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Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis

Fibroblast activation including proliferation, survival, and ECM production is central to initiation and maintenance of fibrotic lesions in idiopathic pulmonary fibrosis (IPF). However, druggable molecules that target fibroblast activation remain limited. In this study, we show that multiple pro‐fib...

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Autores principales: Kasam, Rajesh K, Ghandikota, Sudhir, Soundararajan, Divyalakshmi, Reddy, Geereddy B, Huang, Steven K, Jegga, Anil G, Madala, Satish K
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7507328/
https://www.ncbi.nlm.nih.gov/pubmed/32761869
http://dx.doi.org/10.15252/emmm.202012131
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author Kasam, Rajesh K
Ghandikota, Sudhir
Soundararajan, Divyalakshmi
Reddy, Geereddy B
Huang, Steven K
Jegga, Anil G
Madala, Satish K
author_facet Kasam, Rajesh K
Ghandikota, Sudhir
Soundararajan, Divyalakshmi
Reddy, Geereddy B
Huang, Steven K
Jegga, Anil G
Madala, Satish K
author_sort Kasam, Rajesh K
collection PubMed
description Fibroblast activation including proliferation, survival, and ECM production is central to initiation and maintenance of fibrotic lesions in idiopathic pulmonary fibrosis (IPF). However, druggable molecules that target fibroblast activation remain limited. In this study, we show that multiple pro‐fibrotic growth factors, including TGFα, CTGF, and IGF1, increase aurora kinase B (AURKB) expression and activity in fibroblasts. Mechanistically, we demonstrate that Wilms tumor 1 (WT1) is a key transcription factor that mediates TGFα‐driven AURKB upregulation in fibroblasts. Importantly, we found that inhibition of AURKB expression or activity is sufficient to attenuate fibroblast activation. We show that fibrosis induced by TGFα is highly dependent on AURKB expression and treating TGFα mice with barasertib, an AURKB inhibitor, reverses fibroblast activation, and pulmonary fibrosis. Barasertib similarly attenuated fibrosis in the bleomycin model of pulmonary fibrosis. Together, our preclinical studies provide important proof‐of‐concept that demonstrate barasertib as a possible intervention therapy for IPF.
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spelling pubmed-75073282020-09-28 Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis Kasam, Rajesh K Ghandikota, Sudhir Soundararajan, Divyalakshmi Reddy, Geereddy B Huang, Steven K Jegga, Anil G Madala, Satish K EMBO Mol Med Articles Fibroblast activation including proliferation, survival, and ECM production is central to initiation and maintenance of fibrotic lesions in idiopathic pulmonary fibrosis (IPF). However, druggable molecules that target fibroblast activation remain limited. In this study, we show that multiple pro‐fibrotic growth factors, including TGFα, CTGF, and IGF1, increase aurora kinase B (AURKB) expression and activity in fibroblasts. Mechanistically, we demonstrate that Wilms tumor 1 (WT1) is a key transcription factor that mediates TGFα‐driven AURKB upregulation in fibroblasts. Importantly, we found that inhibition of AURKB expression or activity is sufficient to attenuate fibroblast activation. We show that fibrosis induced by TGFα is highly dependent on AURKB expression and treating TGFα mice with barasertib, an AURKB inhibitor, reverses fibroblast activation, and pulmonary fibrosis. Barasertib similarly attenuated fibrosis in the bleomycin model of pulmonary fibrosis. Together, our preclinical studies provide important proof‐of‐concept that demonstrate barasertib as a possible intervention therapy for IPF. John Wiley and Sons Inc. 2020-08-06 2020-09-07 /pmc/articles/PMC7507328/ /pubmed/32761869 http://dx.doi.org/10.15252/emmm.202012131 Text en © 2020 The Authors. Published under the terms of the CC BY 4.0 license This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Articles
Kasam, Rajesh K
Ghandikota, Sudhir
Soundararajan, Divyalakshmi
Reddy, Geereddy B
Huang, Steven K
Jegga, Anil G
Madala, Satish K
Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis
title Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis
title_full Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis
title_fullStr Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis
title_full_unstemmed Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis
title_short Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis
title_sort inhibition of aurora kinase b attenuates fibroblast activation and pulmonary fibrosis
topic Articles
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7507328/
https://www.ncbi.nlm.nih.gov/pubmed/32761869
http://dx.doi.org/10.15252/emmm.202012131
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