@article{4cbb1af7c8e04ded89d9312858aa7949,
title = "PK11195, a peripheral benzodiazepine receptor ligand, chemosensitizes acute myeloid leukemia cells to relevant therapeutic agents by more than one mechanism",
abstract = "Like Bcl-2, peripheral benzodiazepine receptors (pBzRs) reside in mitochondrial pores, are frequently over-expressed in tumor cells, and can protect cells from apoptotic cell death. We now show that the high-affinity, pBzR-specific ligand, PK11195, chemosensitizes AML cells to relevant chemotherapeutics, but is relatively non-toxic as a single agent, and does not chemosensitize normal myeloid cells. PK11195 can block p-glycoprotein efflux in AMLs, contributing to increased daunomycin toxicity in efflux-competent AMLs, but can also sensitize AMLs to cytarabine and DNR-sensitize efflux-incompetent AMLs, presumably via mitochondrial pore effects documented in other models. Therefore, PK11195 might contribute to improved clinical outcomes in AML.",
keywords = "Apoptosis, Chemotherapy, Cytarabine, Daunorubicin, MDR",
author = "Banker, {Deborah E.} and Cooper, {John J.} and Fennell, {Dean A.} and Willman, {Cheryl L.} and Appelbaum, {Frederick R.} and Cotter, {Finbarr E.}",
note = "Funding Information: Supported by the Leukemia and Lymphoma Society (DEB, JJC). The Medical Research Council (DAF), NIH grants UO1-CA32102 supporting the Southwest Oncology Group (CLW) and CA 18029 (FRA), and the Leukemia Research Fund (FEC). D.E. Banker provided the concept and design, collected the data as well as data analysis and interpretation, drafted the manuscript, and obtained the necessary funding. J.J. Cooper provided technical support, collected data, and gave final approval. D.A. Fennell contributed to the concept and design and gave final approval. C.L. Willman provided study materials and gave final approval. F.R. Appelbaum contributed to the revision as well as giving final approval. F.E. Cotter contributed to the study design and gave final approval. ",
year = "2002",
doi = "10.1016/S0145-2126(01)00112-6",
language = "English (US)",
volume = "26",
pages = "91--106",
journal = "Leukemia Research",
issn = "0145-2126",
publisher = "Elsevier Limited",
number = "1",
}