Estrone phosphate explained
Estrone phosphate (E1P), or estrone 3-phosphate, is an estrogen and steroid sulfatase inhibitor which was never marketed.[1] [2] [3] It has similar affinity for steroid sulfatase as estrone sulfate and acts as a competitive inhibitor of the enzyme.[4] In contrast to estrone sulfate however, it is not hydrolyzed by steroid sulfatase and is instead metabolized by phosphatases.
See also
Notes and References
- Bourne GH . The histochemical dephosphorylation of oestrogen phosphates . The Journal of Physiology . 124 . 2 . 409–416 . May 1954 . 13175141 . 1366276 . 10.1113/jphysiol.1954.sp005117 .
- Li PK, Pillai R, Dibbelt L . Estrone sulfate analogs as estrone sulfatase inhibitors . Steroids . 60 . 3 . 299–306 . March 1995 . 7792836 . 10.1016/0039-128x(94)00048-h . 3070641 .
- Anderson CJ, Lucas LJ, Widlanski TS . Molecular Recognition in Biological Systems: Phosphate Esters vs Sulfate Esters and the Mechanism of Action of Steroid Sulfatases. Journal of the American Chemical Society. 117. 13. 1995. 3889–3890. 0002-7863. 10.1021/ja00118a034.
- Phan CM, Liu Y, Kim BM, Mostafa Y, Taylor SD . Inhibition of steroid sulfatase with 4-substituted estrone and estradiol derivatives . Bioorganic & Medicinal Chemistry . 19 . 20 . 5999–6005 . October 2011 . 21925885 . 10.1016/j.bmc.2011.08.046 .