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Molecular properties generated using the CDK
|Compound class||Synthetic organic|
|International Nonproprietary Names|
|Astemizole was originally identified as a histamine H1 receptor antagonist. Astemizole use as an antihistamine was withdrawn from the US market in 1999 as it caused arrhythmias, probably due to blocking the hERG potassium channel (Kv11.1) .
A 2014 publication showed that astemizole's anti-proliferative effects in cancer cells is due to disruption of a protein-protein interaction required for the formation of the active polycomb repressive complex 2 (PRC2) . PRC2 contains the histone methyltransferase EZH2, which is responsible for catalytic trimethylation of lysine 27 on histone H3 (H3K27me3), an epigenetic modification that is a hallmark of silent chromatin. Aberrant PRC2 activity is associated with cancer initiation and progression. Astemizole was shown to inhibit the interaction between EZH2 and a PRC2 structural protein called embryonic ectoderm development (EED) , and that this action destabilizes PRC2 and reduces its methylation activity.
|CAS Registry No.||68844-77-9|
|GtoPdb PubChem SID||135649968|
|Search Google for chemical match using the InChIKey||GXDALQBWZGODGZ-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||GXDALQBWZGODGZ|
|Search PubMed clinical trials||astemizole|
|Search PubMed titles||astemizole|
|Search PubMed titles/abstracts||astemizole|
|Search UniChem for chemical match using the InChIKey||GXDALQBWZGODGZ-UHFFFAOYSA-N|
|Search UniChem for chemicals with the same backbone||GXDALQBWZGODGZ|
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Cat. No. 3489