CBP/p300 bromodomain inhibitor TT125-802
Term · Oncology and biomedicine · MLC-T-ONC-012350
An orally bioavailable small molecule inhibitor of the bromodomain of the histone acetyltransferase (HAT) paralogs, CREB binding protein (CBP; CREBBP) and p300 (E1A-associated protein p300; p300 HAT), with potential immunomodulating and antineoplastic activities. Upon oral administration, CBP/p300 bromodomain inhibitor TT125-802 targets and binds to the bromodomains of CBP and p300. This disrupts the acetylation of histones and other proteins and decreases regulatory T cells (Tregs) generation, inhibits its suppressive function and causes Tregs apoptosis. This modulates T-helper cells, induces an anti-tumor immune response and decreases tumor growth. The HAT paralogs CBP and p300 are key transcriptional co-activators that are essential for a multitude of cellular processes and play a key role in the regulation of gene expression in both tumor and immune cells.
| Identifier | MLC-T-ONC-012350 |
|---|---|
| Field | Oncology and biomedicine |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-012350",
"term": "CBP/p300 bromodomain inhibitor TT125-802",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable small molecule inhibitor of the bromodomain of the histone acetyltransferase (HAT) paralogs, CREB binding protein (CBP; CREBBP) and p300 (E1A-associated protein p300; p300 HAT), with potential immunomodulating and antineoplastic activities. Upon oral administration, CBP/p300 bromodomain inhibitor TT125-802 targets and binds to the bromodomains of CBP and p300. This disrupts the acetylation of histones and other proteins and decreases regulatory T cells (Tregs) generation, inhibits its suppressive function and causes Tregs apoptosis. This modulates T-helper cells, induces an anti-tumor immune response and decreases tumor growth. The HAT paralogs CBP and p300 are key transcriptional co-activators that are essential for a multitude of cellular processes and play a key role in the regulation of gene expression in both tumor and immune cells.",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/cbp-p300-bromodomain-inhibitor-tt125-802/"
}
Record 4,348 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.