Conditional degrons for controlling protein expression at the protein level
T Natsume, MT Kanemaki - Annual Review of Genetics, 2017 - annualreviews.org
The conditional depletion of a protein of interest (POI) is useful not only for loss-of-function
studies, but also for the modulation of biological pathways. Technologies that work at the …
studies, but also for the modulation of biological pathways. Technologies that work at the …
Structure-guided development of YEATS domain inhibitors by targeting π-π-π stacking
Chemical probes of epigenetic 'readers' of histone post-translational modifications (PTMs)
have become powerful tools for mechanistic and functional studies of their target proteins in …
have become powerful tools for mechanistic and functional studies of their target proteins in …
MELK is not necessary for the proliferation of basal-like breast cancer cells
Thorough preclinical target validation is essential for the success of drug discovery efforts. In
this study, we combined chemical and genetic perturbants, including the development of a …
this study, we combined chemical and genetic perturbants, including the development of a …
Plasticity of the Cullin-RING ligase repertoire shapes sensitivity to ligand-induced protein degradation
Inducing protein degradation via small molecules is a transformative therapeutic paradigm.
Although structural requirements of target degradation are emerging, mechanisms …
Although structural requirements of target degradation are emerging, mechanisms …
Nucleosome turnover regulates histone methylation patterns over the genome
Recent studies have indicated that nucleosome turnover is rapid, occurring several times
per cell cycle. To access the effect of nucleosome turnover on the epigenetic landscape, we …
per cell cycle. To access the effect of nucleosome turnover on the epigenetic landscape, we …
Identification of a potent and selective covalent Pin1 inhibitor
BJ Pinch, ZM Doctor, B Nabet, CM Browne… - Nature chemical …, 2020 - nature.com
Peptidyl-prolyl cis/trans isomerase NIMA-interacting 1 (Pin1) is commonly overexpressed in
human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is …
human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is …
Target protein localization and its impact on PROTAC-mediated degradation
LM Simpson, L Glennie, A Brewer, JF Zhao… - Cell Chemical …, 2022 - cell.com
Proteolysis-targeting chimeras (PROTACs) bring a protein of interest (POI) into spatial
proximity of an E3 ubiquitin ligase, promoting POI ubiquitylation and proteasomal …
proximity of an E3 ubiquitin ligase, promoting POI ubiquitylation and proteasomal …
Targeted protein degradation tools: overview and future perspectives
Y Prozzillo, G Fattorini, MV Santopietro, L Suglia… - Biology, 2020 - mdpi.com
Simple Summary Gene inactivation is a powerful strategy to study the function of specific
proteins in the context of cellular physiology that can be applied for only non-essential …
proteins in the context of cellular physiology that can be applied for only non-essential …
Unleashing cell-intrinsic inflammation as a strategy to kill AML blasts
Leukemic blasts are immune cells gone awry. We hypothesized that dysregulation of
inflammatory pathways contributes to the maintenance of their leukemic state and can be …
inflammatory pathways contributes to the maintenance of their leukemic state and can be …
Rewiring the Epigenetic Networks in MLL-Rearranged Leukemias: Epigenetic Dysregulation and Pharmacological Interventions
Leukemias driven by chromosomal translocation of the mixed-lineage leukemia gene (MLL
or KMT2A) are highly prevalent in pediatric oncology. The poor survival rate and lack of an …
or KMT2A) are highly prevalent in pediatric oncology. The poor survival rate and lack of an …