Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX.


Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 03 2019
Historique:
received: 19 10 2018
revised: 12 01 2019
accepted: 16 01 2019
pubmed: 27 1 2019
medline: 15 1 2020
entrez: 27 1 2019
Statut: ppublish

Résumé

Carbonic anhydrase IX (CA IX) is the first carbonic anhydrase found to be associated with cancer that is over-expressed in a variety of human solid tumors. As a surrogate marker for hypoxia, the expression of CA IX is strongly upregulated in hypoxic tumors by hypoxia and hypoxia-inducible factor 1a (HIF-1a). In our pursuit of a CA IX-specific PET probe, we designed and synthesized a peptide-based CA IX imaging probe by the efficient click reaction of 1,3-dipolar cycloaddition of terminal alkynes and organic azides. The probe

Identifiants

pubmed: 30683555
pii: S0968-0896(18)31659-6
doi: 10.1016/j.bmc.2019.01.014
pii:
doi:

Substances chimiques

Antigens, Neoplasm 0
Biomarkers, Tumor 0
Fluorine Radioisotopes 0
Peptides 0
Radiopharmaceuticals 0
Triazoles 0
CA9 protein, human EC 4.2.1.1
Carbonic Anhydrase IX EC 4.2.1.1
Fluorine-18 GZ5I74KB8G

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

785-789

Informations de copyright

Copyright © 2019 Elsevier Ltd. All rights reserved.

Auteurs

Lina Jia (L)

Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China.

Xiao Li (X)

Department of Nuclear Medicine, Changhai Hospital, Shanghai 200433, China.

Dengfeng Cheng (D)

Zhongshan Hospital, Fudan University, Shanghai 200032, China.

Lan Zhang (L)

Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China. Electronic address: zhanglan@sinap.ac.cn.

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Classifications MeSH