Bromodomains: a new target class for drug development
AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
[HTML][HTML] Histone acetyltransferases CBP/p300 in tumorigenesis and CBP/p300 inhibitors as promising novel anticancer agents
Q Chen, B Yang, X Liu, XD Zhang, L Zhang, T Liu - Theranostics, 2022 - ncbi.nlm.nih.gov
The histone acetyltransferases CBP and p300, often referred to as CBP/p300 due to their
sequence homology and functional overlap and co-operation, are emerging as critical …
sequence homology and functional overlap and co-operation, are emerging as critical …
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 …
induces cell-cycle arrest and differentiation in hematologic malignancy model systems. In …
Current development of CBP/p300 inhibitors in the last decade
ZX He, BF Wei, X Zhang, YP Gong, LY Ma… - European Journal of …, 2021 - Elsevier
CBP/p300, functioning as histone acetyltransferases and transcriptional co-factors,
represents an attractive target for various diseases, including malignant tumor. The …
represents an attractive target for various diseases, including malignant tumor. The …
LPCAT3 is transcriptionally regulated by YAP/ZEB/EP300 and collaborates with ACSL4 and YAP to determine ferroptosis sensitivity
J Cui, Y Wang, X Tian, Y Miao, L Ma… - Antioxidants & redox …, 2023 - liebertpub.com
Aims: Lipid peroxidation occurring in lung adenocarcinoma (LUAD) cells leads to
ferroptosis. Lysophosphatidylcholine acyl-transferase 3 (LPCAT3) plays a key role in …
ferroptosis. Lysophosphatidylcholine acyl-transferase 3 (LPCAT3) plays a key role in …
A fast chemical reprogramming system promotes cell identity transition through a diapause-like state
Cellular reprogramming by only small molecules holds enormous potentials for regenerative
medicine. However, chemical reprogramming remains a slow process and labour intensive …
medicine. However, chemical reprogramming remains a slow process and labour intensive …
Epithelial-mesenchymal transition and metabolic switching in cancer: lessons from somatic cell reprogramming
Epithelial-mesenchymal transition (EMT) and its critical roles during cancer progression
have long been recognized and extensively reviewed. Recent studies on the generation of …
have long been recognized and extensively reviewed. Recent studies on the generation of …
CREB stimulates GPX4 transcription to inhibit ferroptosis in lung adenocarcinoma
Z Wang, X Zhang, X Tian, Y Yang, L Ma… - Oncology …, 2021 - spandidos-publications.com
Ferroptosis is a new form of regulated cell death and closely related to cancer. However, the
mechanism underlying the regulation of ferroptosis in lung adenocarcinoma (LUAD) …
mechanism underlying the regulation of ferroptosis in lung adenocarcinoma (LUAD) …
Enhancers are activated by p300/CBP activity-dependent PIC assembly, RNAPII recruitment, and pause release
T Narita, S Ito, Y Higashijima, WK Chu, K Neumann… - Molecular Cell, 2021 - cell.com
The metazoan-specific acetyltransferase p300/CBP is involved in activating signal-induced,
enhancer-mediated transcription of cell-type-specific genes. However, the global kinetics …
enhancer-mediated transcription of cell-type-specific genes. However, the global kinetics …
Identifying collagen VI as a target of fibrotic diseases regulated by CREBBP/EP300
LM Williams, FE McCann, MA Cabrita… - Proceedings of the …, 2020 - National Acad Sciences
Fibrotic diseases remain a major cause of morbidity and mortality, yet there are few effective
therapies. The underlying pathology of all fibrotic conditions is the activity of myofibroblasts …
therapies. The underlying pathology of all fibrotic conditions is the activity of myofibroblasts …