fig1

Identification of antibody-drug conjugate payloads that are substrates of ATP-binding cassette drug efflux transporters

Figure 1. Heatmap of ADC payload activity across multidrug-resistant and control cell lines. (A) P-gp efflux potential: Unsupervised clustering of AUC values from dose-response viability assays of a panel of cytotoxic agents tested against parental, multidrug-resistant, and genetically modified KB and MDR-19 cell lines. Cell lines include KB-3-1 (parental) and KB-8-5-11 (P-gp overexpressing); HEK-293-derived MDR-19 (ABCB1 transfected) and its vector control (pcDNA), as well as P-gp–inhibited counterparts (+TQR, tariquidar); (B) ABCG2 efflux potential: Unsupervised clustering of AUC values from dose-response viability assays of a panel of cytotoxic agents tested against parental, genetically modified, and multidrug-resistant HEK and H460 cell lines. Cell lines include H460 (parental) and H460-MX20 (ABCG2 overexpressing); HEK-derived HEK-R5 (ABCG2 transfected) and its vector control (pcDNA), as well as ABCG2–inhibited counterparts (+Ko143). ADC: Antibody-drug conjugate; P-gp: P-glycoprotein; AUC: area under the curve; ABCB1: adenosine triphosphate-binding cassette B1; TQR: tariquidar; MOA: mechanism of action.

Cancer Drug Resistance
ISSN 2578-532X (Online)

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