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Evidence for the mechanism of the irreversible inhibition of oestrone sulphatase (ES) by aminosulphonate based compounds

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Date
2002
ICR Author
James, Karen
Author
Ahmed, S
Owen, CP
James, K
Patel, CK
Sampson, L
Type
Journal Article
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Abstract
In our search for the mechanism of the enzyme oestrone sulphatase (ES) we have synthesised and evaluated a number of compounds that were predicted to possess some inhibitory activity. Some of these compounds were indeed found to be inhibitors of ES, whilst other compounds were not. From a consideration of the structure–activity relationship (SAR) of the inhibitors and non-inhibitors of this enzyme, we discovered a factor which we now believe is the main inhibitory moiety within the aminosulphonated inhibitors. We therefore report the results of our study into a series of phenyl and alkyl sulphamated compounds as inhibitors of ES. The results of the study show that the substituted phenyl sulphamates are potent inhibitors, whereas the alkyl compounds are, in general, non-inhibitors. Using the results of our SAR study, we postulate the probable mechanism for the irreversible and reversible inhibition of ES, and rationalise the role of the different physicochemical factors in the inhibition of this crucial enzyme.
URI
https://repository.icr.ac.uk/handle/internal/2799
DOI
https://doi.org/10.1016/S0960-0760(02)00036-5
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  • Other ICR Research
Language
eng
License start date
2002
Citation
The Journal of Steroid Biochemistry and Molecular Biology, 2002, 80 pp. 429 - 440

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