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Mechanistic Basis of Breast Cancer Resistance Protein Inhibition by New Indeno[1,2-b]indoles by Kita, Diogo Henrique (author);Guragossian, Nathalie (author);Zattoni, Ingrid Fatima (author);Moure, Vivian Rotuno (author);Rego, Fabiane Gomes de Moraes (author);Lusvarghi, Sabrina (author);Moulenat, Thomas (author);Belhani, Billel (author);Picheth, Geraldo (author);Bouacida, Sofiane (author);Bouaziz, Zouhair (author);Marminon, Christelle (author);Berredjem, Malika (author);Jose, Joachim (author);Gonçalves, Marcos Brown (author);Ambudkar, Suresh V. (author);Valdameri, Glaucio (author);Le Borgne, Marc (author) is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract The ATP-binding cassette transporter ABCG2 mediates the efflux of several chemotherapeutic drugs, contributing to the development of multidrug resistance (MDR) in many cancers. The most promising strategy to overcome ABCG2-mediated MDR is the use of specific inhibitors. Despite many efforts, the identification of new potent and specific ABCG2 inhibitors remains urgent. In this study, a structural optimization of indeno[1,2-b]indole was performed and a new generation of 18 compounds was synthesized and tested as ABCG2 inhibitors. Most compounds showed ABCG2 inhibition with IC~50~ values below 0.5 μM. The ratio between cytotoxicity (IG~50~) and ABCG2 inhibition potency (IC~50~) was used to identify the best inhibitors. In addition, it was observed that some indeno[1,2-b]indole derivatives produced complete inhibition, while others only partially inhibited the transport function of ABCG2. All indeno[1,2-b]indole derivatives are not transported by ABCG2, and even the partial inhibitors are able to fully chemosensitize cancer cells overexpressing ABCG2. The high affinity of these indeno[1,2-b]indole derivatives was confirmed by the strong stimulatory effect on ABCG2 ATPase a

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Author

Kita, Diogo Henrique (author);Guragossian, Nathalie (author);Zattoni, Ingrid Fatima (author);Moure, Vivian Rotuno (author);Rego, Fabiane Gomes de Moraes (author);Lusvarghi, Sabrina (author);Moulenat, Thomas (author);Belhani, Billel (author);Picheth, Geraldo (author);Bouacida, Sofiane (author);Bouaziz, Zouhair (author);Marminon, Christelle (author);Berredjem, Malika (author);Jose, Joachim (author);Gonçalves, Marcos Brown (author);Ambudkar, Suresh V. (author);Valdameri, Glaucio (author);Le Borgne, Marc (author)

Publisher

Springer Science and Business Media LLC

Published

2021

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)