Chemistry team

Chemistry group of iMIT

The chemistry lab of iMIT are focused on the development of novel molecular imaging tracers including radiopharmaceuticals and optical dye conjugated small molecules for the diagnosis and treatment of diseases. Not only medical radionuclide 18F, 11C, 123I, 131I and 13N but also emerging radionuclide, such as 68Ga, 64Cu and 89Zr were used to synthesize PET radiotracers for imaging. Furthermore, we are aimed to develop novel imaging strategies to address un-met needs of clinic.

 

Members

Kim, Dong-Yeon, Ph.D. (Assistant professor)

  • • Development and preclinical evaluation of radiopharmaceuticals
  • • Email address: blueburr@gmail.com

    Pyo, Ayoung, Ph.D. (Post doctoral course)

  • • Organic synthesis and radioisotope labeling, Evaluation using small animals
  • • Email address: payjal@naver.com

    Jung, Ye-Rim (Researcher)

  • • Organic synthesis and radioisotope labeling, Evaluation using small animals
  • • Email address: daniel1356@naver.com
  • Research Interests

    Development of 18F labeled myocardial imaging agents

    18F-labeled phosphonium cations accumulate to a higher degree in cardiomyocytes than in normal cells because of the higher mitochondrial membrane potential (MMP) in cardiomyocytes. This type of mitochondrial voltage sensor would be useful to detect myocardial abnormalities because loss of MMP is an early event in cell death caused by myocardial ischemia. Thus we developed several kinds of 18F-labeled phosphonium cations and reported in vivo characteristics.

    Development of 18F labeled tracers to visualize malignant melanoma

    Malignant melanoma is one of the most lethal cancers because of its high systemic metastatic potential. Benzamide derivatives are known as to have selective affinities with melanin and, over the past 2 decades, have been extensively investigated for development of SPECT agents for melanoma detection. Thus we modified structure of bezamide and labeled radionuclide 18F to develop novel PET tracer to visualize malignant melanoma.

    Development of optimized synthetic module for routine [11C]acetate production

    [11C]Acetate is quickly metabolized into acetyl-CoA in human cells and can enter the tricarboxylic acid cycle to participate in cell membrane lipid synthesis in tumor cells. Thus, [11C]acetate, a radiotracer for PET imaging, is under investigation for use in a number of cancers. we developed the optimized synthetic module and proved its high reproducibility and simplicity, with high radio chemical yield for routine clinical use.

    Development of 64Cu labeled artificial protein binders

    Longer half-life (12.7 h) of 64Cu among positron emitters allows for imaging at later time points than 18F (half-life, 109.7 min) and is more appropriate for imaging of protein binders. Thus we optimized 64Cu labeling methods using 3 kinds of chelators (NOTA, DOTA, DTPA) and reported in vivo characteristics of artificial protein binder (repebody) which have high affinity for the epidermal growth factor receptor (EGFR).

    Publications (2012-present)

