Peripheral benzodiazepine receptor and its clinical targeting.
Tumor cell targeted therapies, by induction or enhancement of apoptosis, constitute recent promising approaches achieving more specific anti-tumor efficacy. The peripheral benzodiazepine receptor (PBR), which belongs to the permeability transition pore (PTP), the central regulatory complex of apoptosis, is a potential target. A number of findings argue in favor of the development of PBR targeting approaches: (i) overexpression of PBR has been described in a large range of human cancers, (ii) PTP-mediated regulation of programmed cell death is an apoptotic-inducing factor-independent check-point that could be modulated by various conventional cancer therapies, and (iii) PBR ligation enhances apoptosis induction in many types of tumors and reverses Bcl-2 cytoprotective effects. Altogether, these observations support the use of PBR-directed drugs, particularly PBR ligands such as Ro5-4864, in the treatment of human cancers.
Decaudin
Didier
D
Department of Clinical Hematology, Institut Curie, Paris, France. didier.decaudin@curie.net
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D016503:Drug Delivery Systems / Q000379:methods* / Q000639:trends*; D005602:France; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000502:physiology
D000970:Antineoplastic Agents; D011963:Receptors, GABA-A