Preparation and Evaluation of ZD2 Peptide 64 Cu-DOTA Conjugate as a Positron Emission Tomography Probe for Detection and Characterization of Prostate Cancer

Zheng Han, Olga Sergeeva, Sarah Roelle, Han Cheng, Songqi Gao, Yajuan Li, Zhenghong Lee, Zheng Rong Lu

Research output: Contribution to journalArticle

Abstract

Positron emission tomography (PET) is a sensitive modality for cancer molecular imaging. We aim to develop a PET probe for sensitive detection and risk stratification of prostate cancer by targeting an abundant microenvironment oncoprotein, extradomain-B fibronectin (EDB-FN). The probe consists of a small ZD2 peptide specific to EDB-FN and a 64 Cu-DOTA chelate. The probe was synthesized using standard solid-phase peptide chemistry and chelated to 64 Cu prior to imaging. PET images were acquired at 4 and 22 h after intravenously injecting a 200 μCi probe into mice bearing human PC3 and LNCaP tumors, which represent highly aggressive and slow-growing prostate tumors, respectively. At 4 and 22 h postinjection, tumors could be clearly identified in the PET images. A significant higher signal was observed in PC3 tumors than in LNCaP tumors at 22 h (p = 0.01). Probe accumulation was also higher in PC3 tumors at 24 h. These data demonstrated that PET molecular imaging of EDB-FN in the tumor microenvironment of prostate cancer allows efficient differentiation of PC3 and LNCaP tumors in vivo. The ZD2 peptide-targeted PET probe shows potential in the detection and characterization of high-risk prostate cancer to improve the clinical management of prostate cancer.

Original languageEnglish (US)
Pages (from-to)1185-1190
Number of pages6
JournalACS Omega
Volume4
Issue number1
DOIs
StatePublished - Jan 14 2019

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Positron emission tomography
Peptides
Tumors
Fibronectins
Molecular imaging
Bearings (structural)
Oncogene Proteins
Imaging techniques

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

Cite this

Preparation and Evaluation of ZD2 Peptide 64 Cu-DOTA Conjugate as a Positron Emission Tomography Probe for Detection and Characterization of Prostate Cancer . / Han, Zheng; Sergeeva, Olga; Roelle, Sarah; Cheng, Han; Gao, Songqi; Li, Yajuan; Lee, Zhenghong; Lu, Zheng Rong.

In: ACS Omega, Vol. 4, No. 1, 14.01.2019, p. 1185-1190.

Research output: Contribution to journalArticle

Han, Zheng ; Sergeeva, Olga ; Roelle, Sarah ; Cheng, Han ; Gao, Songqi ; Li, Yajuan ; Lee, Zhenghong ; Lu, Zheng Rong. / Preparation and Evaluation of ZD2 Peptide 64 Cu-DOTA Conjugate as a Positron Emission Tomography Probe for Detection and Characterization of Prostate Cancer In: ACS Omega. 2019 ; Vol. 4, No. 1. pp. 1185-1190.
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abstract = "Positron emission tomography (PET) is a sensitive modality for cancer molecular imaging. We aim to develop a PET probe for sensitive detection and risk stratification of prostate cancer by targeting an abundant microenvironment oncoprotein, extradomain-B fibronectin (EDB-FN). The probe consists of a small ZD2 peptide specific to EDB-FN and a 64 Cu-DOTA chelate. The probe was synthesized using standard solid-phase peptide chemistry and chelated to 64 Cu prior to imaging. PET images were acquired at 4 and 22 h after intravenously injecting a 200 μCi probe into mice bearing human PC3 and LNCaP tumors, which represent highly aggressive and slow-growing prostate tumors, respectively. At 4 and 22 h postinjection, tumors could be clearly identified in the PET images. A significant higher signal was observed in PC3 tumors than in LNCaP tumors at 22 h (p = 0.01). Probe accumulation was also higher in PC3 tumors at 24 h. These data demonstrated that PET molecular imaging of EDB-FN in the tumor microenvironment of prostate cancer allows efficient differentiation of PC3 and LNCaP tumors in vivo. The ZD2 peptide-targeted PET probe shows potential in the detection and characterization of high-risk prostate cancer to improve the clinical management of prostate cancer.",
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