title: Reversal effects of Raloxifene on paclitaxel resistance in 2 MDR breast cancer cells.
abstract: Raloxifene hydrochloride (RAL), one of second generation of selective estrogen receptor modulators (SERMs), is usually used in preventing osteoporosis and breast cancer. The present study evaluated whether Raloxifene might sensitize multidrug resistant (MDR) breast cancers to chemotherapies, especially in estrogen receptor negative (ER-) breast cancer. The results showed that RAL could significantly sensitize ER- MDR breast tumors to paclitaxel both in vitro and in vivo. Combination of Raloxifene could significantly enhance paclitaxel-induced cell apoptosis, G2-M arrest as well as inhibition of cell proliferation in MDR tumors. Further studies showed that the combined treatment did not alter P-glycoprotein expression but increased P-gp ATPase activity. These results suggested that raloxifene might be a valuable chemosensitizer agent for breast cancer therapy.
authors.affiliation: a Program of Innovative Cancer Therapeutics; Department of Surgery.|b Clinical Research Center; First Affiliated Hospital of Zhejiang University School of Medicine ; Hangzhou , China.
authors.forename: Liang
authors.initials: L
authors.lastname: Xu
authors.affiliation: a Program of Innovative Cancer Therapeutics; Department of Surgery.
authors.forename: Jingyu
authors.initials: J
authors.lastname: Lei
authors.affiliation: a Program of Innovative Cancer Therapeutics; Department of Surgery.
authors.forename: Donghai
authors.initials: D
authors.lastname: Jiang
authors.affiliation: a Program of Innovative Cancer Therapeutics; Department of Surgery.
authors.forename: Lin
authors.initials: L
authors.lastname: Zhou
authors.affiliation: a Program of Innovative Cancer Therapeutics; Department of Surgery.|c Department of Biological Sciences ; National University of Singapore ; Singapore.
authors.forename: Shu
authors.initials: S
authors.lastname: Wang
authors.affiliation: a Program of Innovative Cancer Therapeutics; Department of Surgery.|d Department of Pathology and Laboratory Medicine ; Medical University of South Carolina ; SC , USA.
authors.forename: Weimin
authors.initials: W
authors.lastname: Fan
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics*; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D050071:Bone Density Conservation Agents / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000235:genetics / Q000378:metabolism; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056744:Cyclin B1 / Q000378:metabolism; D019008:Drug Resistance, Neoplasm / Q000235:genetics*; D005260:Female; D006801:Humans; D008938:Mitosis / Q000187:drug effects; D017239:Paclitaxel / Q000494:pharmacology*; D010766:Phosphorylation; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D020849:Raloxifene Hydrochloride / Q000494:pharmacology*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000972:Antineoplastic Agents, Phytogenic; D050071:Bone Density Conservation Agents; D056744:Cyclin B1; D019253:Proto-Oncogene Proteins c-bcl-2; D020849:Raloxifene Hydrochloride; D017239:Paclitaxel
keywords: breast cancer; multidrug resistance; paclitaxel; raloxifene