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Steroid Hormone Transforming Aldo-Keto Reductases.
The aldo-keto reductase (AKR) superfamily contains mammalian hydroxysteroid dehydrogenases (HSDs). For each sex steroid there are a pair of HSDs, which by acting as reductases or oxidases can convert potent steroid hormones into their cognate inactive metabolites or vice versa. When found in steroid target tissues they can regulate the occupancy and trans-activation of steroid hormone receptors, providing a pre-receptor regulation of steroid hormone action. Many HSDs are considered therapeutic targets. For example, aldo-keto reductase AKR1C3 (type 5 17beta-hydroxysteroid dehydrogenase) catalyses the formation of the potent androgens, testosterone and 5alpha-dihydrotestosterone, in castrate resistant prostate cancer (CRPC). CRPC is dependent upon intratumoral androgen biosynthesis that reactivate the androgen receptor and is uniformly fatal. Structure-based inhibitor design is being used to develop selective AKR1C3 inhibitors for the treatment of CRPC. In another area structure-function studies on steroid 5beta-reductase (AKR1D1) are being pursued. This enzyme catalyzes a pivotal step in bile-acid biosynthesis and natural mutations are causal in bile-acid deficiency syndromes which are often neonatal fatal. In both areas we use the following techniques: site-directed mutagenesis, x-ray crystallography, transient and steady state kinetics, transfection studies and si-RNA.
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A. M. Api, A. Bartlet, D. Belsito, D. Botelho, M. Bruze, A. Bryant-Freidrich, G. A. Burton, M. A. Cancellieri, H. Chon, M. L. Dagli, W. Dekant,C. Deodhar,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114514-114514
A M Api, A Bartlett, D Belsito, D Botelho, M Bruze, A Bryant-Freidrich, G A Burton, M A Cancellieri, H Chon, M L Dagli, W Dekant,C Deodhar,
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association (2024): 114692-114692
A. M. Api, D. Belsito, D. Botelho, M. Bruze, G. A. Burton, M. A. Cancellieri, H. Chon, M. L. Dagli, W. Dekant,C. Deodhar,A. D. Fryer, L. Jones,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114442-114442
A. M. Api, D. Belsito, D. Botelho, M. Bruze,G. A. Burton, M. A. Cancellieri, H. Chon, M. L. Dagli, M. Date, W. Dekant,C. Deodhar,A. D. Fryer,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114272
A. M. Api, D. Belsito, D. Botelho, M. Bruze, G. A. Burton, M. A. Cancellieri, H. Chon, M. L. Dagli, W. Dekant,C. Deodhar,A. D. Fryer, L. Jones,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114332-114332
A. M. Api, D. Belsito, D. Botelho, M. Bruze, G. A. Burton, M. A. Cancellieri, H. Chon, M. L. Dagli, W. Dekant,C. Deodhar,A. D. Fryer, L. Jones,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114267-114267
A. M. A. Api, D. B. Belsito, D. A. Botelho, M. C. Bruze,G. A. JrD Burton, M. A. A. Cancellieri, H. A. Chon, M. L. E. Dagli, M. A. Date, W. F. Dekant,C. A. Deodhar, A. D. G. Fryer,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114294-114294
A. M. Api, D. Belsito, D. Botelho, M. Bruze,G. A. Burton Jr, M. A. Cancellieri, H. Chon, M. L. Dagli, M. Date, W. Dekant,C. Deodhar,A. D. Fryer,
A M Api, A Bartlett, D Belsito, D Botelho, M Bruze, A Bryant-Freidrich, G A Burton, M A Cancellieri, H Chon, M L Dagli, W Dekant,C Deodhar,
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association (2024): 114542-114542
A. M. Api, D. Belsito, D. Botelho, M. Bruze,G. A. Burton, M. A. Cancellieri, H. Chon, M. L. Dagli, W. Dekant,C. Deodhar,A. D. Fryer, L. Jones,
FOOD AND CHEMICAL TOXICOLOGY (2024): 114303-114303
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