High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma

Localized scleroderma is a rare autoimmune disease characterized by progressive fibrosis of the skin and its underlying structures, causing loss of normal tissue structure and function. Myofibroblasts, differentiated from fibroblasts by high expression of α-smooth muscle actin, play a key role in th...

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Main Authors: Katariina Mähönen, Isabel Mogollon, Antti Hassinen, Minttu Polso, Katja Välimäki, Swapnil Potdar, Al-Amin Chowdhury, Annamari Ranki, Jani Saarela, Vilja Pietiäinen, Jaana Panelius
Format: Article
Language:English
Published: Medical Journals Sweden 2025-08-01
Series:Acta Dermato-Venereologica
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Online Access:https://medicaljournalssweden.se/actadv/article/view/43088
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author Katariina Mähönen
Isabel Mogollon
Antti Hassinen
Minttu Polso
Katja Välimäki
Swapnil Potdar
Al-Amin Chowdhury
Annamari Ranki
Jani Saarela
Vilja Pietiäinen
Jaana Panelius
author_facet Katariina Mähönen
Isabel Mogollon
Antti Hassinen
Minttu Polso
Katja Välimäki
Swapnil Potdar
Al-Amin Chowdhury
Annamari Ranki
Jani Saarela
Vilja Pietiäinen
Jaana Panelius
author_sort Katariina Mähönen
collection DOAJ
description Localized scleroderma is a rare autoimmune disease characterized by progressive fibrosis of the skin and its underlying structures, causing loss of normal tissue structure and function. Myofibroblasts, differentiated from fibroblasts by high expression of α-smooth muscle actin, play a key role in the pathogenesis with continuous production of collagen and other extracellular matrix components. Transforming growth factor β promotes myofibroblast transformation and is central to the pathogenesis of fibrotic diseases. Targeted therapies for skin fibrosis are lacking, and current treatment consisting of topical steroids and immunosuppressive drugs often has limited efficacy. In this study, testing was performed with 78 drugs on lesional localized scleroderma fibroblasts to find potential new therapies, with α-smooth muscle actin and collagen-1 expression as markers for antifibrotic effect. Several drugs belonging to inhibitors of tyrosine kinase, phosphoinositide-3 kinase, and transforming growth factor β receptor were found to have an antifibrotic effect in localized scleroderma fibroblasts. Along with increased expression of transforming growth factor β1, Smad3, and AKT found in lesional localized scleroderma skin, these results confirm transforming growth factor β pathway as a treatment target. Additionally, androgen receptor antagonists showed potential antifibrotic effects, co-aligning with an increased expression of androgen receptor in localized scleroderma skin.
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spelling doaj-art-aaccce4a7e6e4e419d4649740e7011db2025-08-20T03:37:09ZengMedical Journals SwedenActa Dermato-Venereologica0001-55551651-20572025-08-0110510.2340/actadv.v105.43088High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized SclerodermaKatariina Mähönen0Isabel Mogollon1Antti Hassinen2Minttu Polso3Katja Välimäki4Swapnil Potdar5Al-Amin Chowdhury6Annamari Ranki7Jani Saarela8Vilja Pietiäinen9Jaana Panelius10epartment of Dermatology and Allergology, University of Helsinki and Helsinki University Hospital, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, Finlandepartment of Dermatology and Allergology, University of Helsinki and Helsinki University Hospital, Helsinki, Finlandepartment of Dermatology and Allergology, University of Helsinki and Helsinki University Hospital, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, FinlandInstitute for Molecular Medicine Finland – FIMM, Helsinki Institute for Life Sciences – HiLIFE, University of Helsinki, Helsinki, Finlandepartment of Dermatology and Allergology, University of Helsinki and Helsinki University Hospital, Helsinki, FinlandLocalized scleroderma is a rare autoimmune disease characterized by progressive fibrosis of the skin and its underlying structures, causing loss of normal tissue structure and function. Myofibroblasts, differentiated from fibroblasts by high expression of α-smooth muscle actin, play a key role in the pathogenesis with continuous production of collagen and other extracellular matrix components. Transforming growth factor β promotes myofibroblast transformation and is central to the pathogenesis of fibrotic diseases. Targeted therapies for skin fibrosis are lacking, and current treatment consisting of topical steroids and immunosuppressive drugs often has limited efficacy. In this study, testing was performed with 78 drugs on lesional localized scleroderma fibroblasts to find potential new therapies, with α-smooth muscle actin and collagen-1 expression as markers for antifibrotic effect. Several drugs belonging to inhibitors of tyrosine kinase, phosphoinositide-3 kinase, and transforming growth factor β receptor were found to have an antifibrotic effect in localized scleroderma fibroblasts. Along with increased expression of transforming growth factor β1, Smad3, and AKT found in lesional localized scleroderma skin, these results confirm transforming growth factor β pathway as a treatment target. Additionally, androgen receptor antagonists showed potential antifibrotic effects, co-aligning with an increased expression of androgen receptor in localized scleroderma skin. https://medicaljournalssweden.se/actadv/article/view/43088Localized sclerodermaMyofibroblaststransforming growth factor betaantifibrotic agentshigh throughput screening assay
spellingShingle Katariina Mähönen
Isabel Mogollon
Antti Hassinen
Minttu Polso
Katja Välimäki
Swapnil Potdar
Al-Amin Chowdhury
Annamari Ranki
Jani Saarela
Vilja Pietiäinen
Jaana Panelius
High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma
Acta Dermato-Venereologica
Localized scleroderma
Myofibroblasts
transforming growth factor beta
antifibrotic agents
high throughput screening assay
title High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma
title_full High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma
title_fullStr High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma
title_full_unstemmed High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma
title_short High-content Image-based Drug Testing of Patients’ Primary Fibroblasts Reveals Potential New Treatment Options for Localized Scleroderma
title_sort high content image based drug testing of patients primary fibroblasts reveals potential new treatment options for localized scleroderma
topic Localized scleroderma
Myofibroblasts
transforming growth factor beta
antifibrotic agents
high throughput screening assay
url https://medicaljournalssweden.se/actadv/article/view/43088
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