Evidence for the existence of a sulfhydryl group in the adenylate cyclase active site.

Alexander Skurat, M. S. Yurkova, L. A. Baranova, N. N. Gulyaev, T. V. Bulargina, E. S. Severin

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

6-Cloro-9-beta-d-ribofuranosylpurine 5'-triphosphate (CIRTP) and 6-mercapto-9-beta-d-ribofuranosylpurine 5'-triphosphate (SRTP) irreversibly inhibit adenylate cyclase from rat brain. Adenosine 5'-[beta, gamma -imido] triphosphate protects the enzyme against inactivation by CIRTP and SRTP and acts as a competitive inhibitor with respect to ATP with the Ki value 2 X 10(-4) M. Study of the pH-dependence of the rate of the enzyme inactivation by CIRTP showed that pK for the group modified by this compound is equal to 7.45. Inactivation is first order with respect to the enzyme; the saturation effect is observed at the increased concentration of CIRTP. The k2 and KI values for irreversible inhibition of brain adenylate cyclase by CIRTP were 0.25 min-1 and 1.9 X 10(-4) M, respectively. Adenylate cyclase inhibition by SRTP is also time-dependent. Partial protection against the enzyme inactivation was observed. Dithiothreitol restores the activity of SRTP-inactivated adenylate cyclase. The results obtained indicate the presence of an -SH group in the purine amino group binding area of the enzyme active site.

Original languageEnglish
Pages (from-to)451-461
Number of pages11
JournalBiochemistry International
Volume10
Issue number3
StatePublished - Mar 1985
Externally publishedYes

Fingerprint

Adenylyl Cyclases
Catalytic Domain
Enzymes
Brain
Dithiothreitol
Adenosine
Rats
Adenosine Triphosphate
6-thioinosine-5'-triphosphate
6-chloro-9 beta-D-ribofuranosylpurine-5'-triphosphate
triphosphoric acid

ASJC Scopus subject areas

  • Biochemistry

Cite this

Skurat, A., Yurkova, M. S., Baranova, L. A., Gulyaev, N. N., Bulargina, T. V., & Severin, E. S. (1985). Evidence for the existence of a sulfhydryl group in the adenylate cyclase active site. Biochemistry International, 10(3), 451-461.

Evidence for the existence of a sulfhydryl group in the adenylate cyclase active site. / Skurat, Alexander; Yurkova, M. S.; Baranova, L. A.; Gulyaev, N. N.; Bulargina, T. V.; Severin, E. S.

In: Biochemistry International, Vol. 10, No. 3, 03.1985, p. 451-461.

Research output: Contribution to journalArticle

Skurat, A, Yurkova, MS, Baranova, LA, Gulyaev, NN, Bulargina, TV & Severin, ES 1985, 'Evidence for the existence of a sulfhydryl group in the adenylate cyclase active site.', Biochemistry International, vol. 10, no. 3, pp. 451-461.
Skurat A, Yurkova MS, Baranova LA, Gulyaev NN, Bulargina TV, Severin ES. Evidence for the existence of a sulfhydryl group in the adenylate cyclase active site. Biochemistry International. 1985 Mar;10(3):451-461.
Skurat, Alexander ; Yurkova, M. S. ; Baranova, L. A. ; Gulyaev, N. N. ; Bulargina, T. V. ; Severin, E. S. / Evidence for the existence of a sulfhydryl group in the adenylate cyclase active site. In: Biochemistry International. 1985 ; Vol. 10, No. 3. pp. 451-461.
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