
The Role of CREBBP/EP300 and Its Therapeutic Implications in ...
CREB-binding protein (CREBBP) and E1A-binding protein P300 (EP300) are two key acetyltransferases and transcriptional cofactors that regulate gene expression by regulating the acetylation levels of histone proteins and non-histone proteins.
Tumour suppressor EP300, a modulator of paclitaxel resistance …
We have previously described a novel pathway controlling drug resistance, epithelial-to-mesenchymal transition (EMT) and stemness in breast cancer cells. Upstream in the pathway, three miRs (miR-106b, miR-93 and miR-25) target EP300, a transcriptional activator of …
Exploitation of EP300 and CREBBP Lysine Acetyltransferases by …
EP300 (hereafter referred to as p300) and its closely related paralog CREB-binding protein (CREBBP, hereafter CBP) are ubiquitously expressed transcriptional coactivators and major lysine acetyltransferases (KATs) in metazoans.
Analysis and therapeutic targeting of the EP300 and CREBBP
Dec 1, 2022 · In the current study, we investigated the physiological roles of EP300 and CREBBP in both ALCL and HL, and exploited the therapeutic potential of EP300/CREBBP small molecule inhibitors that...
OPN-6602, an Orally Bioavailable EP300/CBP Bromodomain …
Nov 5, 2024 · EP300/CBP inhibition causes cell cycle arrest and apoptosis in multiple myeloma (MM) models through concomitant suppression of interferon regulatory factor 4 (IRF4) and MYC, highlighting the rationale for targeting EP300/CBP as a novel therapy for MM.
Genetic dysregulation of EP300 in cancers in light of cancer …
In this review, we describe the role of p300 in cancer initiation and progression regarding EP300 aberrations that have been identified in TGCA Pan-Cancer Atlas studies and we also discuss possible anticancer strategies that target EP300 mutated cancers.
Molecular Characterization of EP300 Mutant Myeloid Neoplasia
Nov 13, 2019 · EP300 (22q13.2) encodes the adenovirus E1A associated cellular p300 transcriptional co-activator protein with lysine acetyltransferase activity as does its paralog CBP (16p13.3). Ablation of EP300 in mice results in embryonic lethality.
In silico analysis reveals EP300 as a panCancer inhibitor of
Jun 10, 2020 · In panCancer analyses anti-tumor immune activity was increased in EP300 mutated esophageal, stomach and prostate cancers. Downregulation of EP300 gene expression was associated with higher...
Therapeutic targeting of EP300/CBP by bromodomain inhibition in ...
Dec 11, 2023 · CCS1477 (inobrodib) is a potent, selective EP300/CBP bromodomain inhibitor which induces cell-cycle arrest and differentiation in hematologic malignancy model systems.
Tumour suppressor EP300, a modulator of paclitaxel ... - Springer
Mar 24, 2017 · We used lentiviruses expressing EP300-targeting shRNA to downregulate its expression in MCF-7 cells as well as an EP300 -knocked-out colon carcinoma cell line. An EP300-expression plasmid was used to upregulate its expression in basal-like CAL51 and MDA-MB-231 breast cancer cells.