کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371194 981839 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Development of anti-EGF receptor peptidomimetics (AERP) as tumor imaging agent
چکیده انگلیسی

EGFR is over-expressed in several solid tumors including breast, prostate, pancreas, and lung cancers and is correlated to the metastasic potential of the tumor. Anti-EGFR receptor-binding peptidomimetics (AERP) were examined to assess the small molecule’s potential use as tumor-specific imaging agents. The aim of this work was to design and characterize the binding specificity of the radiolabeled peptidomimetics to EGFR over-expressing cell lysate and to A431 xenograft tumors. Our newly designed peptidomimetic, AERP, was conjugated to DTPA and labeled with 99mTc. The in vivo tumor accumulation of [99mTc] DTPA-AERP-2 was 1.6 ± 0.1 %ID/g and tumor to muscle ratio was 5.5. Our studies suggest that this novel peptidomimetic, AERP-2, warrants further development as an EGFR specific tumor-imaging agent.

In certain human cancers, EGFR is over-expressed and is related to the metastasic potential of the tumor. We have developed two anti-EGFR receptor-binding peptidomimetics (AERP), as tumor-specific imaging agents. Our newly designed peptidomimetic, AERP, was conjugated to DTPA and labeled with 99mTc. The in vivo tumor accumulation of [99mTc] DTPA-AERP-2 was 1.6 ± 0.1 %ID/g and tumor to muscle ratio was 5.5.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 8, 15 April 2011, Pages 2550–2553
نویسندگان
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