Related Experiment Video

Updated: May 30, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

Steroid sulfatase inhibitors for estrogen- and androgen-dependent cancers

Atul Purohit1, Paul A Foster

  • 1Oncology Drug Discovery Group, Section of Investigative Medicine, Imperial College London, Hammersmith Hospital, London W12 0NN, UK.

The Journal of Endocrinology
|August 24, 2011
PubMed

Insights

Steroid sulfatase (STS) inhibitors show promise for treating hormone-dependent cancers by blocking estrogen and androgen synthesis. Clinical trials are underway for breast, prostate, and endometrial cancers, indicating a potential future therapeutic role.

Area of Science:

  • Endocrinology
  • Oncology
  • Medicinal Chemistry

Background:

  • Estrogens and androgens are crucial for hormone-dependent cancer development.
  • Steroid sulfatase (STS) is a key enzyme in synthesizing these hormones, making it a therapeutic target.
  • STS hydrolyzes sulfate-conjugated precursors to active androgens and estrogens.

Purpose of the Study:

  • To review the chemical development and biological activity of steroid sulfatase (STS) inhibitors.
  • To assess the current status of clinical trials involving STS inhibitors for hormone-dependent cancers.
  • To highlight the potential of STS inhibitors in cancer therapy and other conditions.

Main Methods:

  • Review of chemical synthesis and development of STS inhibitors.
  • Evaluation of in vitro and in vivo biological activity of STS inhibitors.
  • Analysis of ongoing and completed clinical trials for STS inhibitors.

Main Results:

  • Development of novel in vivo models for pre-clinical testing of STS inhibitors.
  • Completion of Phase I/II clinical trials in postmenopausal women with breast cancer.
  • Active clinical trials in patients with hormone-dependent prostate and endometrial cancer.

Conclusions:

  • STS inhibitors are a promising therapeutic strategy for hormone-dependent cancers.
  • Potent STS inhibitors are expected to be valuable in treating various cancers and non-oncological conditions.
  • Continued research and clinical evaluation are essential for realizing the full therapeutic potential of STS inhibitors.

Related Concept Videos

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids01:19

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme activation, sulfur...
Sulfur Assimilation01:20

Sulfur Assimilation

Sulfur is an essential element in biological systems, contributing to synthesizing key biomolecules, including amino acids such as cysteine and methionine, and cofactors such as coenzyme A and biotin. Microorganisms primarily assimilate sulfur as sulfate (SO₄²⁻) from the environment, which must undergo a series of biochemical transformations before it can be incorporated into cellular components. As sulfate is highly oxidized, it must undergo assimilatory sulfate reduction to become...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Preparation and Reactions of Sulfides02:26

Preparation and Reactions of Sulfides

Sulfides are the sulfur analog of ethers, just as thiols are the sulfur analog of alcohol. Like ethers, sulfides also consist of two hydrocarbon groups bonded to the central sulfur atom. Depending upon the type of groups present, sulfides can be symmetrical or asymmetrical. Symmetrical sulfides can be prepared via an SN2 reaction between 2 equivalents of an alkyl halide and one equivalent of sodium sulfide.
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Drugs for Treatment of Ulcerative Colitis in IBD01:29

Drugs for Treatment of Ulcerative Colitis in IBD

Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide generation.