A Synthetic Loop Replacement Peptide That Blocks Canonical NFâ κB Signaling
dc.contributor.author | Bruno, Paul A. | |
dc.contributor.author | Morriss‐andrews, Alex | |
dc.contributor.author | Henderson, Andrew R. | |
dc.contributor.author | Brooks, Charles L. | |
dc.contributor.author | Mapp, Anna K. | |
dc.date.accessioned | 2017-01-06T20:50:43Z | |
dc.date.available | 2018-01-08T19:47:52Z | en |
dc.date.issued | 2016-11-21 | |
dc.identifier.citation | Bruno, Paul A.; Morriss‐andrews, Alex ; Henderson, Andrew R.; Brooks, Charles L.; Mapp, Anna K. (2016). "A Synthetic Loop Replacement Peptide That Blocks Canonical NFâ κB Signaling." Angewandte Chemie 128(48): 15221-15225. | |
dc.identifier.issn | 0044-8249 | |
dc.identifier.issn | 1521-3757 | |
dc.identifier.uri | https://hdl.handle.net/2027.42/135091 | |
dc.description.abstract | Aberrant canonical NFâ κB signaling is implicated in diseases from autoimmune disorders to cancer. A major therapeutic challenge is the need for selective inhibition of the canonical pathway without impacting the many nonâ canonical NFâ κB functions. Here we show that a selective peptideâ based inhibitor of canonical NFâ κB signaling, in which a hydrogen bond in the NBD peptide is synthetically replaced by a nonâ labile bond, shows an about 10â fold increased potency relative to the original inhibitor. Not only is this molecule, NBD2, a powerful tool for dissection of canonical NFâ κB signaling in disease models and healthy tissues, the success of the synthetic loop replacement suggests that the general strategy could be useful for discovering modulators of the many proteinâ protein interactions mediated by such structures.Ein Peptidâ basierter Inhibitor für die kanonische NFâ κBâ Signalisierung, in dem eine Wasserstoffbrücke im NBDâ Peptid synthetisch durch eine nichtlabile Bindung ersetzt wurde, wirkt 10â mal stärker als der Originalinhibitor. Der Erfolg des Peptidschleifenaustauschs legt nahe, dass die Strategie nützlich sein könnte, um Modulatoren für viele durch solche Strukturen vermittelte Proteinâ Proteinâ Wechselwirkungen zu finden. | |
dc.publisher | Wiley Periodicals, Inc. | |
dc.subject.other | Inhibitoren | |
dc.subject.other | Peptidschleifen | |
dc.subject.other | Peptidmimetika | |
dc.subject.other | Protein-Protein-Wechselwirkungen | |
dc.subject.other | Medizinische Chemie | |
dc.title | A Synthetic Loop Replacement Peptide That Blocks Canonical NFâ κB Signaling | |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | |
dc.subject.hlbsecondlevel | Chemical Engineering | |
dc.subject.hlbsecondlevel | Chemistry | |
dc.subject.hlbsecondlevel | Materials Science and Engineering | |
dc.subject.hlbtoplevel | Engineering | |
dc.subject.hlbtoplevel | Science | |
dc.description.peerreviewed | Peer Reviewed | |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/135091/1/ange201607990-sup-0001-misc_information.pdf | |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/135091/2/ange201607990.pdf | |
dc.identifier.doi | 10.1002/ange.201607990 | |
dc.identifier.source | Angewandte Chemie | |
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dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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