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Preliminary observations of malignant melanoma therapy using radiolabeled alpha-methyltyrosine

✍ Scribed by William H. McLaughlin; William M. Thramann Jr.; Richard M. Lambrecht; Richard A. Milius; William D. Bloomer


Publisher
John Wiley and Sons
Year
1988
Tongue
English
Weight
503 KB
Volume
37
Category
Article
ISSN
0022-4790

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✦ Synopsis


A strategy for cancer therapy using astatine-2 1 1 -labeled alpha-methyltyrosine (21'At-AMT) was studied in cultured B16 melanoma cells and compared to the radiotoxicity of iodine-125-labeled iododeoxyuridine (1251UdR), a thymidine analogue. Both 1251 and 211 At deliver lethal doses of irradiation to melanoma cells when administered as 12%JdR and 211At-AMT. The alpha decay of astatine-21 1 is more effective however, needing only a fraction of the cellular radioactivity of '251UdR to effect comparable clonogenic survival. Compared with 12%JdR, 12%AMT is not cytotoxic because the range of the low energy electrons released does not interact with DNA. Uptake of radiolabeled AMT by melanotic cells is enhanced by theophylline. This preliminary evidence suggests that 211At-labeled melanin precursors may be exquisitely cytotoxic to B 16 melanoma cells.