Essays in biochemistry, 2017-11, Vol.61 (5), p.543-560
2017
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- Autor(en) / Beteiligte
- Titel
- The potential of cryo-electron microscopy for structure-based drug design
- Ist Teil von
- Essays in biochemistry, 2017-11, Vol.61 (5), p.543-560
- Ort / Verlag
- England
- Erscheinungsjahr
- 2017
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Structure-based drug design plays a central role in therapeutic development. Until recently, protein crystallography and NMR have dominated experimental approaches to obtain structural information of biological molecules. However, in recent years rapid technical developments in single particle cryo-electron microscopy (cryo-EM) have enabled the determination to near-atomic resolution of macromolecules ranging from large multi-subunit molecular machines to proteins as small as 64 kDa. These advances have revolutionized structural biology by hugely expanding both the range of macromolecules whose structures can be determined, and by providing a description of macromolecular dynamics. Cryo-EM is now poised to similarly transform the discipline of structure-based drug discovery. This article reviews the potential of cryo-EM for drug discovery with reference to protein ligand complex structures determined using this technique.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0071-1365eISSN: 1744-1358DOI: 10.1042/ebc20170032Titel-ID: cdi_pubmed_primary_29118099
- Format
- –
- Schlagworte
- Animals, Cryoelectron Microscopy - instrumentation, Cryoelectron Microscopy - methods, Crystallography, X-Ray, Drug Design, Drug Discovery, Escherichia coli - chemistry, Humans, Ligands, Models, Molecular, Multiprotein Complexes - agonists, Multiprotein Complexes - antagonists & inhibitors, Multiprotein Complexes - chemistry, Proteins - agonists, Proteins - antagonists & inhibitors, Proteins - chemistry, Saccharomyces cerevisiae - chemistry, Small Molecule Libraries - chemical synthesis, Small Molecule Libraries - chemistry, Structure-Activity Relationship