The role of CREBBP/EP300 and its therapeutic implications in hematological malignancies

Y Zhu, Z Wang, Y Li, H Peng, J Liu, J Zhang, X Xiao - Cancers, 2023 - mdpi.com
Simple Summary Through their regulatory effects on gene expression, histone
acetyltransferases have been implicated in the normal physiological activities and genesis …

Bromodomain inhibitors and therapeutic applications

BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

Recent advances on small-molecule bromodomain-containing histone acetyltransferase inhibitors

M Liu, K Zhang, Q Li, H Pang, Z Pan… - Journal of Medicinal …, 2023 - ACS Publications
In recent years, substantial research has been conducted on molecular mechanisms and
inhibitors targeting bromodomains (BRDs) and extra-terminal (BET) family proteins. On this …

Design, synthesis, and biological evaluation of 1-(indolizin-3-yl) ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer

Q Xiang, C Wang, T Wu, C Zhang, Q Hu… - Journal of Medicinal …, 2021 - ACS Publications
CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential
target for prostate cancer treatment. Herein, we report the structural optimization of a series …

Characteristics of anticancer activity of CBP/p300 inhibitors–Features of their classes, intracellular targets and future perspectives of their application in cancer …

M Strachowska, A Robaszkiewicz - Pharmacology & Therapeutics, 2024 - Elsevier
Due to the contribution of highly homologous acetyltransferases CBP and p300 to
transcription elevation of oncogenes and other cancer promoting factors, these enzymes …

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 …

Targeting bromodomain-containing proteins: Research advances of drug discovery

Z Pan, Y Zhao, X Wang, X Xie, M Liu, K Zhang… - Molecular …, 2023 - Springer
Bromodomain (BD) is an evolutionarily conserved protein module found in 46 different BD-
containing proteins (BCPs). BD acts as a specific reader for acetylated lysine residues (KAc) …

Exploring the landscape of post-translational modification in drug discovery

Y Cao, T Yu, Z Zhu, Y Zhang, S Sun, N Li, C Gu… - Pharmacology & …, 2024 - Elsevier
Post-translational modifications (PTMs) play a crucial role in regulating protein function, and
their dysregulation is frequently associated with various diseases. The emergence of …

Discovery of a potent and selective CBP bromodomain inhibitor (Y08262) for treating acute myeloid leukemia

Q Xiang, T Wu, C Zhang, C Wang, H Xu, Q Hu, J Hu… - Bioorganic …, 2024 - Elsevier
The bromodomain of CREB (cyclic-AMP response element binding protein) binding protein
(CBP) is an epigenetic “reader” and plays a key role in transcriptional regulation. CBP …

Synthesis of Spiro[chromene-imidazo[1,2-a]pyridin]-3′-imines via 6-exo-dig Cyclization Reaction

B Nayebzadeh, K Amiri, H Khosravi… - The Journal of …, 2021 - ACS Publications
A transition-metal-free postmodification of the Groebke–Blackburn–Bienaymé (GBB)
reaction for the synthesis of spiro [chromene-imidazo [1, 2-a] pyridin]-3′-imine was …