CBP/p300 bromodomain inhibitor OPN-6602
Term · Oncology and biomedicine · MLC-T-ONC-012349
An orally bioavailable small molecule inhibitor of the bromodomain of the histone acetyltransferase (HAT) paralogs, CREB binding protein (CBP) and p300 (E1A-associated protein p300; EP300; p300 HAT), with potential antineoplastic activity. Upon oral administration, CBP/p300 bromodomain inhibitor OPN-6602 targets and binds to the bromodomains of p300 and CBP. This disrupts the acetylation of histones and other proteins, prevents the co-activation of key transcription factors that contribute to tumor progression including the androgen receptor (AR), interferon regulatory factor 4 (IRF4) and Myc proto-oncogene protein (c-Myc), and downregulates AR and IRF4/MYC signaling, thereby inhibiting tumor cell proliferation. The HAT paralogs p300 and CBP are key transcriptional co-activators that are essential for a multitude of cellular processes and are implicated in the progression and therapeutic resistance of certain cancers.
| Identifier | MLC-T-ONC-012349 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | EP300/CBP bromodomain inhibitor OPN-6602 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-012349",
"term": "CBP/p300 bromodomain inhibitor OPN-6602",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable small molecule inhibitor of the bromodomain of the histone acetyltransferase (HAT) paralogs, CREB binding protein (CBP) and p300 (E1A-associated protein p300; EP300; p300 HAT), with potential antineoplastic activity. Upon oral administration, CBP/p300 bromodomain inhibitor OPN-6602 targets and binds to the bromodomains of p300 and CBP. This disrupts the acetylation of histones and other proteins, prevents the co-activation of key transcription factors that contribute to tumor progression including the androgen receptor (AR), interferon regulatory factor 4 (IRF4) and Myc proto-oncogene protein (c-Myc), and downregulates AR and IRF4/MYC signaling, thereby inhibiting tumor cell proliferation. The HAT paralogs p300 and CBP are key transcriptional co-activators that are essential for a multitude of cellular processes and are implicated in the progression and therapeutic resistance of certain cancers.",
"synonyms": [
"EP300/CBP bromodomain inhibitor OPN-6602"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/cbp-p300-bromodomain-inhibitor-opn-6602/"
}
Record 4,347 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.