    1.
    64Cu-Labeled Repebody Molecules for Imaging of Epidermal Growth Factor Receptor Expressing Tumors. J Nucl Med. 2017. Article in Press (2016 IF: 6.646)
    2.
    Small bowel metastasis from hepatocellular carcinoma detected by F-18 FDG PET/CT but not by C-11 acetate PET/CT. Clinical Nuclear Medicine. 2017 Article in Press (2016 IF: 4.563)
    3.
    Potential visualization of sorafenib-induced acidosis using 11C-acetate positron emission tomographycComputed Tomography in Patients with Hepatocellular Carcinoma. Clinical Nuclear Medicine. 2017 Article in Press (2016 IF: 4.563)
    4.
    Engineering of monobody conjugates for human EphA2-specific optical imaging. PLoS ONE. 2017 12(7): e0180786 (2016 IF: 2.806)
    5.
    Optimization of diagnostic performance for differentiation of recurrence from radiation necrosis in patients with metastatic brain tumors using tumor volume-corrected 11C-methionine uptake. EJNMMI Research. 2017; 7: 45 (2016 IF: 2.033)
    6.
    A high-affinity repebody for molecular imaging of EGFR-expressing malignant tumors. Theranostics. 2017; 7: 2620-2633 (2016 IF: 8.712)
    7.
    Comparative evaluation of the algorithms for parametric mapping of the novel myocardial PET imaging agent 18F-FPTP. Ann Nucl Med. 2017; 31: 469-479 (2016 IF: 1.396)
    8.
    Comparison of reconstruction methods in a small animal cardiac PET study using a 18F-labeled myocardial agent, [18F]FPTP. Iranian Journal of Radiology. 2017; 14(1)e26806 (2016 IF: 0.554)
    9.
    Prognostic value of post-treatment metabolic tumor volume from 11C-methionine PET/CT in recurrent malignant glioma. Neurosurg Rev. 2017; 40: 223-229 (2016 IF: 2.060)
    10.
    RGD Peptide Cell-Surface Display Enhances the Targeting and Therapeutic Efficacy of Attenuated Salmonella-mediated Cancer Therapy. Theranostics. 2016; 6; 1672-1682 (2016 IF: 8.712)
    11.
    Radiolabeled Phosphonium Salts as Mitochondrial Voltage Sensors for Positron Emission Tomography Myocardial Imaging Agents. Nucl Med Mol Imaging. 2016; 50; 185-195
    12.
    Comparison of 18F-labeled fluoroalkylphosphonium cations with 13N-NH3 for PET myocardial perfusion imaging. J Nucl Med. 2015; 56; 1581-1586 (2016 IF: 6.646)
    13.
    Isolation and characterization of a monobody with a fibronectin domain III scaffold that specifically binds EphA2. PLoS ONE. 2015 10(7): e0132976 (2016 IF: 2.806)
    14.
    Radiosynthesis and evaluation of 18F-labeled aliphatic phosphonium cations as a myocardial imaging agent for positron emission tomography. Nuclear Medicine Communications. 2015; 36; 747-754 (2016 IF: 1.472)
    15.
    Synthesis and evaluation of 18F-labeled fluoroalkyl triphenylphosphonium salts as mitochondrial voltage sensors in PET myocardial imaging. Methods in Molecular Biology. 2015; 1265; 59-72
    16.
    Synthesis and evaluation of 18F-labeled pyrido[3,2-b]pyrazine derivative as a potential imaging agent for non-small-cell lung cancer. Bulletin of the Korean Chemical Society. 2015 ; 36 ;1778-1783 (2016 IF: 0.602)
    17.
    In-house development of an optimized synthetic module for routine [11C]acetate production. Nuclear Medicine Communications. 2015; 36; 102–106 (2016 IF: 1.472)
    18.
    Dong-Yeon Kim*, Hyeon Sik Kim*, Hwa Youn Jang, Ju Han Kim, Hee-Seung Bom, and Jung-Joon Min. Comparison of the cardiac microPET images obtained using [18F]FPTP and [13N]NH3 in rat myocardial infarction. ACS Med. Chem. Lett. 2014; 5; 1124-1128 (2016 IF: 3.746)
    19.
    Development of the [11C] Acetate Synthesis Module. Journal of the Korean Physical Society. 2013; 63(7); 1390-1394 (2016 IF: 0.467)
    20.
    Evaluation of a mitochondrial voltage sensor, (18F-fluoropentyl)triphenylphosphonium cation, in a rat myocardial infarction model. J. Nucl. Med. 2012; 53:1779-1785 (2016 IF: 6.646)
    21.
    Synthesis of [18F]-labeled (2-(2-fluoroethoxy)ethyl)tris(4-methoxyphenyl)phosphonium cation as a potential agent for positron emission tomography myocardial imaging. Nuclear Medicine and Biology. 2012; 39; 1093–1098 (2016 IF: 2.426)
    22.
    Synthesis of [18F]-labeled (6-fluorohexyl)triphenylphosphonium cation as a potential agent for myocardial imaging using positron emission tomography. Bioconjugate Chem. 2012; 23; 431-437. (2016 IF: 4.818)
    23.
    Synthesis of [18F]-labeled (2-(2-fluoroethoxy)ethyl)triphenylphosphonium cation as a potential agent for myocardial imaging using positron emission tomography. Bioorg. Med. Chem. Lett. 2012; 22; 319–322. (2016 IF: 2.454)
    24.
    Synthesis and characterization of a 68Ga-labeled N-(2-diethylaminoethyl)benzamide derivative as potential PET Probe for malignant melanoma. Bioorg. Med. Chem. 2012; 20; 4915–4920. (2016 IF: 2.930)
    25.
    Synthesis and evaluation of a novel 68Ga-labeled DOTA-benzamide derivative for malignant melanoma imaging. Bioorg. Med. Chem. Lett. 2012; 22; 5288–5292 (2016 IF: 2.454)

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