Preferred Label : Apomine;
NCIt synonyms : Phosphonic acid, (2-(3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)ethylidene)bis-, tetrakis(1-methylethyl)
Ester; Tetraisopropyl-2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethylidene-1,1-diphosphonate;
NCIt related terms : SR-45023A; SR-45023A (Apomine);
NCIt definition : A 1,1-bisphosphonate ester with potential antineoplastic and hypocholesterolemic activities.
Apomine binds to hydroxyapatite crystals in the bone matrix where it inhibits enzymatic
activity of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, which is required
for the formation of mevalonate, the precursor of cholesterol. Consequently, shortage
of mevalonate impedes the synthesis of downstream isoprenoids that are essential for
protein prenylation. This leads to the loss of activity of proteins involved in osteoclast
function and cellular proliferation, such as Ras and Rho, leading to an inhibition
of cellular proliferation, and induction of osteoclasts apoptosis. In addition, apomine
activates the farnesoid X activated receptor (FXR), a member of the nuclear hormone
superfamily implicated in cholesterol metabolism and bile acid transport and may play
a role in this agent's antineoplastic effect.;
Alternative definition : NCI-GLOSS: An anticancer drug that belongs to the family of drugs called bisphosphonates.
It affects cancer cell receptors governing cell growth and cell death.;
UNII : JQ95208805;
InChIKey : YLJOVCWVJCDPLN-UHFFFAOYSA-N;
CAS number : 126411-13-0;
Molecule name : SKF 99085; SR-45023A;
Chemical formula : C28H52O7P2;
Codes from synonyms : 20013; CDR0000046662;
Origin ID : C1873;
UMLS CUI : C0919349;
Currated CISMeF NLP mapping
- apomine [MeSH Supplementary Concept]
- Semantic type(s)
- UMLS correspondences (same concept)
- apomine [MeSH Supplementary Concept]
- concept_is_in_subset
