Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway
Activation of nuclear factor-kappa B (NF-κB) and related upstream signal transduction pathways have long been associated with the pathogenesis of a variety of inflammatory diseases and has recently been implicated in the onset of cancer. This report provides a synthetic and compound-based property s...
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doaj-789311d353004329b484f281ae36bb752021-02-02T01:35:20ZengBeilstein-InstitutBeilstein Journal of Organic Chemistry1860-53972013-05-019190090710.3762/bjoc.9.1031860-5397-9-103Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathwayPaul M. Hershberger0Satyamaheshwar Peddibhotla1E. Hampton Sessions2Daniela B. Divlianska3Ricardo G. Correa4Anthony B. Pinkerton5John C. Reed6Gregory P. Roth7Conrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute at Lake Nona, 6400 Sanger Road Orlando, FL 32827, USAConrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute at Lake Nona, 6400 Sanger Road Orlando, FL 32827, USAConrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute at Lake Nona, 6400 Sanger Road Orlando, FL 32827, USAConrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute at Lake Nona, 6400 Sanger Road Orlando, FL 32827, USASanford-Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USASanford-Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USASanford-Burnham Medical Research Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USAConrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute at Lake Nona, 6400 Sanger Road Orlando, FL 32827, USAActivation of nuclear factor-kappa B (NF-κB) and related upstream signal transduction pathways have long been associated with the pathogenesis of a variety of inflammatory diseases and has recently been implicated in the onset of cancer. This report provides a synthetic and compound-based property summary of five pathway-related small-molecule chemical probes identified and optimized within the National Institutes of Health-Molecular Libraries Probe Center Network (NIH-MLPCN) initiative. The chemical probes discussed herein represent first-in-class, non-kinase-based modulators of the NF-κB signaling pathway, which were identified and optimized through either cellular phenotypic or specific protein-target-based screening strategies. Accordingly, the resulting new chemical probes may allow for better fundamental understanding of this highly complex biochemical signaling network and could advance future therapeutic translation toward the clinical setting.https://doi.org/10.3762/bjoc.9.103ML029ML130ML146ML236ML237 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Paul M. Hershberger Satyamaheshwar Peddibhotla E. Hampton Sessions Daniela B. Divlianska Ricardo G. Correa Anthony B. Pinkerton John C. Reed Gregory P. Roth |
spellingShingle |
Paul M. Hershberger Satyamaheshwar Peddibhotla E. Hampton Sessions Daniela B. Divlianska Ricardo G. Correa Anthony B. Pinkerton John C. Reed Gregory P. Roth Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway Beilstein Journal of Organic Chemistry ML029 ML130 ML146 ML236 ML237 |
author_facet |
Paul M. Hershberger Satyamaheshwar Peddibhotla E. Hampton Sessions Daniela B. Divlianska Ricardo G. Correa Anthony B. Pinkerton John C. Reed Gregory P. Roth |
author_sort |
Paul M. Hershberger |
title |
Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway |
title_short |
Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway |
title_full |
Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway |
title_fullStr |
Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway |
title_full_unstemmed |
Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway |
title_sort |
synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa b signaling pathway |
publisher |
Beilstein-Institut |
series |
Beilstein Journal of Organic Chemistry |
issn |
1860-5397 |
publishDate |
2013-05-01 |
description |
Activation of nuclear factor-kappa B (NF-κB) and related upstream signal transduction pathways have long been associated with the pathogenesis of a variety of inflammatory diseases and has recently been implicated in the onset of cancer. This report provides a synthetic and compound-based property summary of five pathway-related small-molecule chemical probes identified and optimized within the National Institutes of Health-Molecular Libraries Probe Center Network (NIH-MLPCN) initiative. The chemical probes discussed herein represent first-in-class, non-kinase-based modulators of the NF-κB signaling pathway, which were identified and optimized through either cellular phenotypic or specific protein-target-based screening strategies. Accordingly, the resulting new chemical probes may allow for better fundamental understanding of this highly complex biochemical signaling network and could advance future therapeutic translation toward the clinical setting. |
topic |
ML029 ML130 ML146 ML236 ML237 |
url |
https://doi.org/10.3762/bjoc.9.103 |
work_keys_str_mv |
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