Steroid sulfatase inhibitors: the current landscape

Area of Science:

• Biochemistry
• Enzyme kinetics
• Pharmacology

Background:

• Steroid sulfatase (STS) enzyme activates steroid sex hormones.
• Dysregulation of STS is implicated in various diseases.
• Recent advancements focus on developing STS inhibitors.

Purpose of the Study:

• To review the structure, function, and disease relevance of STS.
• To comprehensively analyze recently reported STS inhibitors (2016-present).
• To discuss the therapeutic potential of STS inhibition.

Main Methods:

• Literature review of STS enzyme properties.
• Analysis of published studies on STS inhibitors.
• Evaluation of clinical trial data for drug candidates.

Main Results:

• Irosustat identified as a leading STS inhibitor drug candidate.
• Non-steroidal sulfamates represent a promising scaffold for STS inhibitor design.
• Dual-acting molecules offer potential therapeutic advantages.

Conclusions:

• STS inhibitors, particularly non-steroidal sulfamates, hold therapeutic potential for hormone-dependent cancers and neurodegenerative diseases.
• Irosustat is a key drug candidate in clinical trials for breast cancer.
• Targeting STS offers a strategy to manage steroid hormone-related pathologies effectively.