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Chen Y, Sajjad M, Wang Y, et al. TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT. ACS Med Chem Lett. 2010;2(2):136-41doi: 10.1021/ml100211g.
Chen, Y., Sajjad, M., Wang, Y., Batt, C., Nabi, H. A., & Pandey, R. K. (2011). TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT. ACS medicinal chemistry letters, 2(2), 136-41. https://doi.org/10.1021/ml100211g
Chen, Yihui, et al. "TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT." ACS medicinal chemistry letters vol. 2,2 (2011): 136-41. doi: https://doi.org/10.1021/ml100211g
Chen Y, Sajjad M, Wang Y, Batt C, Nabi HA, Pandey RK. TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT. ACS Med Chem Lett. 2010 Nov 23;2(2):136-41. doi: 10.1021/ml100211g. eCollection 2011 Feb 10. PMID: 24900292; PMCID: PMC4018113.
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ACS Med Chem Lett. 2010 Nov 23;2(2):136-41. doi: 10.1021/ml100211g. eCollection 2011 Feb 10.

TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT.

ACS medicinal chemistry letters

Yihui Chen, Munawwar Sajjad, Yanfang Wang, Carrie Batt, Hani A Nabi, Ravindra K Pandey

Affiliations

  1. PDT Center, Roswell Park Cancer Institute, Buffalo, New York 14263, United States ; Department of Nuclear Medicine, State University of New York, Buffalo, New York 14214, United States.
  2. Department of Nuclear Medicine, State University of New York, Buffalo, New York 14214, United States.
  3. PDT Center, Roswell Park Cancer Institute, Buffalo, New York 14263, United States.

PMID: 24900292 PMCID: PMC4018113 DOI: 10.1021/ml100211g

Abstract

Translocator protein (TSPO) 18 kDa overexpression has been observed in a large variety of human cancers, especially breast cancers. PK 11195, an isoquinoline analogue, is one of the ligands of highest TSPO binding affinity. Due to the long biological half life of our photosensitizers, there is a need to label them with a long lived radioisotope, for example I-124. Our objectives are to find translocator protein targeted photosensitizers for both tumor imaging (PET) and photodynamic therapy (PDT). I-PK 11195 is conjugated with the tumor avid photosensitizer HPPH. We find that those two tumor avid components complement each other and make the conjugate molecule even more tumor avid; compared to the photosensitizer itself, the conjugate is found to show improved PDT efficacy. It is concluded that I-PK 11195 can be a good vehicle to deliver radionuclide and photosensitizer to TSPO overexpressed tumor regions. Such conjugates could be useful for both tumor imaging (PET) and PDT.

Keywords: PK 11195; Photodynamic therapy (PDT); cancer target specific; peripheral benzodiazepine receptor (PBR); positron emission tomography (PET); translocator protein (TSPO)

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