The path to venetoclax resistance is paved with mutations, metabolism, and more

GP Sullivan, L Flanagan, DA Rodrigues… - Science Translational …, 2022 - science.org
Venetoclax is a B cell lymphoma 2 (BCL-2)–selective antagonist used to treat chronic
lymphocytic leukemia (CLL) and acute myelogenous leukemia (AML). Although this has …

Addressing transcriptional dysregulation in cancer through CDK9 inhibition

MA Toure, AN Koehler - Biochemistry, 2023 - ACS Publications
Undermining transcriptional addiction, the dependence of cancers on selected
transcriptional programs, is critically important for addressing cancers with high unmet …

Targeting CDK9 with selective inhibitors or degraders in tumor therapy: an overview of recent developments

L Xiao, Y Liu, H Chen, L Shen - Cancer Biology & Therapy, 2023 - Taylor & Francis
As a catalytic subunit of the positive transcription elongation factor b (P-TEFb), cyclin-
dependent kinase 9 (CDK9) has been demonstrated to contribute to carcinogenesis. This …

[HTML][HTML] Targeting YTHDF2 inhibits tumorigenesis of diffuse large B-cell lymphoma through ACER2-mediated ceramide catabolism

X Chen, T Lu, M Ding, Y Cai, Z Yu, X Zhou… - Journal of Advanced …, 2024 - Elsevier
Introduction Epigenetic alterations play crucial roles in diffuse large B-cell lymphoma
(DLBCL). Disturbances in lipid metabolism contribute to tumor progression. However …

Relapsed acute myeloid leukemia in children and adolescents: current treatment options and future strategies

S Zarnegar-Lumley, KJ Caldwell, JE Rubnitz - Leukemia, 2022 - nature.com
Pediatric acute myeloid leukemia (AML) develops from clonal expansion of hematopoietic
precursor cells and is characterized by morphologic and cytomolecular heterogeneity …

Transcriptional cyclin-dependent kinases: Potential drug targets in cancer therapy

Y Liu, L Fu, J Wu, M Liu, G Wang, B Liu… - European Journal of …, 2022 - Elsevier
In the wake of the development of the concept of cell cycle and its limiting points, cyclin-
dependent kinases (CDKs) are considered to play a central role in regulating cell cycle …

Targeting OXPHOS de novo purine synthesis as the nexus of FLT3 inhibitor–mediated synergistic antileukemic actions

P Zhang, LT Brinton, M Gharghabi, S Sher… - Science …, 2022 - science.org
Using a genome-wide CRISPR screen, we identified CDK9, DHODH, and PRMT5 as
synthetic lethal partners with gilteritinib treatment in fms-like tyrosine kinase 3 (FLT3) …

Tipping the balance: toward rational combination therapies to overcome venetoclax resistance in mantle cell lymphoma

YJ Thus, E Eldering, AP Kater, M Spaargaren - Leukemia, 2022 - nature.com
Mantle cell lymphoma (MCL), an aggressive, but incurable B-cell lymphoma, is genetically
characterized by the t (11; 14) translocation, resulting in the overexpression of Cyclin D1. In …

Oncogenic dysregulation of pre‐mRNA processing by protein kinases: challenges and therapeutic opportunities

C Naro, P Bielli, C Sette - The FEBS Journal, 2021 - Wiley Online Library
Alternative splicing and polyadenylation represent two major steps in pre‐mRNA‐
processing, which ensure proper gene expression and diversification of human …

Ceramide-induced integrated stress response overcomes Bcl-2 inhibitor resistance in acute myeloid leukemia

AC Lewis, VS Pope, MN Tea, M Li… - Blood, The Journal …, 2022 - ashpublications.org
Inducing cell death by the sphingolipid ceramide is a potential anticancer strategy, but the
underlying mechanisms remain poorly defined. In this study, triggering an accumulation of …