Dysregulated haematopoietic stem cell behaviour in myeloid leukaemogenesis

M Yamashita, PV Dellorusso, OC Olson… - Nature Reviews …, 2020 - nature.com
Haematopoiesis is governed by haematopoietic stem cells (HSCs) that produce all lineages
of blood and immune cells. The maintenance of blood homeostasis requires a dynamic …

Clinical advances in targeting epigenetics for cancer therapy

S Feng, DD De Carvalho - The FEBS journal, 2022 - Wiley Online Library
The appropriate coordination between epigenetic regulators is essential for spatial and
temporal regulation of gene expression and maintenance of cell identity. Cancer is a …

BRD4 prevents the accumulation of R-loops and protects against transcription–replication collision events and DNA damage

FC Lam, YW Kong, Q Huang, TL Vu Han… - Nature …, 2020 - nature.com
Proper chromatin function and maintenance of genomic stability depends on spatiotemporal
coordination between the transcription and replication machinery. Loss of this coordination …

BET bromodomain inhibition rescues PD-1-mediated T-cell exhaustion in acute myeloid leukemia

M Zhong, R Gao, R Zhao, Y Huang, C Chen, K Li… - Cell death & …, 2022 - nature.com
Sustained expression of programmed cell death receptor-1 (PD-1) is correlated with the
exhaustion of T cells, and blockade of the PD-1 pathway is an effective immunotherapeutic …

First-in-human study of mivebresib (ABBV-075), an oral pan-inhibitor of bromodomain and extra terminal proteins, in patients with relapsed/refractory solid tumors

SA Piha-Paul, JC Sachdev, M Barve, P LoRusso… - Clinical Cancer …, 2019 - AACR
Purpose: Bromodomain and extraterminal (BET) proteins play important roles in
transcriptional regulation relevant to cancer pathogenesis, and therapeutic …

Functional analysis of the replication fork proteome identifies BET proteins as PCNA regulators

SR Wessel, KN Mohni, JW Luzwick, H Dungrawala… - Cell reports, 2019 - cell.com
Identifying proteins that function at replication forks is essential to understanding DNA
replication, chromatin assembly, and replication-coupled DNA repair mechanisms …

Make your best BET: The emerging role of BET inhibitor treatment in malignant tumors

O Bechter, P Schöffski - Pharmacology & therapeutics, 2020 - Elsevier
Bromodomains are protein-protein interaction modules with a great diversity in terms of
number of proteins and their function. The bromodomain and extraterminal protein (BET) …

Phase I results of bromodomain and Extra-terminal inhibitor PLX51107 in combination with azacitidine in patients with Relapsed/Refractory myeloid malignancies

J Senapati, WC Fiskus, N Daver, NR Wilson… - Clinical Cancer …, 2023 - AACR
Purpose: Treatment outcomes in patients with relapsed/refractory (R/R) myelodysplastic
syndrome (MDS) and acute myeloid leukemia (AML) remains dismal. On the basis of both …

A phase 1 study of the pan‐bromodomain and extraterminal inhibitor mivebresib (ABBV‐075) alone or in combination with venetoclax in patients with relapsed …

G Borthakur, O Odenike, I Aldoss, DA Rizzieri… - Cancer, 2021 - Wiley Online Library
Background Acute myeloid leukemia (AML) is a heterogenous malignancy driven by genetic
and epigenetic factors. Inhibition of bromodomain and extraterminal (BET) proteins …

NF-κB: a druggable target in acute myeloid leukemia

B Di Francesco, D Verzella, D Capece, D Vecchiotti… - Cancers, 2022 - mdpi.com
Simple Summary AML is a highly heterogeneous hematological disease and is the second
most common form of leukemia. Around 40% of AML patients display elevated nuclear NF …