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Horm Metab Res 1978; 10(5): 392-395
DOI: 10.1055/s-0028-1093399
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© Georg Thieme Verlag KG Stuttgart · New York

The Effect of Streptozotocin Analogues on Guanylate Cyclase Activity[*]

D. L. Vesely , G. S. Levey [+]
  • Division of Endocrinology and Metabolism, Department of Medicine, University of Miami School of Medicine, Miami, Florida, U.S.A.
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Publikationsdatum:
23. Dezember 2008 (online)

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Abstract

Streptozotocin, a nitrosamide carcinogen, enhances the activity of guanylate cyclase. Six analogues of streptozotocin were studied in order to elucidate critical structure-activity relationships pertaining to the activation of guanylate cyclase. Analogue 1, known as chlorozotocin, has a nitroso group and increased guanylate cyclase activity 17 to 28-fold. Analogue Ill, which also has a nitroso group, but greater structural modifications with 4 acetate groups extending off of the glucose moiety, activated guanylate cyclase in colon but not in kidney. The other analogues (II, IV, VI, and VIII) lacking nitroso groups, either had no effect or produced mild decreases in guanylate cyclase activity.

Key words

Streptozotocin Analogues - Guanylate Cyclase Activity - Colon - Kidney

1 Supported by NIH grant HL 13715-07, 08

1 Supported by NIH grant HL 13715-07, 08

2 Investigator, Howard Hughes Medical Institute.

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