TY - JOUR PY - 1992// TI - Androst-5-ene-7,17-dione: a novel class of suicide substrate of aromatase JO - Biochemical and biophysical research communications A1 - Numazawa, M. A1 - Mutsumi, A. A1 - Hoshi, K. A1 - Tanaka, Y. SP - 32 EP - 39 VL - 186 IS - 1 N2 - 5-En-7-one steroid 1 was found to be a potent inhibitor of aromatase. This along with its 19-hydroxy derivative 7 was characterized as suicide substrate of human placental aromatase (k(inact)'s of 0.069 and 0.058 min-1 and KI's of 143 nM and 11.1 microM, respectively, for steroids 1 and 7). The results suggest that the 19-oxygenation would be involved in the irreversible inactivation of aromatase by the 5-en-7-one steroids.

Language: en

LA - en SN - 0006-291X UR - http://dx.doi.org/10.1016/s0006-291x(05)80771-5 ID - ref1 ER -