Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin

Autores
Vendrell Navarro, Gloria; Rúa, Federico; Bujons, Jordi; Brockmeyer, Andreas; Janning, Petra; Ziegler, Slava; Messeguer, Angel; Waldmann, Herbert
Año de publicación
2015
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
We describe the synthesis of a library of 11 638 N-alkylglycine peptoid trimers in a positional scanning format with adjustment of reaction conditions to account for different reactivities of the monomer building blocks. Evaluation of the library by high-content phenotypic screening for modulators of the cytoskeleton and mitosis resulted in the identification of two apoptosis-inducing peptoids, which, despite their structural similarity, target different proteins and cellular mechanisms. Whereas one peptoid binds to karyopherins, which mediate nuclear transport, the other N-alkylglycine trimer binds tubulin at the vinca alkaloid binding site.
Fil: Vendrell Navarro, Gloria. Institut Max Planck Fur Molekulare Physiologie; Alemania. Consejo Superior de Investigaciones Cientificas; España
Fil: Rúa, Federico. Consejo Superior de Investigaciones Cientificas; España. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Bujons, Jordi. Consejo Superior de Investigaciones Cientificas; España
Fil: Brockmeyer, Andreas. Institut Max Planck Fur Molekulare Physiologie; Alemania
Fil: Janning, Petra . Institut Max Planck Fur Molekulare Physiologie; Alemania
Fil: Ziegler, Slava. Institut Max Planck Fur Molekulare Physiologie; Alemania
Fil: Messeguer, Angel. Consejo Superior de Investigaciones Cientificas; España
Fil: Waldmann, Herbert. Institut Max Planck Fur Molekulare Physiologie; Alemania. Technische Universitä t Dortmund; Alemania
Materia
Apoptosis
Química Combinatoria
Peptidomimeticos
Relación Estructura-Actividad
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/13406
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/13406
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and TubulinVendrell Navarro, GloriaRúa, FedericoBujons, JordiBrockmeyer, AndreasJanning, PetraZiegler, SlavaMesseguer, AngelWaldmann, HerbertApoptosisQuímica CombinatoriaPeptidomimeticosRelación Estructura-Actividadhttps://purl.org/becyt/ford/1.2https://purl.org/becyt/ford/1https://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1https://purl.org/becyt/ford/3.4https://purl.org/becyt/ford/3We describe the synthesis of a library of 11 638 N-alkylglycine peptoid trimers in a positional scanning format with adjustment of reaction conditions to account for different reactivities of the monomer building blocks. Evaluation of the library by high-content phenotypic screening for modulators of the cytoskeleton and mitosis resulted in the identification of two apoptosis-inducing peptoids, which, despite their structural similarity, target different proteins and cellular mechanisms. Whereas one peptoid binds to karyopherins, which mediate nuclear transport, the other N-alkylglycine trimer binds tubulin at the vinca alkaloid binding site.Fil: Vendrell Navarro, Gloria. Institut Max Planck Fur Molekulare Physiologie; Alemania. Consejo Superior de Investigaciones Cientificas; EspañaFil: Rúa, Federico. Consejo Superior de Investigaciones Cientificas; España. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Bujons, Jordi. Consejo Superior de Investigaciones Cientificas; EspañaFil: Brockmeyer, Andreas. Institut Max Planck Fur Molekulare Physiologie; AlemaniaFil: Janning, Petra . Institut Max Planck Fur Molekulare Physiologie; AlemaniaFil: Ziegler, Slava. Institut Max Planck Fur Molekulare Physiologie; AlemaniaFil: Messeguer, Angel. Consejo Superior de Investigaciones Cientificas; EspañaFil: Waldmann, Herbert. Institut Max Planck Fur Molekulare Physiologie; Alemania. Technische Universitä t Dortmund; AlemaniaWiley VCH Verlag2015-07info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/13406Vendrell Navarro, Gloria; Rúa, Federico; Bujons, Jordi; Brockmeyer, Andreas; Janning, Petra ; et al.; Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin; Wiley VCH Verlag; Chembiochem; 16; 11; 7-2015; 1580-15871439-7633enginfo:eu-repo/semantics/altIdentifier/doi/10.1002/cbic.201500169info:eu-repo/semantics/altIdentifier/url/http://onlinelibrary.wiley.com/doi/10.1002/cbic.201500169/abstractinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2026-03-31T15:05:53Zoai:ri.conicet.gov.ar:11336/13406instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982026-03-31 15:05:54.047CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
title Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
spellingShingle Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
