Gossypol inhibition of adenylate cyclase

Katherine L. Olgiati; Diane G. Toscano; William M. Atkins; William A. Toscano

doi:10.1016/0003-9861(84)90404-1

Gossypol inhibition of adenylate cyclase

Katherine L. Olgiati, Diane G. Toscano, William M. Atkins, William A. Toscano

Environmental Health Sciences

Research output: Contribution to journal › Article › peer-review

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Abstract

Gossypol, a polyphenolic binaphthalene-dialdehyde reputed to exert contraceptive action in males, reversibly inhibits adenylate cyclase [ATP pyrophosphate lyase (cyclizing), EC 4.6.1.1] in a concentration-dependent manner. In membranes prepared from a variety of organs, the half-maximal inhibitory concentration (IC₅₀) ranges from 75 μm (rat Leydig tumor cells) to 250 μm (rat liver membranes). Kinetic studies using partially purified catalytic subunit isolated from bovine testis show that gossypol is competitive with ATP with an apparent K_i of 110 μm. These data suggest that gossypol inhibition of adenylate cyclase is due to direct interaction at the nucleotide-binding domain of the catalytic subunit of the enzyme.

Original language	English (US)
Pages (from-to)	411-415
Number of pages	5
Journal	Archives of Biochemistry and Biophysics
Volume	231
Issue number	2
DOIs	https://doi.org/10.1016/0003-9861(84)90404-1
State	Published - Jun 1984

Bibliographical note

Funding Information:
‘This work was supported by a grant from the National Institutes of Health, GM 28897. ’ To whom reprint requests should be addressed.

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title = "Gossypol inhibition of adenylate cyclase",

abstract = "Gossypol, a polyphenolic binaphthalene-dialdehyde reputed to exert contraceptive action in males, reversibly inhibits adenylate cyclase [ATP pyrophosphate lyase (cyclizing), EC 4.6.1.1] in a concentration-dependent manner. In membranes prepared from a variety of organs, the half-maximal inhibitory concentration (IC50) ranges from 75 μm (rat Leydig tumor cells) to 250 μm (rat liver membranes). Kinetic studies using partially purified catalytic subunit isolated from bovine testis show that gossypol is competitive with ATP with an apparent Ki of 110 μm. These data suggest that gossypol inhibition of adenylate cyclase is due to direct interaction at the nucleotide-binding domain of the catalytic subunit of the enzyme.",

author = "Olgiati, {Katherine L.} and Toscano, {Diane G.} and Atkins, {William M.} and Toscano, {William A.}",

note = "Funding Information: {\textquoteleft}This work was supported by a grant from the National Institutes of Health, GM 28897. {\textquoteright} To whom reprint requests should be addressed.",

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T1 - Gossypol inhibition of adenylate cyclase

AU - Olgiati, Katherine L.

AU - Toscano, Diane G.

AU - Atkins, William M.

AU - Toscano, William A.

N1 - Funding Information: ‘This work was supported by a grant from the National Institutes of Health, GM 28897. ’ To whom reprint requests should be addressed.

PY - 1984/6

Y1 - 1984/6

N2 - Gossypol, a polyphenolic binaphthalene-dialdehyde reputed to exert contraceptive action in males, reversibly inhibits adenylate cyclase [ATP pyrophosphate lyase (cyclizing), EC 4.6.1.1] in a concentration-dependent manner. In membranes prepared from a variety of organs, the half-maximal inhibitory concentration (IC50) ranges from 75 μm (rat Leydig tumor cells) to 250 μm (rat liver membranes). Kinetic studies using partially purified catalytic subunit isolated from bovine testis show that gossypol is competitive with ATP with an apparent Ki of 110 μm. These data suggest that gossypol inhibition of adenylate cyclase is due to direct interaction at the nucleotide-binding domain of the catalytic subunit of the enzyme.

AB - Gossypol, a polyphenolic binaphthalene-dialdehyde reputed to exert contraceptive action in males, reversibly inhibits adenylate cyclase [ATP pyrophosphate lyase (cyclizing), EC 4.6.1.1] in a concentration-dependent manner. In membranes prepared from a variety of organs, the half-maximal inhibitory concentration (IC50) ranges from 75 μm (rat Leydig tumor cells) to 250 μm (rat liver membranes). Kinetic studies using partially purified catalytic subunit isolated from bovine testis show that gossypol is competitive with ATP with an apparent Ki of 110 μm. These data suggest that gossypol inhibition of adenylate cyclase is due to direct interaction at the nucleotide-binding domain of the catalytic subunit of the enzyme.

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Gossypol inhibition of adenylate cyclase

Abstract

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