Acute BAF perturbation causes immediate changes in chromatin accessibility

S Schick, S Grosche, KE Kohl, D Drpic, MG Jaeger… - Nature …, 2021 - nature.com
Abstract Cancer-associated, loss-of-function mutations in genes encoding subunits of the
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 …

[HTML][HTML] Proteomic discovery of chemical probes that perturb protein complexes in human cells

MR Lazear, JR Remsberg, MG Jaeger, K Rothamel… - Molecular cell, 2023 - cell.com
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 …

A chemoproteomic approach to query the degradable kinome using a multi-kinase degrader

HT Huang, D Dobrovolsky, J Paulk, G Yang… - Cell chemical …, 2018 - cell.com
Heterobifunctional molecules that recruit E3 ubiquitin ligases, such as cereblon, for targeted
protein degradation represent an emerging pharmacological strategy. A major unanswered …

[HTML][HTML] CRISPR/Cas9 for cancer research and therapy

T Zhan, N Rindtorff, J Betge, MP Ebert… - Seminars in cancer …, 2019 - Elsevier
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 …

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 …

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 …

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 …

[HTML][HTML] Hotspot mutations in the structured ENL YEATS domain link aberrant transcriptional condensates and cancer

L Song, X Yao, H Li, B Peng, AP Boka, Y Liu, G Chen… - Molecular cell, 2022 - cell.com
Growing evidence suggests prevalence of transcriptional condensates on chromatin, yet
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

B Nabet, FM Ferguson, BKA Seong, M Kuljanin… - Nature …, 2020 - nature.com
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …