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. 2019 Dec 29;21(1):238. doi: 10.3390/ijms21010238

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© 2019 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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TMP195 re-sensitizes ABCB1-overexpressing cells to paclitaxel and ABCG2-overexpressing cells to mitoxantrone. The chemosensitization effect of TMP195 was examined by treating cells with increasing concentrations of paclitaxel (a known substrate drug of ABCB1), or mitoxantrone (a known substrate drug of ABCG2) or etoposide (a known substrate drug of ABCC1) in the presence of DMSO (open circles) or TMP195 at 1 μM (open squares), 2 μM (filled squares), 3 μM (open triangles) or 5 μM (filled triangles). (A) Drug-sensitive parental KB-3-1 (left panel) and the ABCB1-overexpressing multidrug resistance (MDR) variant KB-V-1 (right panel) human epidermal cancer cells, as well as (B) HEK293 cells (left panel) and HEK293 cells transfected with human ABCB1 (MDR1, right panel) were used to determine the effect of TMP195 on ABCB1-mediated paclitaxel resistance. (C) Drug-sensitive parental S1 (left panel) and the ABCG2-overexpressing MDR variant S1-M1-80 (right panel) human colon cancer cells, as well as (D) HEK293 cells (left panel) and HEK293 cells transfected with human ABCG2 (R482, right panel) were used to determine the effect of TMP195 on ABCG2-mediated mitoxantrone resistance. (E) Drug-sensitive parental COR-L23/P (left panel) and the ABCC1-overexpressing MDR variant COR-L23/R (right panel) human lung cancer cells, as well as (F) HEK293 cells (left panel) and HEK293 cells transfected with human ABCC1 (MRP1, right panel) were used to determine the effect of TMP195 on ABCC1-mediated etoposide resistance. Points, mean values from at least three independent experiments; error bars, SEM.

TMP195 re-sensitizes ABCB1-overexpressing cells to paclitaxel and ABCG2-overexpressing cells to mitoxantrone. The chemosensitization effect of TMP195 was examined by treating cells with increasing concentrations of paclitaxel (a known substrate drug of ABCB1), or mitoxantrone (a known substrate drug of ABCG2) or etoposide (a known substrate drug of ABCC1) in the presence of DMSO (open circles) or TMP195 at 1 μM (open squares), 2 μM (filled squares), 3 μM (open triangles) or 5 μM (filled triangles). (A) Drug-sensitive parental KB-3-1 (left panel) and the ABCB1-overexpressing multidrug resistance (MDR) variant KB-V-1 (right panel) human epidermal cancer cells, as well as (B) HEK293 cells (left panel) and HEK293 cells transfected with human ABCB1 (MDR1, right panel) were used to determine the effect of TMP195 on ABCB1-mediated paclitaxel resistance. (C) Drug-sensitive parental S1 (left panel) and the ABCG2-overexpressing MDR variant S1-M1-80 (right panel) human colon cancer cells, as well as (D) HEK293 cells (left panel) and HEK293 cells transfected with human ABCG2 (R482, right panel) were used to determine the effect of TMP195 on ABCG2-mediated mitoxantrone resistance. (E) Drug-sensitive parental COR-L23/P (left panel) and the ABCC1-overexpressing MDR variant COR-L23/R (right panel) human lung cancer cells, as well as (F) HEK293 cells (left panel) and HEK293 cells transfected with human ABCC1 (MRP1, right panel) were used to determine the effect of TMP195 on ABCC1-mediated etoposide resistance. Points, mean values from at least three independent experiments; error bars, SEM.