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. Author manuscript; available in PMC: 2022 May 19.
Published in final edited form as: J Am Chem Soc. 2021 May 10;143(19):7380–7387. doi: 10.1021/jacs.1c00451

Figure 2.

Figure 2.

Folate-ARV-771 degrades BRD4 in a FOLR1-dependent manner. (A) Western blot analysis of BRD4 level in HeLa cells after treatment with the indicated doses of free folic acid with either 30 nM folate-ARV-771 or ARV-771 for 12 h. (B) Cell viability of HeLa cells treated with folate-ARV-771 with or without free folic acid for 72 h. (C) HeLa cells with or without knockdown of endogenous FOLR1 were treated with folate-ARV-771 for 2 h, and then the levels of BRD4 were determined by Western blot. (D) Western blot analysis of basal BRDs and FOLR1/2 levels in a panel of BRCA cell lines and the noncancerous normal breast epithelial MCF10A cells. (E) Western blot analysis of BRD4 level in BRCA cell lines with either high FOLR1 expression (ZR-75-1, SK-BR-3, and AU565) or low FOLR1 expression levels (BT549 and MDA-MB-231) or noncancerous normal breast epithelial MCF10A cells after treatment with folate-ARV-771 for 12 h.