KAT6A and ENL form an epigenetic transcriptional control module to drive critical leukemogenic gene-expression programs
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 …
an oncogenic state of differentiation arrest. To identify key epigenetic regulators of AML cell …
Pharmacological targeting of the cancer epigenome
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …
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
Gene editing has great potential in treating diseases caused by well-characterized
molecular alterations. The introduction of clustered regularly interspaced short palindromic …
molecular alterations. The introduction of clustered regularly interspaced short palindromic …
Current approaches in CRISPR-Cas9 mediated gene editing for biomedical and therapeutic applications
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 …
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 …
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
Chromatin regulation involves the selective recruitment of chromatin factors to facilitate DNA
repair, replication and transcription. Here we demonstrate the utility of coupling unbiased …
repair, replication and transcription. Here we demonstrate the utility of coupling unbiased …
[HTML][HTML] Proteotoxicity from aberrant ribosome biogenesis compromises cell fitness
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 …
proteins) and RNAs (rRNAs) to produce thousands of ribosomes every minute. Although …
Mammalian cell proliferation requires noncatalytic functions of O-GlcNAc transferase
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 …
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 …
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 …
and validate drug targets. An efficient strategy to achieve this involves expression of a …