Acute BAF perturbation causes immediate changes in chromatin accessibility
Abstract Cancer-associated, loss-of-function mutations in genes encoding subunits of the
BRG1/BRM-associated factor (BAF) chromatin-remodeling complexes,,,,,,–often cause …
BRG1/BRM-associated factor (BAF) chromatin-remodeling complexes,,,,,,–often cause …
Targeting transcription cycles in cancer
SJ Vervoort, JR Devlin, N Kwiatkowski, M Teng… - Nature Reviews …, 2022 - nature.com
Accurate control of gene expression is essential for normal development and dysregulation
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …
of transcription underpins cancer onset and progression. Similar to cell cycle regulation …
[HTML][HTML] Proteomic discovery of chemical probes that perturb protein complexes in human cells
Most human proteins lack chemical probes, and several large-scale and generalizable small-
molecule binding assays have been introduced to address this problem. How compounds …
molecule binding assays have been introduced to address this problem. How compounds …
A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader
Heterobifunctional molecules that recruit E3 ubiquitin ligases, such as cereblon, for targeted
protein degradation represent an emerging pharmacological strategy. A major unanswered …
protein degradation represent an emerging pharmacological strategy. A major unanswered …
[HTML][HTML] CRISPR/Cas9 for cancer research and therapy
CRISPR/Cas9 has become a powerful method for making changes to the genome of many
organisms. First discovered in bacteria as part of an adaptive immune system …
organisms. First discovered in bacteria as part of an adaptive immune system …
Chemically induced proximity in biology and medicine
BZ Stanton, EJ Chory, GR Crabtree - Science, 2018 - science.org
BACKGROUND Nature has evolved elegant mechanisms to regulate the physical distance
between molecules, or proximity, for a wide variety of purposes. Whether it is activation of …
between molecules, or proximity, for a wide variety of purposes. Whether it is activation of …
Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex
DE Bussiere, L Xie, H Srinivas, W Shu, A Burke… - Nature Chemical …, 2020 - nature.com
The anticancer agent indisulam inhibits cell proliferation by causing degradation of RBM39,
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …
an essential mRNA splicing factor. Indisulam promotes an interaction between RBM39 and …
Targeted protein degradation: from chemical biology to drug discovery
PM Cromm, CM Crews - Cell chemical biology, 2017 - cell.com
Traditional pharmaceutical drug discovery is almost exclusively focused on directly
controlling protein activity to cure diseases. Modulators of protein activity, especially …
controlling protein activity to cure diseases. Modulators of protein activity, especially …
[HTML][HTML] Hotspot mutations in the structured ENL YEATS domain link aberrant transcriptional condensates and cancer
Growing evidence suggests prevalence of transcriptional condensates on chromatin, yet
their mechanisms of formation and functional significance remain largely unclear. In human …
their mechanisms of formation and functional significance remain largely unclear. In human …
Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …