Development of steroid sulfatase inhibitors

Hydrolysis of biologically inactive steroid sulfates to unconjugated steroids by steroid sulfatase (STS) is strongly implicated in rendering estrogenic stimulation to hormone-dependent cancers such as those of the breast. Considerable progress has been made in the past two decades with regard to the...

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Bibliographic Details
Published in:Molecular and cellular endocrinology 2011-07, Vol.340 (2), p.175-185
Main Authors: Woo, L.W. Lawrence, Purohit, Atul, Potter, Barry V.L.
Format: Article
Language:English
Subjects:
aromatase
arylsulfatase
Cancer
clinical trials
Drug Design
Dual aromatase and sulfatase inhibitors
Endocrinology
Enzyme inhibitors
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Estrone - analogs & derivatives
Estrone - pharmacology
Hormone-dependent breast cancer
Humans
Hydrolysis
Inhibitors
neoplasms
Rendering
Review
Steroid sulfatase
Steroid sulfatase inhibitors
Steroids
Steryl-Sulfatase - antagonists & inhibitors
Steryl-Sulfatase - metabolism
Stimulation
Sulfates
Sulfonic Acids - chemistry
Sulfonic Acids - pharmacology
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Summary:Hydrolysis of biologically inactive steroid sulfates to unconjugated steroids by steroid sulfatase (STS) is strongly implicated in rendering estrogenic stimulation to hormone-dependent cancers such as those of the breast. Considerable progress has been made in the past two decades with regard to the discovery, design and development of STS inhibitors. We outline historical aspects of their development, cumulating in the discovery of the first clinical trial candidate STX64 (BN83495, Irosustat) and other sulfamate-based inhibitors. The development of reversible STS inhibitors and the design of dual inhibitors of both aromatase and STS is also discussed.
ISSN:0303-7207
1872-8057
DOI:10.1016/j.mce.2010.12.035