title: Priming BCL-2 to kill: the combination therapy of tamoxifen and ABT-199 in ER+ breast cancer.
abstract: The B-cell lymphoma/leukemia 2 protein (BCL-2) may help many types of cancers to evade cell death. However, identifying exactly where this is the case is a challenge. ABT-199 is a small molecule that selectively inhibits BCL-2, which is currently in clinical trials in lymphoid malignancies. While inhibiting BCL-2 by itself can cause cell death in hematopoietic tumors, single-agent activity is harder to observe in solid tumors. Combining ABT-199 with tamoxifen, the standard endocrine therapy for estrogen receptor-positive breast cancers, 85% of which have BCL-2 expression, represents a new strategy to prime cancer cells for apoptosis and elicit better cancer cell death responses.
authors.forename: Jing
authors.initials: J
authors.lastname: Deng
authors.forename: Anthony
authors.initials: A
authors.lastname: Letai
mesh_terms: D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology*; D005260:Female; D006801:Humans; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors*; D011960:Receptors, Estrogen / Q000032:analysis*; D013449:Sulfonamides / Q000494:pharmacology*
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D019253:Proto-Oncogene Proteins c-bcl-2; D011960:Receptors, Estrogen; D013449:Sulfonamides