TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis

Abstract The TGFβ signaling pathway is known for its pleiotropic functions in a plethora of biological processes. In melanoma, TGFβ signaling promotes invasiveness and metastasis formation. However, its involvement in the response to therapy is controversial. While several studies have linked TGFβ s...

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Main Authors: Benjamin Loos, Adrian Salas-Bastos, Anna Nordin, Julien Debbache, Salome Stierli, Phil F. Cheng, Stefanie Rufli, Conrad Wyss, Mitchell P. Levesque, Reinhard Dummer, Wendy Wei-Lynn Wong, Steve Pascolo, Claudio Cantù, Lukas Sommer
Format: Article
Language:English
Published: Nature Publishing Group 2024-12-01
Series:Cell Death and Disease
Online Access:https://doi.org/10.1038/s41419-024-07305-1
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author Benjamin Loos
Adrian Salas-Bastos
Anna Nordin
Julien Debbache
Salome Stierli
Phil F. Cheng
Stefanie Rufli
Conrad Wyss
Mitchell P. Levesque
Reinhard Dummer
Wendy Wei-Lynn Wong
Steve Pascolo
Claudio Cantù
Lukas Sommer
author_facet Benjamin Loos
Adrian Salas-Bastos
Anna Nordin
Julien Debbache
Salome Stierli
Phil F. Cheng
Stefanie Rufli
Conrad Wyss
Mitchell P. Levesque
Reinhard Dummer
Wendy Wei-Lynn Wong
Steve Pascolo
Claudio Cantù
Lukas Sommer
author_sort Benjamin Loos
collection DOAJ
description Abstract The TGFβ signaling pathway is known for its pleiotropic functions in a plethora of biological processes. In melanoma, TGFβ signaling promotes invasiveness and metastasis formation. However, its involvement in the response to therapy is controversial. While several studies have linked TGFβ signaling to elevated resistance to targeted therapy in melanoma, separate findings have indicated a favorable treatment response through TGFβ-mediated increase of cell death. We now found that the outcome of TGFβ signaling in the context of targeted therapy is dose dependent. Unlike low doses, high levels of TGFβ signal activation induce apoptosis upon simultaneous MAPK pathway inhibition, even in targeted therapy resistant melanoma cell lines. Using transcriptomic analyses, combined with genomic target identification of the critical TGFβ signaling effector SMAD4, we demonstrate that parallel activation of TGFβ signaling and MAPK pathway inhibition causes a complete switch of TGFβ target genes from promoting pro-invasive processes to fueling pro-apoptotic pathways. Investigations of underlying mechanisms identified a novel apoptosis-inducing gene signature. Functional validation of signature members highlighted a central role of the pro-apoptotic BCL2 family member BCL2L11 (BIM) in mediating apoptosis in this condition. Using a modified, synthetic version of the TGFB1 mRNA for intra-tumoral injections, we additionally showcase a potential therapeutic application of this treatment combination.
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spelling doaj-art-ffa3a422e75549078e48baa042793f682024-12-22T12:51:01ZengNature Publishing GroupCell Death and Disease2041-48892024-12-01151211810.1038/s41419-024-07305-1TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosisBenjamin Loos0Adrian Salas-Bastos1Anna Nordin2Julien Debbache3Salome Stierli4Phil F. Cheng5Stefanie Rufli6Conrad Wyss7Mitchell P. Levesque8Reinhard Dummer9Wendy Wei-Lynn Wong10Steve Pascolo11Claudio Cantù12Lukas Sommer13University of Zürich, Institute of AnatomyUniversity of Zürich, Institute of AnatomyWallenberg Centre for Molecular Medicine, Linköping UniversityUniversity of Zürich, Institute of AnatomyUniversity of Zürich, Institute of AnatomyUniversity of Zürich Hospital, University of Zürich, Department of DermatologyUniversity of Zurich, Institute of Experimental ImmunologyUniversity of Zürich Hospital, University of Zürich, Department of DermatologyUniversity of Zürich Hospital, University of Zürich, Department of DermatologyUniversity of Zürich Hospital, University of Zürich, Department of DermatologyUniversity of Zurich, Institute of Experimental ImmunologyUniversity of Zürich Hospital, University of Zürich, Department of DermatologyWallenberg Centre for Molecular Medicine, Linköping UniversityUniversity of Zürich, Institute of AnatomyAbstract The TGFβ signaling pathway is known for its pleiotropic functions in a plethora of biological processes. In melanoma, TGFβ signaling promotes invasiveness and metastasis formation. However, its involvement in the response to therapy is controversial. While several studies have linked TGFβ signaling to elevated resistance to targeted therapy in melanoma, separate findings have indicated a favorable treatment response through TGFβ-mediated increase of cell death. We now found that the outcome of TGFβ signaling in the context of targeted therapy is dose dependent. Unlike low doses, high levels of TGFβ signal activation induce apoptosis upon simultaneous MAPK pathway inhibition, even in targeted therapy resistant melanoma cell lines. Using transcriptomic analyses, combined with genomic target identification of the critical TGFβ signaling effector SMAD4, we demonstrate that parallel activation of TGFβ signaling and MAPK pathway inhibition causes a complete switch of TGFβ target genes from promoting pro-invasive processes to fueling pro-apoptotic pathways. Investigations of underlying mechanisms identified a novel apoptosis-inducing gene signature. Functional validation of signature members highlighted a central role of the pro-apoptotic BCL2 family member BCL2L11 (BIM) in mediating apoptosis in this condition. Using a modified, synthetic version of the TGFB1 mRNA for intra-tumoral injections, we additionally showcase a potential therapeutic application of this treatment combination.https://doi.org/10.1038/s41419-024-07305-1
spellingShingle Benjamin Loos
Adrian Salas-Bastos
Anna Nordin
Julien Debbache
Salome Stierli
Phil F. Cheng
Stefanie Rufli
Conrad Wyss
Mitchell P. Levesque
Reinhard Dummer
Wendy Wei-Lynn Wong
Steve Pascolo
Claudio Cantù
Lukas Sommer
TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis
Cell Death and Disease
title TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis
title_full TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis
title_fullStr TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis
title_full_unstemmed TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis
title_short TGFβ signaling sensitizes MEKi-resistant human melanoma to targeted therapy-induced apoptosis
title_sort tgfβ signaling sensitizes meki resistant human melanoma to targeted therapy induced apoptosis
url https://doi.org/10.1038/s41419-024-07305-1
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