A novel 111indium-labeled dual carbonic anhydrase 9-targeted probe as a potential SPECT imaging radiotracer for detection of hypoxic colorectal cancer cells

Guan, Siao-Syun; Wu, Cheng-Tien; Liao, Tse-Zung; Lin, Kun-Liang; Peng, Cheng‐Liang; Shih, Ying-Hsia; Weng, Mao-Feng; Chen, Chun-Tang; Yeh, Chung-Hsin; Wang, Daqing; Liu, Shing‐Hwa

doi:10.1016/j.ejpb.2021.08.004

Cited by 5 publications

(2 citation statements)

References 56 publications

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“…The authors suggested that 34 has potential for further clinical applications. Recently, a new 111 In-labeled dual-CAIX-targeted probe containing a CA9tp peptide (NHVPLSP) and an AAZ moiety was reported [ 73 ]. AAZ-CA9tp showed high selectivity toward CAIX ( K d = 8.7 nM toward rhCA9; K d = 226.4 nM toward rhCA2) and possessed good CA9-targeting ability in hypoxic HCT15 cells ( K d = 6.17 nM).…”

Section: Small-molecule-based Compoundsmentioning

confidence: 99%

New Developments in Carbonic Anhydrase IX-Targeted Fluorescence and Nuclear Imaging Agents

Chen

Seimbille

2022

IJMS

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Carbonic anhydrase IX (CAIX) is a tumor-specific and hypoxia-induced biomarker for the molecular imaging of solid malignancies. The nuclear- and optical-imaging of CAIX-expressing tumors have received great attention due to their potential for clinical applications. Nuclear imaging is a powerful tool for the non-invasive diagnosis of primary and metastatic CAIX-positive tumors and for the assessment of responses to antineoplastic treatment. Intraoperative optical fluorescence imaging provides improved visualization for surgeons to increase the discrimination of tumor lesions, allowing for safer surgical treatment. Over the past decades, many CAIX-targeted molecular imaging probes, based on monoclonal antibodies, antibody fragments, peptides, and small molecules, have been reported. In this review, we outline the recent development of CAIX-targeted probes for single-photon emission computerized tomography (SPECT), positron emission tomography (PET), and near-infrared fluorescence imaging (NIRF), and we discuss issues yet to be addressed.

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Section: Small-molecule-based Compoundsmentioning

confidence: 99%

New Developments in Carbonic Anhydrase IX-Targeted Fluorescence and Nuclear Imaging Agents

Chen

Seimbille

2022

IJMS

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“…In addition, using CA IX as an imaging biomarker for hypoxia, a number of CA IX-targeted molecular imaging probes involving the conjugation of CA IX inhibitors (such as acetazolamide derivatives) with fluorescent optical reporters or radiotracers have also been developed to study tumor hypoxia. − Kulterer et al recently reported a Technetium-99m (Tc-99m) SPECT probe, 99m Tc-PHC-102, targeted to CA IX for imaging primary and metastatic renal cell carcinoma lesions. They conducted a microdosing study in patients and found 99m Tc-PHC-102 uptake in both primary tumors and metastases, demonstrating its potential to detect CA IX expression for identifying tumor lesions …”

Section: Introductionmentioning

confidence: 99%

Carbonic Anhydrase IX Targeting Mn(II)-Based Magnetic Resonance Molecular Imaging Probe for Hypoxia Tumors

et al. 2023

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Physiological hypoxic conditions in the tumor microenvironment and consequential overexpression of carbonic anhydrase IX (CA IX) are two characteristics shared by numerous types of solid malignant tumors. Early detection with hypoxia assessment is crucial to improve the prognosis and therapy outcomes of hypoxia tumors. Herein, using acetazolamide (AZA) as a CA IX-targeting moiety, we design and synthesize an Mn(II)-based MR imaging probe (named AZA-TA-Mn) incorporating AZA and two Mn(II) chelates of Mn-TyEDTA on a rigid triazine (TA) scaffold. The per Mn relaxivity of AZA-TA-Mn is 2-fold higher than its monomeric Mn-TyEDTA, which allows it for lowdose imaging of hypoxic tumors. In a xenograft mice model of esophageal squamous cell carcinoma (ESCC), a low dosage of AZA-TA-Mn (0.05 mmol/kg) can selectively produce prolonged and stronger contrast enhancement in the tumor compared to the non-specific Gd-DTPA (0.1 mmol/kg). A competition study of co-injection of free AZA and Mn(II) probes confirms the in vivo tumor selectivity of AZA-TA-Mn, resulting in a more than 2.5fold decreased tumor-to-muscle contrast-to-noise ratio (ΔCNR) at 60 min post-injection. MR imaging results were further supported by the quantitative analysis of Mn tissue levels, as the co-injection of free AZA resulted in significantly reduced Mn accumulation in tumor tissues. Finally, immunofluorescence staining of tissue sections confirms the positive correlation between the tumor accumulation of AZA-TA-Mn and CA IX overexpression. Hence, using CA IX as the hypoxia biomarker, our results illustrate a practical strategy for the development of novel imaging probes for hypoxic tumors.

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Develop companion radiopharmaceutical YKL40 antibodies as potential theranostic agents for epithelial ovarian cancer

Chang

Chiang

Kuo

et al. 2022

Biomedicine & Pharmacotherapy

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A novel 111indium-labeled dual carbonic anhydrase 9-targeted probe as a potential SPECT imaging radiotracer for detection of hypoxic colorectal cancer cells

Cited by 5 publications

References 56 publications

New Developments in Carbonic Anhydrase IX-Targeted Fluorescence and Nuclear Imaging Agents

New Developments in Carbonic Anhydrase IX-Targeted Fluorescence and Nuclear Imaging Agents

Carbonic Anhydrase IX Targeting Mn(II)-Based Magnetic Resonance Molecular Imaging Probe for Hypoxia Tumors

Develop companion radiopharmaceutical YKL40 antibodies as potential theranostic agents for epithelial ovarian cancer

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