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Gene Review

Tspo  -  translocator protein

Mus musculus

Synonyms: Bzrp, IBP, Mbr, Mitochondrial benzodiazepine receptor, PBR, ...
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Disease relevance of Tspo

  • Ocular development was highly sensitive to periods of hypoxia through a mechanism blocked with the potent Bzrp ligand PK11195 [1].
  • In search of a PBR functional antagonist that would facilitate the studies on the biological function of PBR, we screened a phage display library [2].
  • Cholesterol binding at the cholesterol recognition/ interaction amino acid consensus (CRAC) of the peripheral-type benzodiazepine receptor and inhibition of steroidogenesis by an HIV TAT-CRAC peptide [3].
  • PBR was also found to be expressed at high levels in aggressive metastatic human breast tumor biopsies compared with normal breast tissues [4].
  • Increased PBR levels were associated with the degree of demyelination and temporal activation of glial cell types in different anatomical regions [5].

Psychiatry related information on Tspo

  • Acute, maximal electroshock (MES) increased the density of PBR in mouse cerebral cortex as evidenced by a 30% increase in the Bmax of this archetypic ligand [6].

High impact information on Tspo

  • [(3)H]Promegestone photoincorporated into recombinant PBR, and this labeling was displaced by cholesterol [3].
  • The normal functional state of mitochondria was restored with PK11195, a specific ligand of the mitochondrial peripheral-type benzodiazepine receptor [7].
  • In addition, the PBR-dependent MDA-231 cell proliferation was found to highly correlate (r = -0.99) with the PBR-mediated changes in nuclear membrane cholesterol levels [4].
  • Subcellular localization with both antibodies and a fluorescent PBR drug ligand revealed that PBR from the MDA-231 cell line as well as from aggressive metastatic human breast tumor biopsies localized primarily in and around the nucleus [4].
  • In this study, we examined the expression, characteristics, localization, and function of PBR in a battery of human breast cancer cell lines differing in their invasive and chemotactic potential as well as in several human tissue biopsies [4].

Chemical compound and disease context of Tspo


Biological context of Tspo


Anatomical context of Tspo


Associations of Tspo with chemical compounds


Physical interactions of Tspo

  • Deletion of the C-terminal domain of PBR and mutation of the highly conserved among all PBR amino acid sequences Y152 of the CRAC domain resulted in loss of the ability of mutant recPBR to bind cholesterol [17].
  • These results provide strong evidence that PBR is not a single protein receptor but a multimeric complex in which the IQ binding site is on the M(r) 18,000 subunit and expression of the BZ binding site requires both the M(r) 18,000 and 34,000 voltage-dependent anion channel subunits [18].

Other interactions of Tspo


Analytical, diagnostic and therapeutic context of Tspo

  • CONCLUSION: This is the first study to demonstrate that functional antagonism of coexpressed Bcl-X(L) and Mcl-1 proteins using the mBzR antagonist Pk11195 can facilitate apoptosis in cholangiocarcinoma following chemotherapy and radiotherapy [21].
  • Pyropheophorbides and their metal complexes were synthesized to investigate their applications as nonradioactive peripheral benzodiazepine receptor (PBR) binding probes and photosensitizers for use in photodynamic therapy [22].
  • Next, the distribution of PBR in MA-10 Leydig cells was further examined using confocal microscopy [20].
  • First, PBR was immunolocalized in the rat testis using biotin-streptavidin peroxidase immunocytochemistry, and results revealed that PBR was present exclusively in the interstitial Leydig cells [20].
  • To develop a positron emission tomography (PET) ligand for imaging the 'peripheral benzodiazepine receptor' (PBR) in brain and elucidating the relationship between PBR and brain diseases, four analogues (4-7) of N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide (2) were synthesized and evaluated as ligands for PBR [23].


