암세포 내로의 약물 전달 증진 목적의신규 소마토스타틴 수용체 타겟리간드 합성 및 평가
Synthesis and Evaluation of a Ligand Targeting the Somatostatin Receptor for Drug Delivery to Tumor Cell
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involved in the growth and spread of cancer cells to produce its cytotoxic effect. Either small molecule drugs or monoclonal antibodies are mostly used in targeted therapies. Unfortunately, targeted therapy has a certain degree of unwanted side effect like other cytotoxicityinducing chemotherapies. To overcome and to reduce unwanted side effects during a cancertherapy, recently radiopeptide therapies has got the worlds’ attraction for the tumor targetingmodalities due to its beneficial effect on less side effect compared to cytotoxic chemotherapies. Among radiopeptide therapies, 177Lu-DOTATATE is a major modality as an effective one inventedso far in treating neuroendocrine tumor (NET) and it has been in clinical trials at least one decade. Although it does have rather effective therapeutic effect on NET, it has less effective in ratherlarge solid tumor. There are many ways to improve or increase therapeutic effect of radiopeptideare a finding the potent small molecules to target the tumor site selectively, or a labeling withradioisotope of emitting high energy, or an improving its biological half-life by introducingdifferent moieties to increase lipophilicity. Present study was focus to increase a biological halflifeof radio somatostatin which will target the somatostatin receptor by altering the bifunctionalchelator (BFCA) by introducing lipophilic moiety to the somatostatin, which would make thelabeled peptide stay longer in the tumor site and thus it can intensify the therapeutic effect ontumor cell itself and around tissues.
Abstract
involved in the growth and spread of cancer cells to produce its cytotoxic effect. Either small molecule drugs or monoclonal antibodies are mostly used in targeted therapies. Unfortunately, targeted therapy has a certain degree of unwanted side effect like other cytotoxicityinducing chemotherapies. To overcome and to reduce unwanted side effects during a cancertherapy, recently radiopeptide therapies has got the worlds’ attraction for the tumor targetingmodalities due to its beneficial effect on less side effect compared to cytotoxic chemotherapies. Among radiopeptide therapies, 177Lu-DOTATATE is a major modality as an effective one inventedso far in treating neuroendocrine tumor (NET) and it has been in clinical trials at least one decade. Although it does have rather effective therapeutic effect on NET, it has less effective in ratherlarge solid tumor. There are many ways to improve or increase therapeutic effect of radiopeptideare a finding the potent small molecules to target the tumor site selectively, or a labeling withradioisotope of emitting high energy, or an improving its biological half-life by introducingdifferent moieties to increase lipophilicity. Present study was focus to increase a biological halflifeof radio somatostatin which will target the somatostatin receptor by altering the bifunctionalchelator (BFCA) by introducing lipophilic moiety to the somatostatin, which would make thelabeled peptide stay longer in the tumor site and thus it can intensify the therapeutic effect ontumor cell itself and around tissues.
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