Rubinstein-Taybi syndrome: a model of epigenetic disorder

J Van Gils, F Magdinier, P Fergelot, D Lacombe - Genes, 2021 - mdpi.com
The Rubinstein-Taybi syndrome (RSTS) is a rare congenital developmental disorder
characterized by a typical facial dysmorphism, distal limb abnormalities, intellectual …

CREB family transcription factors are major mediators of BDNF transcriptional autoregulation in cortical neurons

EE Esvald, J Tuvikene, A Sirp, S Patil… - Journal of …, 2020 - Soc Neuroscience
BDNF signaling via its transmembrane receptor TrkB has an important role in neuronal
survival, differentiation, and synaptic plasticity. Remarkably, BDNF is capable of modulating …

Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies

L Nicosia, GJ Spencer, N Brooks, FMR Amaral… - Cancer Cell, 2023 - cell.com
CCS1477 (inobrodib) is a potent, selective EP300/CBP bromodomain inhibitor which
induces cell-cycle arrest and differentiation in hematologic malignancy model systems. In …

Diagnosis and management in Rubinstein-Taybi syndrome: first international consensus statement

D Lacombe, A Bloch-Zupan, C Bredrup… - Journal of medical …, 2024 - jmg.bmj.com
Rubinstein-Taybi syndrome (RTS) is an archetypical genetic syndrome that is characterised
by intellectual disability, well-defined facial features, distal limb anomalies and atypical …

[HTML][HTML] Co-condensation between transcription factor and coactivator p300 modulates transcriptional bursting kinetics

L Ma, Z Gao, J Wu, B Zhong, Y Xie, W Huang, Y Lin - Molecular cell, 2021 - cell.com
The coactivator p300/CREB-binding protein (CBP) regulates genes by facilitating the
assembly of transcriptional machinery and by acetylating histones and other factors …

Discovery of exceptionally potent, selective, and efficacious PROTAC degraders of CBP and p300 proteins

JE Thomas, M Wang, W Jiang, M Wang… - Journal of Medicinal …, 2023 - ACS Publications
The histone acetyltransferase CREB-binding protein (CBP) and its paralogue p300 protein
are key transcriptional coactivators and attractive cancer therapeutic targets. We describe …

Transcriptional heterogeneity overcomes super-enhancer disrupting drug combinations in multiple myeloma

SJ Welsh, BG Barwick, EW Meermeier, DL Riggs… - Blood cancer …, 2024 - AACR
Multiple myeloma (MM) is a malignancy that is often driven by MYC and that is sustained by
IRF4, which are upregulated by super-enhancers. IKZF1 and IKZF3 bind to super-enhancers …

Stereo-and regiodefined DNA-encoded chemical libraries enable efficient tumour-targeting applications

N Favalli, G Bassi, C Pellegrino, J Millul, R De Luca… - Nature …, 2021 - nature.com
The encoding of chemical compounds with amplifiable DNA tags facilitates the discovery of
small-molecule ligands for proteins. To investigate the impact of stereo-and regiochemistry …

Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma

Q Chang, J Li, Y Deng, R Zhou, B Wang… - Journal of Medicinal …, 2024 - ACS Publications
Adenoviral E1A binding protein 300 kDa (p300) and its closely related paralog CREB
binding protein (CBP) are promising therapeutic targets for human cancer. Here, we report …

Acetyltransferases CBP/p300 Control Transcriptional Switch of β‐Catenin and Stat1 Promoting Osteoblast Differentiation

L Zhang, K Zhu, J Xu, X Chen, C Sheng… - Journal of Bone and …, 2023 - academic.oup.com
ABSTRACT CREB‐binding protein (CBP)(CREBBP) and p300 (EP300) are multifunctional
histone acetyltransferases (HATs) with extensive homology. Germline mutations of CBP or …