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Design and synthesis of a novel BODIPY-labeled PSMA inhibitor.
Son, Sang-Hyun; Kwon, Hongmok; Ahn, Hye-Hyun; Nam, Hwanhee; Kim, Kyul; Nam, SangJin; Choi, Doyoung; Ha, Hyunsoo; Minn, Il; Byun, Youngjoo.
Afiliação
  • Son SH; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • Kwon H; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • Ahn HH; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD 21287, United States.
  • Nam H; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD 21287, United States; Institute for NanoBioTechnology, Johns Hopkins University, Baltimore, MD 21287, United States.
  • Kim K; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • Nam S; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • Choi D; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • Ha H; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea.
  • Minn I; Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University, Baltimore, MD 21287, United States; Institute for NanoBioTechnology, Johns Hopkins University, Baltimore, MD 21287, United States. Electronic address: iminn1@jhmi.edu.
  • Byun Y; College of Pharmacy, Korea University, 2511 Sejong-ro, Sejong 30019, Republic of Korea; Biomedical Research Center, Korea University Guro Hospital, 148 Gurodong-ro, Guro-gu, Seoul 08308, Republic of Korea. Electronic address: yjbyun1@korea.ac.kr.
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 / Glutamato Carboxipeptidase II / Corantes Fluorescentes Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2020 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Boro / Desenho de Fármacos / Glutamato Carboxipeptidase II / Corantes Fluorescentes Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2020 Tipo de documento: Article