The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice

[EN] Background: TAT-Cx43266-283 is a novel Src inhibitor, which has shown noteworthy antitumor effects in preclinical models of glioblastoma. Because Src plays a pivotal role in several tumor types, including lung cancer brain metastasis derived from non-small cell lung cancer (NSCLC) cells, we inv...

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Autores: Cerveró García, Pilar, Jiménez Madrona, Enrique, Álvarez Vázquez, Andrea, Flores Hernández, Raquel, García Vicente, Laura, García Guerrero, Laura, Alonso Amador, Juan José, González Sánchez, Raúl, Ollauri Ibáñez, Claudia, Paniagua Sancho, María, Talaverón Aguilocho, Rocío, Rodrigues Teixeira, Telmo, Martín Guerrero, Sandra M., Casado, Pedro, Rajeeve, Vinothini, Shields, Tommy, Hijazi Vega, Maruan, Cutillas, Pedro R, Jaraíz Rodríguez, Myriam, Tabernero Urbieta, María Aránzazu
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2026
País:España
Institución:Universidad de Salamanca (USAL)
Repositorio:GREDOS. Repositorio Institucional de la Universidad de Salamanca
OAI Identifier:oai:gredos.usal.es:10366/169127
Acceso en línea:http://hdl.handle.net/10366/169127
Access Level:acceso abierto
Palabra clave:Brain metastasis
lung cancer
CSCs
Src
Connexin
3201.01 Oncología
3207.03 Carcinogénesis
3207.07 Patología Experimental
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oai_identifier_str oai:gredos.usal.es:10366/169127
network_acronym_str ES
network_name_str España
repository_id_str
dc.title.none.fl_str_mv The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
title The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
spellingShingle The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
Cerveró García, Pilar
Brain metastasis
lung cancer
CSCs
Src
Connexin
3201.01 Oncología
3207.03 Carcinogénesis
3207.07 Patología Experimental
title_short The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
title_full The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
title_fullStr The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
title_full_unstemmed The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
title_sort The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in mice
dc.creator.none.fl_str_mv Cerveró García, Pilar
Jiménez Madrona, Enrique
Álvarez Vázquez, Andrea
Flores Hernández, Raquel
García Vicente, Laura
García Guerrero, Laura
Alonso Amador, Juan José
González Sánchez, Raúl
Ollauri Ibáñez, Claudia
Paniagua Sancho, María
Talaverón Aguilocho, Rocío
Rodrigues Teixeira, Telmo
Martín Guerrero, Sandra M.
Casado, Pedro
Rajeeve, Vinothini
Shields, Tommy
Hijazi Vega, Maruan
Cutillas, Pedro R
Jaraíz Rodríguez, Myriam
Tabernero Urbieta, María Aránzazu
author Cerveró García, Pilar
author_facet Cerveró García, Pilar
Jiménez Madrona, Enrique
Álvarez Vázquez, Andrea
Flores Hernández, Raquel
García Vicente, Laura
García Guerrero, Laura
Alonso Amador, Juan José
González Sánchez, Raúl
Ollauri Ibáñez, Claudia
Paniagua Sancho, María
Talaverón Aguilocho, Rocío
Rodrigues Teixeira, Telmo
Martín Guerrero, Sandra M.
Casado, Pedro
Rajeeve, Vinothini
Shields, Tommy
Hijazi Vega, Maruan
Cutillas, Pedro R
Jaraíz Rodríguez, Myriam
Tabernero Urbieta, María Aránzazu
author_role author
author2 Jiménez Madrona, Enrique
Álvarez Vázquez, Andrea
Flores Hernández, Raquel
García Vicente, Laura
García Guerrero, Laura
Alonso Amador, Juan José
González Sánchez, Raúl
Ollauri Ibáñez, Claudia
Paniagua Sancho, María
Talaverón Aguilocho, Rocío
Rodrigues Teixeira, Telmo
Martín Guerrero, Sandra M.
