The time and place for nature in drug discovery

RJ Young, SL Flitsch, M Grigalunas, PD Leeson… - Jacs Au, 2022 - ACS Publications
The case for a renewed focus on Nature in drug discovery is reviewed; not in terms of
natural product screening, but how and why biomimetic molecules, especially those …

Natural product-based proteolysis targeting chimeras (PROTACs)

M Liu, AP Martyn, RJ Quinn - Natural Product Reports, 2022 - pubs.rsc.org
Covering: upto 2022 Natural products have an embedded recognition of protein surfaces.
They possess this property as they are produced by biosynthetic enzymes and are …

Mechanism of degrader-targeted protein ubiquitinability

C Crowe, MA Nakasone, S Chandler, C Craigon… - Science …, 2024 - science.org
Small-molecule degraders of disease-driving proteins offer a clinically proven modality with
enhanced therapeutic efficacy and potential to tackle previously undrugged targets. Stable …

Native Mass Spectrometry: Insights and Opportunities for Targeted Protein Degradation

LM Sternicki, SA Poulsen - Analytical Chemistry, 2023 - ACS Publications
Native mass spectrometry (nMS) is one of the most powerful biophysical methods for the
direct observation of noncovalent protein interactions with both small molecules and other …

[HTML][HTML] Native mass spectrometry-directed drug discovery: Recent advances in investigating protein function and modulation

F Fiorentino, D Rotili, A Mai - Drug Discovery Today, 2023 - Elsevier
Native mass spectrometry (nMS) is a biophysical method for studying protein complexes and
can provide insights into subunit stoichiometry and composition, protein–ligand, and protein …

[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 …

Advances and challenges in preparing membrane proteins for native mass spectrometry

D Cheng, Y Guo, J Lyu, Y Liu, W Xu, W Zheng… - Biotechnology …, 2024 - Elsevier
Native mass spectrometry (nMS) is becoming a crucial tool for analyzing membrane proteins
(MPs), yet challenges remain in solubilizing and stabilizing their native conformations while …

[HTML][HTML] Traversing the drug discovery landscape using native mass spectrometry

HM Britt, CV Robinson - Current Opinion in Structural Biology, 2025 - Elsevier
Highlights•Unravelling the modulation of biochemical pathways by drug candidates.•
Characterising target-small molecule interactions on rapid timescales.•Capturing desirable …

Recent technological developments for native mass spectrometry

IK Webb - Biochimica et Biophysica Acta (BBA)-Proteins and …, 2022 - Elsevier
Native mass spectrometry (MS), the analysis of proteins and protein complexes from
solutions that stabilize native solution structures, is a rapidly expanding area. There is strong …

Targeted protein degradation in CNS disorders: a promising route to novel therapeutics?

S Kuemper, AG Cairns, K Birchall, Z Yao… - Frontiers in Molecular …, 2024 - frontiersin.org
Targeted protein degradation (TPD) is a rapidly expanding field, with various PROTACs
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …