1. Steroid sulfatase inhibitors: the current landscape.
- Author
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Anbar HS, Isa Z, Elounais JJ, Jameel MA, Zib JH, Samer AM, Jawad AF, and El-Gamal MI
- Subjects
- Animals, Antineoplastic Agents pharmacology, Breast Neoplasms drug therapy, Breast Neoplasms pathology, Enzyme Inhibitors administration & dosage, Female, Humans, Patents as Topic, Steryl-Sulfatase metabolism, Sulfonic Acids administration & dosage, Sulfonic Acids pharmacology, Drug Design, Enzyme Inhibitors pharmacology, Steryl-Sulfatase antagonists & inhibitors
- Abstract
Introduction : Steroid sulfatase (STS) enzyme is responsible for transforming the inactive sulfate metabolites of steroid sex hormones into the active free steroids. Both the deficiency and the over-expression of STS are associated with the pathophysiology of certain diseases. This article provides the readership with a comprehensive review about STS enzyme and its recently reported inhibitors. Areas covered : In the present article, we reviewed the structure, location, and substrates of STS enzyme, physiological functions of STS, and disease states related to over-expression or deficiency of STS enzyme. STS inhibitors reported during the last five years (2016-present) have been reviewed as well. Expert opinion : Irosustat is the most successful STS inhibitor drug candidate so far. It is currently under investigation in clinical trials for treatment of estrogen-dependent breast cancer. Non-steroidal sulfamate is the most favorable scaffold for STS inhibitor design. They can be beneficial for the treatment of hormone-dependent cancers and neurodegenerative disorders without significant estrogenic side effects. Moreover, dual-acting molecules (inhibitors of STS + another synergistic mechanism) can be therapeutically efficient.
- Published
- 2021
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