TLDR The document concludes that research on sulfatase inhibitors should continue due to their potential in treating various diseases, despite some clinical trial failures.
The document from 2012 reviews the development of sulfatase inhibitors, with a focus on steroid sulfatase (STS) inhibitors, for the treatment of hormone-dependent diseases such as breast cancer and endometriosis. It discusses the clinical trials of STS inhibitors like STX64 and PGL2001, the development of non-estrogenic steroidal sulfamates to avoid tumor growth stimulation, and the potential of these inhibitors in treating skin disorders, fertility issues, and memory enhancement. The review also covers the dual-acting compounds that inhibit STS and other cancer-related targets, the concept of reversible STS inhibition, and the use of pharmacological chaperones for lysosomal storage disorders. Despite some clinical trial failures, the document suggests continued research into STS inhibitors and their broader therapeutic applications, including their potential role in estrogen-ablative cancer therapy and treatment of androgen-stimulated diseases. The document concludes with the need for more drug-like leads for lysosomal sulfatase deficiencies and acknowledges funding support from the Australian Research Council.
83 citations,
July 2008 in “Current Opinion in Chemical Biology” The document concludes that understanding sulfation biology is crucial for creating treatments due to its importance in biological functions and disease.
17 citations,
December 2004 in “Bioorganic & Medicinal Chemistry Letters” Scientists found new, better-working inhibitors for a hormone-related enzyme.
37 citations,
September 2003 in “Journal of Medicinal Chemistry” A substance called Compound 2g can strongly block STS (a hormone-related enzyme) without affecting estrogen levels, making it potentially good for treating breast cancer.
111 citations,
August 2002 in “Journal of Medicinal Chemistry” New compounds were made that block an enzyme linked to breast cancer better than existing treatments.
25 citations,
May 2003 in “Expert Opinion on Therapeutic Patents” Steroid Sulfatase inhibitors show promise in treating hormone-dependent disorders like cancers, hair loss, and acne, with 667COUMATE being a potential candidate for breast cancer treatment trials.
451 citations,
March 2005 in “Endocrine Reviews” The enzyme steroid sulfatase is linked to breast cancer and other conditions, and inhibitors are being developed for treatment.
431 citations,
October 2008 in “Current Medicinal Chemistry” Coumarin derivatives show promise as anti-estrogenic agents for treating breast cancer, with some in clinical trials.
233 citations,
November 2002 in “The journal of investigative dermatology/Journal of investigative dermatology” Creating stronger blockers for skin enzymes might lead to better treatment for conditions like acne and excessive hair growth.
14 citations,
September 2015 in “Expert Opinion on Therapeutic Targets” The conclusion is that while oral contraceptive pills are effective for PCOS-related high androgen levels, new treatments with fewer side effects are needed.
