[HTML][HTML] Breaking free from the crystal lattice: Structural biology in solution to study protein degraders

K Haubrich, VA Spiteri, W Farnaby, F Sobott… - Current Opinion in …, 2023 - Elsevier
Structural biology offers a versatile arsenal of techniques and methods to investigate the
structure and conformational dynamics of proteins and their assemblies. The growing field of …

Targeting DCAF5 suppresses SMARCB1-mutant cancer by stabilizing SWI/SNF

S Radko-Juettner, H Yue, JA Myers, RD Carter… - Nature, 2024 - nature.com
Whereas oncogenes can potentially be inhibited with small molecules, the loss of tumour
suppressors is more common and is problematic because the tumour-suppressor proteins …

Methods to characterize and discover molecular degraders in cells

Z Lin, CM Woo - Chemical Society Reviews, 2022 - pubs.rsc.org
Cells use many post-translational modifications (PTMs) to tailor proteins and transduce
cellular signals. Recent years have witnessed the rapid growth of small molecule and …

An intramolecular bivalent degrader glues an intrinsic BRD4-DCAF16 interaction

O Hsia - 2023 - dlib.hust.edu.vn
Targeted protein degradation is a drug modality represented by compounds that recruit a
target to an E3 ubiquitin ligase to promote target ubiquitination and proteasomal …

Targeted protein degradation as an antiviral approach

A Chakravarty, PL Yang - Antiviral research, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a new modality in drug discovery. In
this approach, small molecules are used to drive degradation of the target protein of interest …

The application of ubiquitin ligases in the PROTAC drug design

Y Chen, J Jin - Acta Biochimica et Biophysica Sinica, 2020 - academic.oup.com
Protein ubiquitylation plays important roles in many biological activities. Protein
ubiquitylation is a unique process that is mainly controlled by ubiquitin ligases. The ubiquitin …

Emerging strategies for prospective discovery of molecular glue degraders

B Wang, S Cao, N Zheng - Current Opinion in Structural Biology, 2024 - Elsevier
Molecular glue (MG) degraders are monovalent small molecule compounds that co-opt E3
ubiquitin ligases to target neo-substrates for proteasomal degradation. Here, we provide a …

Covalent fragment-based ligand screening approaches for identification of novel ubiquitin proteasome system modulators

EM Rothweiler, PE Brennan, KVM Huber - Biological Chemistry, 2022 - degruyter.com
Ubiquitination is a key regulatory mechanism vital for maintenance of cellular homeostasis.
Protein degradation is induced by E3 ligases via attachment of ubiquitin chains to …

Unlocking DCAFs To Catalyze Degrader Development: An Arena for Innovative Approaches

Q Miao, VD Kadam, A Mukherjee, Z Tan… - Journal of Medicinal …, 2023 - ACS Publications
Chemically induced proximity-based targeted protein degradation (TPD) has become a
prominent paradigm in drug discovery. With the clinical benefit demonstrated by certain …

Targeted protein degradation via intramolecular bivalent glues

O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida… - Nature, 2024 - nature.com
Targeted protein degradation is a pharmacological modality that is based on the induced
proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and …