Uptake of radiolabeled morphiceptin and its analogs by experimental mammary adenocarcinoma: in vitro and in vivo studies.
Nucl Med Biol
; 31(4): 451-7, 2004 May.
Article
en En
| MEDLINE
| ID: mdl-15093815
ABSTRACT
Morphiceptin (Tyr-Pro-Phe-Pro-NH(2)) and its analogs modified at position 3 [D-Phe(3)]morphiceptin, [D-ClPhe(3)]morphiceptin and [D-Cl(2)Phe(3)]morphiceptin were synthesized and labeled with [(125)I] or [(131)I]. Their binding to membranes isolated from experimental adenocarcinoma was examined in vitro with the use of a cross-linking assay followed by the Western blot technique. The radioactive complex had molecular weight of about 65 kDa and was detectable by anti-mu-opioid receptor polyclonal antibody. Expression of the mu-opioid receptor in mouse mammary adenocarcinoma was confirmed by reverse transcriptase-polymerase chain reaction. The binding studies showed the highest affinity and capacity for [D-Phe(3)]morphiceptin (K(d) 0.39 and B(max) 1112) and [D-ClPhe(3)]morphiceptin (K(d) 1.8 and B(max) 220). Morphiceptin and its D-Cl(2)Phe analog had significantly lower B(max) values (131 and 83, respectively). Biodistribution experiments in tumor-bearing C3H/Bi mice with the use of the (131)I-labeled peptides confirmed the results of our in vitro studies. The highest accumulation of radioactive peptides in the tumor tissue was also found for peptides with D-Phe and D-ClPhe.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Endorfinas
/
Adenocarcinoma
/
Receptores Opioides mu
/
Radioisótopos de Yodo
/
Neoplasias Mamarias Experimentales
Tipo de estudio:
Evaluation_studies
Límite:
Animals
Idioma:
En
Revista:
Nucl Med Biol
Asunto de la revista:
BIOLOGIA
/
MEDICINA NUCLEAR
Año:
2004
Tipo del documento:
Article
País de afiliación:
Polonia