Preferred Label : CYP17 Lyase Inhibitor ASN001;
NCIt related terms : EN-3356;
NCIt definition : An orally available non-steroidal, lyase-selective inhibitor of the steroid 17-alpha-hydroxylase/C17,20
lyase (CYP17A1 or CYP17), with potential anti-androgenic and antineoplastic activities.
Upon oral administration, CYP17 lyase inhibitor ASN001 selectively binds to and inhibits
the lyase activity of CYP17A1 in both the testes and adrenal glands, resulting in
a significant reduction in androgen production to castrate-range levels. This may
both decrease androgen-dependent growth signaling and inhibit the proliferation of
androgen-dependent tumor cells. The cytochrome P450 enzyme CYP17A1, which is localized
to the endoplasmic reticulum, exhibits both 17alpha-hydroxylase and 17,20-lyase activities;
it plays a key role in the steroidogenic pathway. The selective inhibition of CYP17A1
lyase activity by ASN001 prevents the increased synthesis of mineralocorticoids that
is normally seen with non-selective CYP17 inhibitors, which also inhibit the 17-alpha-hydroxylase
activity of CYP17A1.;
UNII : J03L4XRQ2R;
CAS number : 1429329-63-4;
Molecule name : ASN001;
Origin ID : C120310;
UMLS CUI : C3896913;
Semantic type(s)
concept_is_in_subset
has_target