2017
DOI: 10.1038/srep39841
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Conformational transition of FGFR kinase activation revealed by site-specific unnatural amino acid reporter and single molecule FRET

Abstract: Protein kinases share significant structural similarity; however, structural features alone are insufficient to explain their diverse functions. Thus, bridging the gap between static structure and function requires a more detailed understanding of their dynamic properties. For example, kinase activation may occur via a switch-like mechanism or by shifting a dynamic equilibrium between inactive and active states. Here, we utilize a combination of FRET and molecular dynamics (MD) simulations to probe the activat… Show more

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Cited by 6 publications
(4 citation statements)
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“…Dysregulation of these signalling cascades leads to several developmental syndromes and a broad range of human malignancies (Dieci et al 2013 ; Katoh 2016 ). Structural and molecular dynamic properties of FGFRs are the subject of extensive study, as part of a mission to understand physiological and aberrant activation mechanisms as well as drug action (Chen et al 2017 ; Huang et al 2013 ; Klein et al 2015 ; Kobashigawa et al 2016 ; Patani et al 2016 ; Perdios et al 2017 ). To date, many kinase inhibitors have been developed and some have reached clinical trials (Zhang et al 2009 ).…”
Section: Biological Contextmentioning
confidence: 99%
“…Dysregulation of these signalling cascades leads to several developmental syndromes and a broad range of human malignancies (Dieci et al 2013 ; Katoh 2016 ). Structural and molecular dynamic properties of FGFRs are the subject of extensive study, as part of a mission to understand physiological and aberrant activation mechanisms as well as drug action (Chen et al 2017 ; Huang et al 2013 ; Klein et al 2015 ; Kobashigawa et al 2016 ; Patani et al 2016 ; Perdios et al 2017 ). To date, many kinase inhibitors have been developed and some have reached clinical trials (Zhang et al 2009 ).…”
Section: Biological Contextmentioning
confidence: 99%
“…In the context of dual labeling, FlAsH has been combined with amber suppression (Perdios et al . 2017) (Fig. 14 b ) or fluorescent proteins such as CFP (Hoffmann et al .…”
Section: Protein Engineering Approaches For Tackling Outstanding Chalmentioning
confidence: 99%
“…( b ) The FlAsH labeling system can be used for the selective modification of a genetically encoded peptide tag, in combination with amber suppression (Perdios et al . 2017). ( c ) A dual labeling strategy based on native chemical ligation and amber suppression (Wissner et al .…”
Section: Protein Engineering Approaches For Tackling Outstanding Chalmentioning
confidence: 99%
“…In addition, nonsense suppression is technically challenging, especially in eukaryotic cells, as it requires the introduction of an engineered tRNA/tRNA-synthetase pair, addition of a cell-permeable unnatural amino acid, and mutation of the gene of interest. Although the modification of eukaryotic transmembrane proteins with Amber suppression technology has been achieved, photo-BOLT has not yet been applied to receptors or ion channels. However, as the technology becomes increasingly popular, it is likely that these applications will emerge.…”
mentioning
confidence: 99%