Cryo-EM analyses of KIT and oncogenic mutants reveal structural oncogenic plasticity and a target for therapeutic intervention

SG Krimmer, N Bertoletti, Y Suzuki… - Proceedings of the …, 2023 - National Acad Sciences
… Here, we report cryo electron microscopy (cryo-EM) structural analyses of full-length wild-…
Mutational analysis of KIT reveals in D5 region an “Achilles heel” for therapeutic intervention. A …

Cryo-EM in drug discovery

T Ceska, CW Chung, R Cooke, C Phillips… - Biochemical Society …, 2019 - portlandpress.com
… of protein targets for therapeutic intervention, until relatively … suggest for this kind of analysis
is 4.2 Å for cryo-EM maps). The vast … , data collection and data analysis over previous years. …

Cryo-EM: the resolution revolution and drug discovery

TM de Oliveira, L van Beek, F Shilliday… - … the Science of Drug …, 2021 - journals.sagepub.com
… imaging analysis and the … cryo-EM has impacted drug discovery in diverse therapeutic
areas. Targets that have been brought into the realm of structure-based drug design by cryo-EM

Developments, applications, and prospects of cryoelectron microscopy

X Benjin, L Ling - Protein Science, 2020 - Wiley Online Library
… application of structural analysis based on cryo-EM more and … This new software can work
without user intervention to a … herpesvirus for targeted treatment. Wang et al.65 determined the …

Cryo-EM structures and atomic model of the HIV-1 strand transfer complex intasome

DO Passos, M Li, R Yang, SV Rebensburg… - Science, 2017 - science.org
cryoelectron microscopy (cryo-EM) structural analysis … than those used in our cryo-EM study
were reported to be … cannot completely exclude their involvement in tetrameric intasomes (…

Cryo-EM structures of NPC1L1 reveal mechanisms of cholesterol transport and ezetimibe inhibition

CS Huang, X Yu, P Fordstrom, K Choi, BC Chung… - Science …, 2020 - science.org
… The therapeutic interventions that reduce circulating cholesterol levels (5), such as statins …
detergent digitonin for cryo-EM analysis (fig. S1). We initially obtained a cryo-EM density map …

How cryo-EM is revolutionizing structural biology

XC Bai, G McMullan, SHW Scheres - Trends in biochemical sciences, 2015 - cell.com
… ] suggested that cryo-EM single-particle analysis could reach atomic resolution for
macromolecular complexes as small as 100 kDa. For many years, this prospect seemed overly …

Activation mechanism of the insulin receptor revealed by cryo-EM structure of the fully liganded receptor–ligand complex

E Uchikawa, E Choi, G Shang, H Yu, X Bai - Elife, 2019 - elifesciences.org
… Our structural and functional analyses indicate that binding of … for the eventual therapeutic
intervention of diseases caused … Our functional analyses indicate that site 1 and site 2 are both …

Cryo-EM: a unique tool for the visualization of macromolecular complexity

E Nogales, SHW Scheres - Molecular cell, 2015 - cell.com
… 3D cryo-electron microscopy (cryo-EM) is an expanding … Therefore, cryo-EM can be used
to investigate complete and … behind the cryo-EM methodology of single particle analysis and …

Cryo-EM structures of human RNA polymerase III in its unbound and transcribing states

M Girbig, AD Misiaszek, MK Vorländer… - Nature structural & …, 2021 - nature.com
… Here, we present cryo-electron microscopy structures at 2.8 to … that selectively target Pol III
for therapeutic interventions. … subjected our cryo-EM reconstructions to 3D variability analysis (…