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 …
Matrin3 mediates differentiation through stabilizing chromatin loop-domain interactions and YY1 mediated enhancer-promoter interactions
Although emerging evidence indicates that alterations in proteins within nuclear
compartments elicit changes in chromosomal architecture and differentiation, the underlying …
compartments elicit changes in chromosomal architecture and differentiation, the underlying …
Acetyl-CoA biosynthesis drives resistance to histone acetyltransferase inhibition
TR Bishop, C Subramanian, EM Bilotta… - Nature chemical …, 2023 - nature.com
Histone acetyltransferases (HATs) are implicated as both oncogene and nononcogene
dependencies in diverse human cancers. Acetyl-CoA-competitive HAT inhibitors have …
dependencies in diverse human cancers. Acetyl-CoA-competitive HAT inhibitors have …
Precision Medicine Approaches in Acute Myeloid Leukemia with Adverse Genetics
N Santoro, P Salutari, M Di Ianni, A Marra - International Journal of …, 2024 - mdpi.com
The treatment of acute myeloid leukemia (AML) with adverse genetics remains
unsatisfactory, with very low response rates to standard chemotherapy and shorter durations …
unsatisfactory, with very low response rates to standard chemotherapy and shorter durations …
A longitudinal single-cell atlas of treatment response in pediatric AML
Pediatric acute myeloid leukemia (pAML) is characterized by heterogeneous cellular
composition, driver alterations and prognosis. Characterization of this heterogeneity and …
composition, driver alterations and prognosis. Characterization of this heterogeneity and …
Transcriptional plasticity drives leukemia immune escape
Relapse of acute myeloid leukemia (AML) after allogeneic bone marrow transplantation has
been linked to immune evasion due to reduced expression of major histocompatibility …
been linked to immune evasion due to reduced expression of major histocompatibility …
High-efficiency knock-in of degradable tags (dTAG) at endogenous loci in cell lines
The dTAG system is a versatile strategy for tunable control of protein abundance and
facilitates the time-resolved assessment of disease-associated protein function. A “co-opted” …
facilitates the time-resolved assessment of disease-associated protein function. A “co-opted” …
The ncBAF complex regulates transcription in AML through H3K27ac sensing by BRD9
The non-canonical BAF complex (ncBAF) subunit BRD9 is essential for acute myeloid
leukemia (AML) cell viability but has an unclear role in leukemogenesis. Because BRD9 is …
leukemia (AML) cell viability but has an unclear role in leukemogenesis. Because BRD9 is …
[HTML][HTML] Leukemia core transcriptional circuitry is a sparsely interconnected hierarchy stabilized by incoherent feed-forward loops
Lineage-defining transcription factors form densely interconnected circuits in chromatin
occupancy assays, but the functional significance of these networks remains underexplored …
occupancy assays, but the functional significance of these networks remains underexplored …
[HTML][HTML] Rapid-kinetics degron benchmarking reveals off-target activities and mixed agonism-antagonism of MYB inhibitors
Attenuating aberrant transcriptional circuits holds great promise for the treatment of
numerous diseases, including cancer. However, development of transcriptional inhibitors is …
numerous diseases, including cancer. However, development of transcriptional inhibitors is …