@article{oai:kanazawa-u.repo.nii.ac.jp:00058958,
 author = {Shiba, Kazuhiro and Mori, Hirofumi and Hisada, Kinichi and 柴, 和弘 and 森, 厚文 and 久田, 欣一},
 issue = {5},
 journal = {Radioisotopes},
 month = {},
 note = {We studied the tumor-localizing characteristics of alicyclic alpha-amino acid analogs (a-j) without alpha-hydrogen, because of the selective affinity of synthetic nonmetabolizing amino acids such as 1-aminocyclopentanecarboxylic acid (ACPC) and alpha-aminoisobutyric acid alpha-AIB) to tumor tissues. Ten different alicyclic alpha-amino acids (a-j) were labeled with 14C using a modified Bücherer synthesis for amino acids. The tissue distributions and whole-body autoradiographic study of these 14C-labeled alicyclic alpha-amino acid analogs (a-j) were investigated in mice bearing Ehrlich tumor. These results showed that the tumor uptakes and tumor to tissue concentration ratios increased with decreasing ringsize in homologous series (8- through 4-membered ring systems) and alicyclic alpha-amino acid analogs containing 3- or 4-methyl group had the higher tumor to tissue concentration ratios. On the other hand, alicyclic alpha-amino acid analogs containing 2-methyl group and 4-phenyl group showed the lower tumor uptakes and the lower tumor to tissue concentration ratios. These results suggest that the small ringsize alicyclic alpha-amino acid analogs containing 3-methyl group such as 3-methyl-1-aminocyclopentanecarboxylic acid (3-MeACPC) may be effective for the early detection of tumors., 腫瘍親和性に優れているa位に水素を有しない脂環式合成アミノ酸である1-aminocyclopentanecarboxylic acid (ACPC) と9種の類似化合物を14Cで標識合成し, これらをニールリッヒ担がんマウスに投与し, 臓器摘出法および全身オートラジオグラフィにて脂環式合成アミノ酸の構造変化 (環の大きさ, 側鎖の種類および位置) による腫瘍親和性の影響についてその相関性を検討した。
その結果, 1.amino-3-methylcy clopentanecarboxylic acid (3-MeACPC) のような比較的環の大きさが小さくまたアミノ酸の官能基 (-NH3, -COOH) から離れた位置にメチル基を有する脂環式合成アミノ酸が優れた腫瘍親和性物質としての可能性が示唆された。, 金沢大学疾患モデル総合研究センター},
 pages = {269--276},
 title = {脂環式合成アミノ酸: その構造と腫瘍親和性の相関性},
 volume = {37},
 year = {1988}
}