The time and place for nature in drug discovery
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 screening, but how and why biomimetic molecules, especially those …
Natural product-based proteolysis targeting chimeras (PROTACs)
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 …
They possess this property as they are produced by biosynthetic enzymes and are …
Mechanism of degrader-targeted protein ubiquitinability
Small-molecule degraders of disease-driving proteins offer a clinically proven modality with
enhanced therapeutic efficacy and potential to tackle previously undrugged targets. Stable …
enhanced therapeutic efficacy and potential to tackle previously undrugged targets. Stable …
Native Mass Spectrometry: Insights and Opportunities for Targeted Protein Degradation
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 …
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
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 …
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
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 …
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 …
(MPs), yet challenges remain in solubilizing and stabilizing their native conformations while …
[HTML][HTML] Traversing the drug discovery landscape using native mass spectrometry
Highlights•Unravelling the modulation of biochemical pathways by drug candidates.•
Characterising target-small molecule interactions on rapid timescales.•Capturing desirable …
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 …
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 …
(proteolysis-targeting chimeras) in clinical trials and molecular glues such as …