  1. Mitochondrial benzodiazepine receptors regulate oxygen homeostasis in the early mouse embryo. O'Hara, M.F., Nibbio, B.J., Craig, R.C., Nemeth, K.R., Charlap, J.H., Knudsen, T.B. Reprod. Toxicol. (2003) [Pubmed]
  2. PBR, StAR, and PKA: partners in cholesterol transport in steroidogenic cells. Hauet, T., Liu, J., Li, H., Gazouli, M., Culty, M., Papadopoulos, V. Endocr. Res. (2002) [Pubmed]
  3. Cholesterol binding at the cholesterol recognition/ interaction amino acid consensus (CRAC) of the peripheral-type benzodiazepine receptor and inhibition of steroidogenesis by an HIV TAT-CRAC peptide. Li, H., Yao, Z., Degenhardt, B., Teper, G., Papadopoulos, V. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  4. Peripheral-type benzodiazepine receptor (PBR) in human breast cancer: correlation of breast cancer cell aggressive phenotype with PBR expression, nuclear localization, and PBR-mediated cell proliferation and nuclear transport of cholesterol. Hardwick, M., Fertikh, D., Culty, M., Li, H., Vidic, B., Papadopoulos, V. Cancer Res. (1999) [Pubmed]
  5. Peripheral benzodiazepine receptor imaging in CNS demyelination: functional implications of anatomical and cellular localization. Chen, M.K., Baidoo, K., Verina, T., Guilarte, T.R. Brain (2004) [Pubmed]
  6. Maximal electroshock increases the density of [3H]Ro 5-4864 binding to mouse cerebral cortex. Basile, A.S., Weissman, B.A., Skolnick, P. Brain Res. Bull. (1987) [Pubmed]
  7. Direct influence of the p53 tumor suppressor on mitochondrial biogenesis and function. Donahue, R.J., Razmara, M., Hoek, J.B., Knudsen, T.B. FASEB J. (2001) [Pubmed]
  8. Antiproliferative and differentiating effects of benzodiazepine receptor ligands on B16 melanoma cells. Landau, M., Weizman, A., Zoref-Shani, E., Beery, E., Wasseman, L., Landau, O., Gavish, M., Brenner, S., Nordenberg, J. Biochem. Pharmacol. (1998) [Pubmed]
  9. Identification of a peptide antagonist to the peripheral-type benzodiazepine receptor that inhibits hormone-stimulated leydig cell steroid formation. Gazouli, M., Han, Z., Papadopoulos, V. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  10. Ligands of the peripheral benzodiazepine receptor have therapeutic effects in pneumopathies in vivo. Bribes, E., Bourrie, B., Casellas, P. Immunol. Lett. (2003) [Pubmed]
  11. Peripheral-type benzodiazepine receptors in association with epileptic seizures in EL mice. Nakamoto, Y., Watabe, S., Shiotani, T., Yoshii, M. Brain Res. (1996) [Pubmed]
  12. Differential utilization of the promoter of peripheral-type benzodiazepine receptor by steroidogenic versus nonsteroidogenic cell lines and the role of Sp1 and Sp3 in the regulation of basal activity. Giatzakis, C., Papadopoulos, V. Endocrinology (2004) [Pubmed]
  13. Regulation of steroid hormone biosynthesis in R2C and MA-10 Leydig tumor cells: role of the cholesterol transfer proteins StAR and PBR. Rao, R.M., Jo, Y., Babb-Tarbox, M., Syapin, P.J., Stocco, D.M. Endocr. Res. (2002) [Pubmed]
  14. Peripheral-type benzodiazepine receptor-mediated action of steroidogenic acute regulatory protein on cholesterol entry into leydig cell mitochondria. Hauet, T., Yao, Z.X., Bose, H.S., Wall, C.T., Han, Z., Li, W., Hales, D.B., Miller, W.L., Culty, M., Papadopoulos, V. Mol. Endocrinol. (2005) [Pubmed]
  15. The peroxisome proliferator perfluorodecanoic acid inhibits the peripheral-type benzodiazepine receptor (PBR) expression and hormone-stimulated mitochondrial cholesterol transport and steroid formation in Leydig cells. Boujrad, N., Vidic, B., Gazouli, M., Culty, M., Papadopoulos, V. Endocrinology (2000) [Pubmed]
  16. Induction of peripheral-type benzodiazepine receptors during differentiation of mouse erythroleukemia cells. A possible involvement of these receptors in heme biosynthesis. Taketani, S., Kohno, H., Okuda, M., Furukawa, T., Tokunaga, R. J. Biol. Chem. (1994) [Pubmed]
  17. Characterization of the cholesterol recognition amino acid consensus sequence of the peripheral-type benzodiazepine receptor. Jamin, N., Neumann, J.M., Ostuni, M.A., Vu, T.K., Yao, Z.X., Murail, S., Robert, J.C., Giatzakis, C., Papadopoulos, V., Lacapère, J.J. Mol. Endocrinol. (2005) [Pubmed]
  18. In vitro reconstitution of a functional peripheral-type benzodiazepine receptor from mouse Leydig tumor cells. Garnier, M., Dimchev, A.B., Boujrad, N., Price, J.M., Musto, N.A., Papadopoulos, V. Mol. Pharmacol. (1994) [Pubmed]
  19. PK11195, a ligand of the mitochondrial benzodiazepine receptor, facilitates the induction of apoptosis and reverses Bcl-2-mediated cytoprotection. Hirsch, T., Decaudin, D., Susin, S.A., Marchetti, P., Larochette, N., Resche-Rigon, M., Kroemer, G. Exp. Cell Res. (1998) [Pubmed]
  20. Diazepam binding inhibitor is a paracrine/autocrine regulator of Leydig cell proliferation and steroidogenesis: action via peripheral-type benzodiazepine receptor and independent mechanisms. Garnier, M., Boujrad, N., Oke, B.O., Brown, A.S., Riond, J., Ferrara, P., Shoyab, M., Suarez-Quian, C.A., Papadopoulos, V. Endocrinology (1993) [Pubmed]
  21. Pk11195, a mitochondrial benzodiazepine receptor antagonist, reduces apoptosis threshold in Bcl-X(L) and Mcl-1 expressing human cholangiocarcinoma cells. Okaro, A.C., Fennell, D.A., Corbo, M., Davidson, B.R., Cotter, F.E. Gut (2002) [Pubmed]
  22. Methyl pyropheophorbide-a analogues: potential fluorescent probes for the peripheral-type benzodiazepine receptor. Effect of central metal in photosensitizing efficacy. Chen, Y., Zheng, X., Dobhal, M.P., Gryshuk, A., Morgan, J., Dougherty, T.J., Oseroff, A., Pandey, R.K. J. Med. Chem. (2005) [Pubmed]
  23. Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain. Zhang, M.R., Maeda, J., Ogawa, M., Noguchi, J., Ito, T., Yoshida, Y., Okauchi, T., Obayashi, S., Suhara, T., Suzuki, K. J. Med. Chem. (2004) [Pubmed]
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