Casado, Pedro
Rajeeve, Vinothini
Shields, Tommy
Hijazi Vega, Maruan
Cutillas, Pedro R
Jaraíz Rodríguez, Myriam
Tabernero Urbieta, María Aránzazu
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Brain metastasis
lung cancer
CSCs
Src
Connexin
3201.01 Oncología
3207.03 Carcinogénesis
3207.07 Patología Experimental
topic Brain metastasis
lung cancer
CSCs
Src
Connexin
3201.01 Oncología
3207.03 Carcinogénesis
3207.07 Patología Experimental
description [EN] Background: TAT-Cx43266-283 is a novel Src inhibitor, which has shown noteworthy antitumor effects in preclinical models of glioblastoma. Because Src plays a pivotal role in several tumor types, including lung cancer brain metastasis derived from non-small cell lung cancer (NSCLC) cells, we investigated the effect of TAT-Cx43266-283 in NSCLC-derived brain metastasis, a disease of unmet clinical need. Methods: The effect of TAT-Cx43266-283 was studied in Lewis Lung Carcinoma (LLC), LSZ4, A549 and H441 NSCLC cells. The non-adherent stem-like LLC cells (LLC-CSCs) were intracranially implanted in immunocompetent mice to study the effect of TAT-Cx43266-283 in vivo. Phosphoproteomic analysis was employed to identify signaling pathways affected by TATCx43266-283, and the most prominent were validated by Western blot and immunohistochemistry. Datasets of human NSCLC adenocarcinoma were also analyzed. Results: TAT-Cx43266-283 significantly reduced LLC-CSCs viability and increased the survival of mice bearing brain tumors derived from these cells. Phosphoproteomic analysis identified MEK and ERK as key effectors of this treatment. TAT-Cx43266-283 induced apoptosis, impaired cytoskeletal dynamics and disrupted tumor vascularization. Patient datasets revealed that the targets of TAT-Cx43266-283 were significantly enriched in KRAS-altered lung tumors. Functional validation in several human and mouse KRAS-mutated non-adherent NSCLC cells confirmed that TAT-Cx43266-283 reduced their growth and invasiveness. Conclusions: Our results suggest that TAT-Cx43266-283 is a promising antitumor drug for lung cancer brain metastasis, as judged by the dual inhibition of Src and the MEK-ERK pathway in KRAS-mutated NSCLC. This study opens new avenues for exploring TAT-Cx43266-283 in other tumor types driven by these molecular alterations.
publishDate 2026
dc.date.none.fl_str_mv 2026
2026
2026
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/10366/169127
url http://hdl.handle.net/10366/169127
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv SA125P20
SA212P24
CLU2023-1-01
PID2021-128549OB-I00
MCIN/AEI/ 10.13039/501100011033
PDC2022-133652-I00
PID2024-161871OB-I00
MCIN/AEI/ 10.13039/501100011033
C15966/A24375
C16420/A18066
RYC2020-029435-I
dc.rights.none.fl_str_mv Attribution-NonCommercial-NoDerivatives 4.0 Internacional
http://creativecommons.org/licenses/by-nc-nd/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivatives 4.0 Internacional
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Oxford University Press
publisher.none.fl_str_mv Oxford University Press
dc.source.none.fl_str_mv reponame:GREDOS. Repositorio Institucional de la Universidad de Salamanca
instname:Universidad de Salamanca (USAL)
instname_str Universidad de Salamanca (USAL)
reponame_str GREDOS. Repositorio Institucional de la Universidad de Salamanca
collection GREDOS. Repositorio Institucional de la Universidad de Salamanca
repository.name.fl_str_mv
repository.mail.fl_str_mv
_version_ 1869404099728900096
