Design and synthesis of a novel BODIPY-labeled PSMA inhibitor.
Bioorg Med Chem Lett
; 30(3): 126894, 2020 02 01.
Article
em En
| MEDLINE
| ID: mdl-31874825
ABSTRACT
Prostate-specific membrane antigen (PSMA) is a zinc-bound metalloprotease which is highly expressed in metastatic prostate cancer. It has been considered an excellent target protein for prostate cancer imaging and targeted therapy because it is a membrane protein and its active site is located in the extracellular region. We successfully synthesized and evaluated a novel PSMA ligand conjugated with BODIPY650/665. Compound 1 showed strong PSMA-inhibitory activity and selective uptake into PSMA-expressing tumors. Compound 1 has the potential to be utilized as a near infrared (NIR) optical imaging probe targeting PSMA-expressing cancers.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos de Boro
/
Desenho de Fármacos
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Glutamato Carboxipeptidase II
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Corantes Fluorescentes
Limite:
Animals
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Humans
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Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2020
Tipo de documento:
Article