PK11195, a peripheral benzodiazepine receptor ligand, chemosensitizes acute myeloid leukemia cells to relevant therapeutic agents by more than one mechanism
DE Banker, JJ Cooper, DA Fennell, CL Willman… - Leukemia research, 2002 - Elsevier
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 …
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 …
