McKenna Neil J, Ochsner Scott A, Waich Alan, Cala-Garcia Juan, Echartrea Maria E Ruiz, Grimm Sandra, Poli Fernando, Castillo Rafael Cardenas, Zuluaga Juan D, Poli Sergio, Adams Taylor S, Pineda Ricardo, Moss Benjamin, Ryter Stefan W, Pillich Rudolf T, Villalba Julian A, Kato Kosuke, Hecker Louise, Celada Lindsay J, Sauler Maor, Koenigshoff Melanie, Kaminski Naftali, Raby Benjamin, Agarwal Sandeep, Tsoyi Konstantin, Coarfa Cristian, Rosas Ivan O
Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX, USA.
Section of Pulmonary, Critical Care and Sleep Medicine, Department of Medicine, Baylor College of Medicine, Houston, TX, USA.
bioRxiv. 2025 Jun 21:2025.06.16.659944. doi: 10.1101/2025.06.16.659944.
Idiopathic pulmonary fibrosis (IPF) is a progressive fibrotic pulmonary disease with unknown etiology. Since approved idiopathic pulmonary fibrosis (IPF) drugs only slow disease progression, novel therapeutics are required that improve clinical outcomes. Here, we report a single cell RNA-Seq and regulatory network analysis of the largest IPF cohort assembled to date. Segregating this cohort based on status of treatment with approved antifibrotics (untreated, nintedanib- and pirfenidone-treated), we describe for the first time the transcriptional landscape of untreated IPF across 40 lung cell types, and the elements of this program that are impacted by approved antifibrotics. On average, 60% of the untreated IPF-dysregulated transcriptome is refractory to treatment with these drugs, a transcriptional deficit we refer to as the IPF therapeutic gap. Regulatory network analysis indicated a dominant functional footprint for the transcription factor STAT3 in both untreated IPF and in the IPF therapeutic gap. Validating our analysis in a translational precision cut lung slice platform that recapitulates IPF explants, treatment with a STAT3 inhibitor reduced the IPF therapeutic gap in numerous lung cell types. Finally, we implicated STAT3 as a master transcription factor that regulates a network comprising numerous profibrotic transcription factors in IPF alveolar fibroblasts, a critical fibrotic cell lineage. Our study represents a comprehensive resource for translational lung fibrosis research and establishes a novel strategy for drug discovery in human disease more broadly.
特发性肺纤维化(IPF)是一种病因不明的进行性纤维化肺部疾病。由于已获批的特发性肺纤维化(IPF)药物只能减缓疾病进展,因此需要新的疗法来改善临床结局。在此,我们报告了对迄今为止组装的最大IPF队列进行的单细胞RNA测序和调控网络分析。根据使用已获批抗纤维化药物的治疗状态(未治疗、尼达尼布和吡非尼酮治疗)对该队列进行分类,我们首次描述了未经治疗的IPF在40种肺细胞类型中的转录图谱,以及该程序中受已获批抗纤维化药物影响的元素。平均而言,未经治疗的IPF失调转录组中有60%对这些药物的治疗无反应,我们将这种转录缺陷称为IPF治疗差距。调控网络分析表明,转录因子STAT3在未经治疗的IPF和IPF治疗差距中均具有主要的功能足迹。在一个模拟IPF外植体的转化精密切割肺切片平台上验证我们的分析,用STAT3抑制剂治疗可减少多种肺细胞类型中的IPF治疗差距。最后,我们认为STAT3是一种主转录因子,它在IPF肺泡成纤维细胞(一种关键的纤维化细胞谱系)中调节一个包含众多促纤维化转录因子的网络。我们的研究为转化性肺纤维化研究提供了一个全面的资源,并更广泛地为人类疾病药物发现建立了一种新策略。