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01:31Transducer Mechanism: Nuclear Receptors
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About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
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01:21Intrauterine Drug Delivery Systems
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01:28Stability of Conjugated Dienes
Introduction
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01:33Hormonal Regulation
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17ß-hydroxysteroid dehydrogenase inhibitors.
J M Day1, H J Tutill, A Purohit
1Department of Endocrinology and Metabolic Medicine, Imperial College London, St. Mary's Hospital, Winsland Street, London, UK. joanna.day@imperial.ac.uk
Minerva Endocrinologica
|July 3, 2010
Summary
17ß-hydroxysteroid dehydrogenases (17ß-HSDs) are key enzymes in hormone regulation. This review highlights recent progress in developing specific 17ß-HSD inhibitors for treating steroid-dependent diseases like cancer.
Area of Science:
- Biochemistry
- Enzymology
- Molecular Biology
Background:
- 17ß-hydroxysteroid dehydrogenases (17ß-HSDs) are crucial enzymes requiring NAD(P)(H) for redox activity.
- They regulate active hormone levels, impacting steroid metabolism and disease progression.
- Fifteen 17ß-HSDs exist, varying in substrate specificity and homology, with 17ß-HSD Type 5 being an aldo-keto reductase.
Purpose of the Study:
- To review recent advances in developing specific inhibitors for 17ß-HSD1, 17ß-HSD3, and 17ß-HSD5.
- To discuss the evaluation models used for these enzyme inhibitors.
- To explore therapeutic potential for steroid-dependent diseases.
Main Methods:
- Literature review focusing on recent research in 17ß-HSD inhibitor development.
- Analysis of in vivo disease models for evaluating inhibitor efficacy.
- Discussion of enzyme kinetics and structural studies related to inhibitor design.
Main Results:
- Significant progress in developing specific inhibitors for 17ß-HSD1, 3, and 5.
- Demonstrable efficacy of these inhibitors in preclinical in vivo models for steroid-dependent diseases.
- Identification of key structural features and mechanisms for targeted inhibition.
Conclusions:
- Targeting 17ß-HSD enzymes offers a promising therapeutic strategy for steroid-dependent diseases.
- Further development and clinical trials are warranted for 17ß-HSD inhibitors.
- Specific inhibitors show potential for treating breast cancer, prostate cancer, and endometriosis.