Vendrell Navarro, Gloria
Apoptosis
Química Combinatoria
Peptidomimeticos
Relación Estructura-Actividad
title_short Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
title_full Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
title_fullStr Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
title_full_unstemmed Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
title_sort Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin
dc.creator.none.fl_str_mv Vendrell Navarro, Gloria
Rúa, Federico
Bujons, Jordi
Brockmeyer, Andreas
Janning, Petra
Ziegler, Slava
Messeguer, Angel
Waldmann, Herbert
author Vendrell Navarro, Gloria
author_facet Vendrell Navarro, Gloria
Rúa, Federico
Bujons, Jordi
Brockmeyer, Andreas
Janning, Petra
Ziegler, Slava
Messeguer, Angel
Waldmann, Herbert
author_role author
author2 Rúa, Federico
Bujons, Jordi
Brockmeyer, Andreas
Janning, Petra
Ziegler, Slava
Messeguer, Angel
Waldmann, Herbert
author2_role author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Apoptosis
Química Combinatoria
Peptidomimeticos
Relación Estructura-Actividad
topic Apoptosis
Química Combinatoria
Peptidomimeticos
Relación Estructura-Actividad
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.2
https://purl.org/becyt/ford/1
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
https://purl.org/becyt/ford/3.4
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv We describe the synthesis of a library of 11 638 N-alkylglycine peptoid trimers in a positional scanning format with adjustment of reaction conditions to account for different reactivities of the monomer building blocks. Evaluation of the library by high-content phenotypic screening for modulators of the cytoskeleton and mitosis resulted in the identification of two apoptosis-inducing peptoids, which, despite their structural similarity, target different proteins and cellular mechanisms. Whereas one peptoid binds to karyopherins, which mediate nuclear transport, the other N-alkylglycine trimer binds tubulin at the vinca alkaloid binding site.
Fil: Vendrell Navarro, Gloria. Institut Max Planck Fur Molekulare Physiologie; Alemania. Consejo Superior de Investigaciones Cientificas; España
Fil: Rúa, Federico. Consejo Superior de Investigaciones Cientificas; España. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Bujons, Jordi. Consejo Superior de Investigaciones Cientificas; España
Fil: Brockmeyer, Andreas. Institut Max Planck Fur Molekulare Physiologie; Alemania
Fil: Janning, Petra . Institut Max Planck Fur Molekulare Physiologie; Alemania
Fil: Ziegler, Slava. Institut Max Planck Fur Molekulare Physiologie; Alemania
Fil: Messeguer, Angel. Consejo Superior de Investigaciones Cientificas; España
Fil: Waldmann, Herbert. Institut Max Planck Fur Molekulare Physiologie; Alemania. Technische Universitä t Dortmund; Alemania
description We describe the synthesis of a library of 11 638 N-alkylglycine peptoid trimers in a positional scanning format with adjustment of reaction conditions to account for different reactivities of the monomer building blocks. Evaluation of the library by high-content phenotypic screening for modulators of the cytoskeleton and mitosis resulted in the identification of two apoptosis-inducing peptoids, which, despite their structural similarity, target different proteins and cellular mechanisms. Whereas one peptoid binds to karyopherins, which mediate nuclear transport, the other N-alkylglycine trimer binds tubulin at the vinca alkaloid binding site.
publishDate 2015
dc.date.none.fl_str_mv 2015-07
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/13406
Vendrell Navarro, Gloria; Rúa, Federico; Bujons, Jordi; Brockmeyer, Andreas; Janning, Petra ; et al.; Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin; Wiley VCH Verlag; Chembiochem; 16; 11; 7-2015; 1580-1587
1439-7633
url http://hdl.handle.net/11336/13406
identifier_str_mv Vendrell Navarro, Gloria; Rúa, Federico; Bujons, Jordi; Brockmeyer, Andreas; Janning, Petra ; et al.; Positional scanning synthesis of a Peptoid library yields new inducers of apoptosis that target Karyopherins and Tubulin; Wiley VCH Verlag; Chembiochem; 16; 11; 7-2015; 1580-1587
1439-7633
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1002/cbic.201500169
info:eu-repo/semantics/altIdentifier/url/http://onlinelibrary.wiley.com/doi/10.1002/cbic.201500169/abstract
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Wiley VCH Verlag
publisher.none.fl_str_mv Wiley VCH Verlag
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1861214282574725120
score 12.822162

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