Hitting a Moving Target: Targeting Transient Protein States

In this issue of Structure, Bista and colleagues report that inhibitors of the MDM2/p53 interaction can be designed to interact with a transiently folded α-helical segment of the MDM2 lid region. This suggests that targeting transient protein states in PPI inhibitor design could be a promising strat...

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Veröffentlicht in:	Structure (London) 2013-12, Vol.21 (12), p.2095-2097
Hauptverfasser:	Bauer, Matthias R., Boeckler, Frank M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Affinity Dipeptides - chemistry Humans Hydroxamic Acids - chemistry Inhibitors Moving targets Proteins Proto-Oncogene Proteins c-mdm2 - chemistry Segments Selectivity Strategy Tryptophan - analogs & derivatives Tryptophan - chemistry Tumor Suppressor Protein p53 - chemistry
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Beschreibung
Zusammenfassung:	In this issue of Structure, Bista and colleagues report that inhibitors of the MDM2/p53 interaction can be designed to interact with a transiently folded α-helical segment of the MDM2 lid region. This suggests that targeting transient protein states in PPI inhibitor design could be a promising strategy to improve affinity and/or selectivity profiles.
ISSN:	0969-2126 1878-4186
DOI:	10.1016/j.str.2013.11.003