HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein

Retrovirology

Table 2 Induction of functional conformation and drug transport inhibition exerted by other IINs in CEM MDR cells.

Compound	Concentration μg/ml	UIC2 epitope up-modulation (A)	Doxorubicin efflux inhibition (B)
RDS 1992	25	NT	+
	50	+	++
	100	++	NT
RDS 1996	25	NT	+
	50	NT	++
	100	NT	NT
RDS 1997	25	NT	+
	50	+	++
	100	++	NT
RDS 2012	25	NT	+
	50	+	++
	100	++	NT
RDS 2022	25	NT	+
	50	+	++
	100	++	NT

A, modulation of UIC2 epitope was studied in CEM-VBL10 cells; B, the effect of IINs on the doxorubicin transport inhibition was analysed in CEM-VBL100 cells; NT, not tested; the + or ++ symbols indicate arbitrary units in measuring and differentiating the level of UIC2 epitope modulation and doxorubicin retention.

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