spelling The src inhibitor peptide TAT-Cx43266-283 improves survival in an intracranial model of lung cancer brain metastasis in miceCerveró García, PilarJiménez Madrona, EnriqueÁlvarez Vázquez, AndreaFlores Hernández, RaquelGarcía Vicente, LauraGarcía Guerrero, LauraAlonso Amador, Juan JoséGonzález Sánchez, RaúlOllauri Ibáñez, ClaudiaPaniagua Sancho, MaríaTalaverón Aguilocho, RocíoRodrigues Teixeira, TelmoMartín Guerrero, Sandra M.Casado, PedroRajeeve, VinothiniShields, TommyHijazi Vega, MaruanCutillas, Pedro RJaraíz Rodríguez, MyriamTabernero Urbieta, María AránzazuBrain metastasislung cancerCSCsSrcConnexin3201.01 Oncología3207.03 Carcinogénesis3207.07 Patología Experimental[EN] Background: TAT-Cx43266-283 is a novel Src inhibitor, which has shown noteworthy antitumor effects in preclinical models of glioblastoma. Because Src plays a pivotal role in several tumor types, including lung cancer brain metastasis derived from non-small cell lung cancer (NSCLC) cells, we investigated the effect of TAT-Cx43266-283 in NSCLC-derived brain metastasis, a disease of unmet clinical need. Methods: The effect of TAT-Cx43266-283 was studied in Lewis Lung Carcinoma (LLC), LSZ4, A549 and H441 NSCLC cells. The non-adherent stem-like LLC cells (LLC-CSCs) were intracranially implanted in immunocompetent mice to study the effect of TAT-Cx43266-283 in vivo. Phosphoproteomic analysis was employed to identify signaling pathways affected by TATCx43266-283, and the most prominent were validated by Western blot and immunohistochemistry. Datasets of human NSCLC adenocarcinoma were also analyzed. Results: TAT-Cx43266-283 significantly reduced LLC-CSCs viability and increased the survival of mice bearing brain tumors derived from these cells. Phosphoproteomic analysis identified MEK and ERK as key effectors of this treatment. TAT-Cx43266-283 induced apoptosis, impaired cytoskeletal dynamics and disrupted tumor vascularization. Patient datasets revealed that the targets of TAT-Cx43266-283 were significantly enriched in KRAS-altered lung tumors. Functional validation in several human and mouse KRAS-mutated non-adherent NSCLC cells confirmed that TAT-Cx43266-283 reduced their growth and invasiveness. Conclusions: Our results suggest that TAT-Cx43266-283 is a promising antitumor drug for lung cancer brain metastasis, as judged by the dual inhibition of Src and the MEK-ERK pathway in KRAS-mutated NSCLC. This study opens new avenues for exploring TAT-Cx43266-283 in other tumor types driven by these molecular alterations.This research was funded by Junta de Castilla y León, FEDER SA125P20, SA212P24, CLU2023-1-01 (A.T.), the grant FEDER PID2021-128549OB-I00 (A.T.) funded by MCIN/AEI/ 10.13039/501100011033 and “ERDF A way of making Europe,” the grant PDC2022-133652-I00 (A.T.) and PID2024-161871OB-I00 funded by MCIN/AEI/ 10.13039/501100011033 and “European Union Next Generation EU/PRTR”, the Cancer Research UK Programme Grant C15966/A24375 and C16420/A18066 (P.R.-C) and Blood Cancer UK grant 20008 (P.R.-C). P.C.G., A.Á.-V. and R.F.-H. received predoctoral fellowships from Junta de Castilla y León. L.G.-V. and E.J.-M. received a FPU predoctoral fellowship from MICIU. C.O.-I. and M.P.-S. received postdoctoral fellowships from Junta de Castilla y León. R.T. received a postdoctoral fellowship from Asociación Española Contra el Cáncer (AECC). P.C.-G and A.Á.-V. were also supported by EMBO Scientific Exchange Grants (#10334 and #9668). M.H. was supported by Ramón y Cajal fellowships from MICIU/AEI (RYC2020-029435-I). M.J-R. was supported by Usal4excellence European Union's Marie Skłodowska-Curie Actions (MSCA).Oxford University Press202620262026info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionhttp://hdl.handle.net/10366/169127reponame:GREDOS. Repositorio Institucional de la Universidad de Salamancainstname:Universidad de Salamanca (USAL)InglésSA125P20SA212P24CLU2023-1-01PID2021-128549OB-I00MCIN/AEI/ 10.13039/501100011033PDC2022-133652-I00PID2024-161871OB-I00MCIN/AEI/ 10.13039/501100011033C15966/A24375C16420/A18066RYC2020-029435-IAttribution-NonCommercial-NoDerivatives 4.0 Internacionalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessoai:gredos.usal.es:10366/1691272026-06-07T06:28:51Z
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