✦ LIBER ✦

1,N6-etheno-2-aza-adenosine 3′,5′-monophosphate: A new fluorescent substrate for cycle nucleotide phosphodiesterase

✍ Scribed by K.C. Tsou; K.F. Yip; K.W. Lo

Book ID: 102629858
Publisher: Elsevier Science
Year: 1974
Tongue: English
Weight: 369 KB
Volume: 60
Category: Article
ISSN: 0003-2697
DOI: 10.1016/0003-2697(74)90141-9

No coin nor oath required. For personal study only.

✦ Synopsis

I,N"-etheno-2-aza-adenosine 3',5'-monophosphate (cyclic Z-aza+AMP) has been shown to be a sensitive and an efficient substrate for the assay of cyclic-nucleotide phosphodiesterase. The relative activity is 75% compared to cyclic AMP. Two K, values of 503 and 15 pM were observed with the beef heart enzyme.

The importance of adenosine 3,'5'-monophosphate (cyclic AMP) as the intracellular mediator for hormonal action needs little emphasis (1). Its tissue level is controlled by two enzymes: adenylate cyclase, which controls the synthetic step; and cyclic-nucleotide phosphodiesterase, which controls the degradation step. While numerous methods have been reported for the determination of cyclic-nucleotide phosphodiesterase activity (2-8), a fluorescent method that can be adapted to both biochemica1 and cytochemical analysis of this important enzyme is needed. An ingenious but complex fluorescent method was developed by Mann and Christiansen (9) for starch gel. More recently, Secrist et nl. (10) synthesized 1,N6-etheno-adenosine 3',5'-monophosphate (cyclic E-AMP), as a new fluorescent substrate. While cyclic E-AMP is a useful substrate, it cannot be adapted to polyacrylamide gel staining because its emission at 410 nm is indistinguishable from the background fluorescence of polyacrylamide gel. Also, it is only 25% as effective as the natural substrate cyclic AMP.

During our search for a fluorescent nucleoside in the cancer chemotherapy study, we recently synthesized l,N"-etheno-2-aza-adenosine, (2aza-E-adenosine), which has a fluorescent emission maximum of 494 nm, a useful range for cytochemical study (11). The adaptation of this novel synthesis to the preparation of the 2-aza analog of cyclic-e-

📜 SIMILAR VOLUMES

Phase-transfer-catalyzed synthesis of ar

Phase-transfer-catalyzed synthesis of aryl α-ketosides of N-acetylneuraminic acid. A 2-methylfluoran-6-yl glycoside of N-acetylneuraminic acid, 2-methyl-6-(5-acetamido-3,5-dideoxy-α-d-glycero-d-galacto-nonulopyranosyl-onic acid)xanthene-9-spiro-1′-isobenzofuran-3′-one, a new substrate for neuraminidase assay

✍ Jörg Rothermel; Hans Faillard 📂 Article 📅 1990 🏛 Elsevier Science 🌐 English ⚖ 884 KB

Glycosidation of N-acetylneuraminic acid by phase-transfer catalysis in chloroform-aqueous alkali gave several known and some new aryl cY-ketosides in a short reaction time and in good yields. The 4-methylumbelliferyl cu-ketoside, the standard substrate for neuraminidase, was prepared in a yield of