KAT6A and ENL form an epigenetic transcriptional control module to drive critical leukemogenic gene-expression programs

F Yan, J Li, J Milosevic, R Petroni, S Liu, Z Shi, S Yuan… - Cancer discovery, 2022 - AACR
Epigenetic programs are dysregulated in acute myeloid leukemia (AML) and help enforce
an oncogenic state of differentiation arrest. To identify key epigenetic regulators of AML cell …

Pharmacological targeting of the cancer epigenome

NW Mabe, JA Perry, CF Malone, K Stegmaier - Nature Cancer, 2024 - nature.com
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …

[HTML][HTML] Integration of CRISPR/Cas9 with artificial intelligence for improved cancer therapeutics

AA Bhat, S Nisar, S Mukherjee, N Saha… - Journal of translational …, 2022 - Springer
Gene editing has great potential in treating diseases caused by well-characterized
molecular alterations. The introduction of clustered regularly interspaced short palindromic …

Current approaches in CRISPR-Cas9 mediated gene editing for biomedical and therapeutic applications

G Bhattacharjee, N Gohil, K Khambhati, I Mani… - Journal of Controlled …, 2022 - Elsevier
A single gene mutation can cause a number of human diseases that affect the quality of life.
Until the development of clustered regularly interspaced short palindromic repeats …

Targeted protein degradation and the enzymology of degraders

SL Fisher, AJ Phillips - Current opinion in chemical biology, 2018 - Elsevier
Targeted protein degradation is an emerging strategy for drug discovery that employs small
molecules to catalyze the ubiquitination of target proteins, ultimately causing their …

[HTML][HTML] CRISPR–ChIP reveals selective regulation of H3K79me2 by Menin in MLL leukemia

O Gilan, L Talarmain, CC Bell, D Neville… - Nature Structural & …, 2023 - nature.com
Chromatin regulation involves the selective recruitment of chromatin factors to facilitate DNA
repair, replication and transcription. Here we demonstrate the utility of coupling unbiased …

[HTML][HTML] Proteotoxicity from aberrant ribosome biogenesis compromises cell fitness

BW Tye, N Commins, LV Ryazanova, M Wühr… - elife, 2019 - elifesciences.org
To achieve maximal growth, cells must manage a massive economy of ribosomal proteins (r-
proteins) and RNAs (rRNAs) to produce thousands of ribosomes every minute. Although …

Mammalian cell proliferation requires noncatalytic functions of O-GlcNAc transferase

ZG Levine, SC Potter, CM Joiner… - Proceedings of the …, 2021 - National Acad Sciences
O-GlcNAc transferase (OGT), found in the nucleus and cytoplasm of all mammalian cell
types, is essential for cell proliferation. Why OGT is required for cell growth is not known …

[HTML][HTML] 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 …

Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader

H Tovell, A Testa, C Maniaci, H Zhou… - ACS chemical …, 2019 - ACS Publications
Inducing post-translational protein knockdown is an important approach to probe biology
and validate drug targets. An efficient strategy to achieve this involves expression of a …