[HTML][HTML] Group 3 medulloblastoma transcriptional networks collapse under domain specific EP300/CBP inhibition

NAM Shendy, M Bikowitz, LH Sigua, Y Zhang… - Nature …, 2024 - nature.com
Chemical discovery efforts commonly target individual protein domains. Many proteins,
including the EP300/CBP histone acetyltransferases (HATs), contain several targetable …

Antitumor activity of the dual BET and CBP/EP300 inhibitor NEO2734

F Spriano, E Gaudio, L Cascione, C Tarantelli… - Blood …, 2020 - ashpublications.org
Bromodomain and extra-terminal domain (BET) proteins, cyclic adenosine monophosphate
response element-binding protein (CBP), and the E1A-binding protein of p300 (EP300) are …

[PDF][PDF] Identification of selective CBP degraders with robust preclinical PK, PD, efficacy and safety across solid tumor indications

D Sappal, B Adams, K Adhikari, W Austin… - Cancer …, 2024 - foghorntx.com
CREB binding protein (CBP) and E1A binding protein p300 (EP300) are paralog histone
acetyltransferases involved in many cellular processes via their activity as transcription …

Development of selective CBP/P300 benzoxazepine bromodomain inhibitors

TA Popp, C Tallant, C Rogers, O Fedorov… - Journal of Medicinal …, 2016 - ACS Publications
CBP (CREB (cAMP responsive element binding protein) binding protein (CREBBP)) and
P300 (adenovirus E1A-associated 300 kDa protein) are two closely related histone …

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

LM Lasko, CG Jakob, RP Edalji, W Qiu, D Montgomery… - Nature, 2017 - nature.com
The dynamic and reversible acetylation of proteins, catalysed by histone acetyltransferases
(HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of …

Fragment-based discovery of a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor (CPI-637)

AM Taylor, A Côté, MC Hewitt, R Pastor… - ACS Medicinal …, 2016 - ACS Publications
CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators
involved in numerous cellular pathways relevant to oncology. As part of our effort to explore …

Knocking off cancer's HAT: CSS1477 disrupts oncogenic programs

LK Xu, P Ntziachristos - Cell Chemical Biology, 2023 - cell.com
EP300/CBP are histone acetyltransferases recruited onto chromatin by oncogenic
transcription factors and control the transcriptional program via their activity in enhancer …

Active medulloblastoma enhancers reveal subgroup-specific cellular origins

CY Lin, S Erkek, Y Tong, L Yin, AJ Federation… - Nature, 2016 - nature.com
Medulloblastoma is a highly malignant paediatric brain tumour, often inflicting devastating
consequences on the developing child. Genomic studies have revealed four distinct …

[HTML][HTML] The whole-genome landscape of medulloblastoma subtypes

PA Northcott, I Buchhalter, AS Morrissy, V Hovestadt… - Nature, 2017 - nature.com
Current therapies for medulloblastoma, a highly malignant childhood brain tumour, impose
debilitating effects on the developing child, and highlight the need for molecularly targeted …

[HTML][HTML] The BET inhibitor OTX015 exhibits in vitro and in vivo antitumor activity in pediatric ependymoma stem cell models

T Servidei, D Meco, M Martini, A Battaglia… - International journal of …, 2021 - mdpi.com
Childhood ependymomas are heterogenous chemoresistant neoplasms arising from
aberrant stem-like cells. Epigenome deregulation plays a pivotal role in ependymoma …