 tumor cell resistance. Biochemical Pharmacology 2009, 79: 1553-1561. PMID: 20005211, PMCID: PMC2885764, DOI: 10.1016/j.bcp.2009.12.004.Peer-Reviewed Original ResearchConceptsAlkylguanine-DNA alkyltransferaseDNA GO6-alkylguanine-DNA alkyltransferaseCell linesBase-catalyzed activationCellular protectionReductive activationCross-link lesionsTumor cell resistanceCultured cellsCell lethalityReductase enzymePosition of guanineDifferent tumor typesIntracellular activationAlkyltransferaseCell resistanceActivationEnzymeCytotoxic effectsCellsOxygen-deficient cellsHypoxic cellsOxygen-deficient conditions
2002
Aggregation of Human Wild-Type and H27A-Prolactin in Cells and in Solution: Roles of Zn2+, Cu2+, and pH
Sankoorikal B, Zhu Y, Hodsdon M, Lolis E, Dannies P. Aggregation of Human Wild-Type and H27A-Prolactin in Cells and in Solution: Roles of Zn2+, Cu2+, and pH. Endocrinology 2002, 143: 1302-1309. DOI: 10.1210/en.143.4.1302.Peer-Reviewed Original ResearchAtT20 cellsSecretory granulesFormation of secretory granulesHuman prolactinZn2+-binding siteTransfected AtT20 cellsCores of secretory granulesHuman wild-typeWild-type prolactinAcidic pHCOS cellsRecombinant human prolactinIntracellular compartmentsWild-typeBinding sitesRat prolactinCu2+Neutral pHProlactinRatio of Zn2Concentrations of hormonesAtT20Cells