An atom-economical design of PET tracer for imaging αvβ3 integrin via utilizing the three-in-one function of 64Copper

Jing Yang; Jian Yang; Huan Wang; Junfeng Wang; Jianping Xiong; Chunhua Qiao; Chongzhao Ran

doi:10.1039/C9CC08690K

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An atom-economical design of PET tracer for imaging α_vβ₃ integrin via utilizing the three-in-one function of ⁶⁴Copper†

Jing Yang,‡^ab Jian Yang,

‡^ac Huan Wang,^a Junfeng Wang,^d Jianping Xiong,^e Chunhua Qiao

^b and Chongzhao Ran

*^a

Author affiliations

* Corresponding authors

^a Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Boston, MA, China
E-mail: cran@nmr.mgh.harvard.edu

^b College of Pharmaceutical Sciences, Soochow University, Suzhou, China

^c School of Pharmacy, China Pharmaceutical University, Nanjing, China

^d Gorden Center for Medical Imaging, Massachusetts General Hospital and Harvard Medical School, Boston, MA, China

^e Program in Structural Biology, Nephrology Division, Massachusetts General Hospital and Harvard Medical School, Boston, MA, China

Abstract

In this study, α_vβ₃ integrin in U87 tumor cells was imaged with a ⁶⁴Cu-peptidic probe, in which the linear peptide GHRGDHG is used as a pre-ligand, while ⁶⁴Cu bears three functional roles that include generation of the PET signal, coordination with two GH moieties of the pre-ligand, and cyclizing the linear pre-ligand into an active cyclic-RGD form (termed as ⁶⁴Cu-Cyclo-RGD) for α_vβ₃ integrin.

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Article information

DOI: https://doi.org/10.1039/C9CC08690K
Article type: Communication
Submitted: 06 Nov 2019
Accepted: 07 Jan 2020
First published: 10 Jan 2020

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Chem. Commun., 2020,56, 1788-1791

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An atom-economical design of PET tracer for imaging α_vβ₃ integrin via utilizing the three-in-one function of ⁶⁴Copper

J. Yang, J. Yang, H. Wang, J. Wang, J. Xiong, C. Qiao and C. Ran, Chem. Commun., 2020, 56, 1788 DOI: 10.1039/C9CC08690K

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