Cryo-EM in drug discovery: achievements, limitations and prospects

JP Renaud, A Chari, C Ciferri, W Liu… - Nature reviews Drug …, 2018 - nature.com
Cryo-electron microscopy (cryo-EM) of non-crystalline single particles is a biophysical
technique that can be used to determine the structure of biological macromolecules and …

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

K Gao, R Oerlemans, MR Groves - Biophysical reviews, 2020 - Springer
Differential scanning fluorimetry (DSF) is an accessible, rapid, and economical biophysical
technique that has seen many applications over the years, ranging from protein folding state …

Targeting a neoantigen derived from a common TP53 mutation

EHC Hsiue, KM Wright, J Douglass, MS Hwang… - Science, 2021 - science.org
INTRODUCTION TP53 (tumor protein P53), a tumor suppressor gene, is the most commonly
mutated cancer-driver gene. Nevertheless, drugs that target mutant p53, the protein product …

Structural stability of SARS-CoV-2 3CLpro and identification of quercetin as an inhibitor by experimental screening

O Abian, D Ortega-Alarcon, A Jimenez-Alesanco… - International journal of …, 2020 - Elsevier
The global health emergency generated by coronavirus disease 2019 (COVID-19) has
prompted the search for preventive and therapeutic treatments for its pathogen, the severe …

Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil

S Omoto, V Speranzini, T Hashimoto, T Noshi… - Scientific reports, 2018 - nature.com
Baloxavir acid (BXA), derived from the prodrug baloxavir marboxil (BXM), potently and
selectively inhibits the cap-dependent endonuclease within the polymerase PA subunit of …

The cellular thermal shift assay for evaluating drug target interactions in cells

R Jafari, H Almqvist, H Axelsson, M Ignatushchenko… - Nature protocols, 2014 - nature.com
Thermal shift assays are used to study thermal stabilization of proteins upon ligand binding.
Such assays have been used extensively on purified proteins in the drug discovery industry …

A primer to single-particle cryo-electron microscopy

Y Cheng, N Grigorieff, PA Penczek, T Walz - Cell, 2015 - cell.com
Cryo-electron microscopy (cryo-EM) of single-particle specimens is used to determine the
structure of proteins and macromolecular complexes without the need for crystals. Recent …

Analysis of protein stability and ligand interactions by thermal shift assay

K Huynh, CL Partch - Current protocols in protein science, 2015 - Wiley Online Library
Purification of recombinant proteins for biochemical assays and structural studies is time‐
consuming and presents inherent difficulties that depend on the optimization of protein …

Structural and mechanistic insights into 5-lipoxygenase inhibition by natural products

NC Gilbert, J Gerstmeier, EE Schexnaydre… - Nature chemical …, 2020 - nature.com
Leukotrienes (LT) are lipid mediators of the inflammatory response that are linked to asthma
and atherosclerosis. LT biosynthesis is initiated by 5-lipoxygenase (5-LOX) with the …

[PDF][PDF] Protein stability: a crystallographer's perspective

MC Deller, L Kong, B Rupp - Acta Crystallographica Section F …, 2016 - journals.iucr.org
Protein stability is a topic of major interest for the biotechnology, pharmaceutical and food
industries, in addition to being a daily consideration for academic researchers studying …