Targeting gastrin-releasing peptide receptors of prostate cancer cells for photodynamic therapy with a phthalocyanine-bombesin conjugate.
Bioorg Med Chem Lett
; 18(7): 2424-7, 2008 Apr 01.
Article
en En
| MEDLINE
| ID: mdl-18329268
ABSTRACT
Sulfonated aluminum phthalocyanines (AlPcS) are potent photosensitizers for the photodynamic therapy (PDT) of cancer. In this study we evaluate the possibility to improve the efficacy of AlPcS-PDT for prostate cancer by targeting tetrasulfonated aluminum phthalocyanines (AlPcS(4)) to the gastrin-releasing peptide receptor (GRPR) through coupling to bombesin. A mono-carbohexyl derivative of AlPcS(4) is attached to 8-Aoc-bombesin(7-14)NH(2) via an amide bridge to yield a bombesin-AlPcS(4) conjugate linked by a C-14 spacer chain. The conjugate is characterized by mass spectroscopy and shown to bind to the GRPR with a relative binding affinity (RBA) of 2.3, taking bombesin (RBA=100) as unity. The in vitro photodynamic efficacy of the conjugate against PC-3 human prostate cancer cells is improved by a factor 2.5 over the non-conjugated mono-carbohexyl derivative of AlPcS(4).
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Compuestos Organometálicos
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Fotoquimioterapia
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Neoplasias de la Próstata
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Bombesina
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Sistemas de Liberación de Medicamentos
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Fármacos Fotosensibilizantes
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Receptores de Bombesina
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Indoles
Límite:
Humans
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Male
Idioma:
En
Año:
2008
Tipo del documento:
Article