基礎有機化学討論会要旨集(基礎有機化学連合討論会予稿集)
第53回有機反応化学討論会
セッションID: P-66
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Estrane-peptide Conjugates
*松本 知広渡辺 正敬又賀 駿太郎Thiemann Thies
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Estrane derivatives can possess a good binding affinity towards the estrogen receptor ERa. Estrogen positive breast cancer cells have heightened concentrations of the estrogen receptor and estranes chelated to radioisotopes (eg., to technetium) are expected to be applicable as radiodiagnostica for the detection of minimal breast cancer. Peptide combinations such as Cys-Gly-Cys or Gly-Gly-Cys act as good ligands for technetium and rhenium, radionuclides, which are versatile and promising in radioimaging. On the other hand, peptidyl steroids, where amino acids or peptides are linked to the steroidal frame, have been reported to play an important role in living systems. Estrane derivatives linked to several combinations of tri-peptides (eg., Cys-Gly-Cys) were synthesized by the DCC method in the liquid phase. It can be expected that the combinations of tri-peptides used may make these moieties suitable ligands for 99m-Tc, as radionuclide, so that these steroidal derivatives can be utilized as new diagnostica for minimal estrogen positive breast cancer.
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