Myofibroblasts are the key players in extracellular matrix remodeling, a core phenomenon in numerous devastating fibrotic diseases. Not only in organ fibrosis, but also the pivotal role of myofibroblasts in tumor progression, invasion and metastasis has recently been highlighted. Myofibroblast targeting has gained tremendous attention in order to inhibit the progression of incurable fibrotic diseases, or to limit the myofibroblast-induced tumor progression and metastasis. In this review, we outline the origin of myofibroblasts, their general characteristics and functions during fibrosis progression in three major organs: liver, kidneys and lungs as well as in cancer. We will then discuss the state-of-the art drug targeting technologies to myofibroblasts in context of the above-mentioned organs and tumor microenvironment. The overall objective of this review is therefore to advance our understanding in drug targeting to myofibroblasts, and concurrently identify opportunities and challenges for designing new strategies to develop novel diagnostics and therapeutics against fibrosis and cancer.

肌成纤维细胞是细胞外基质重塑的关键因素，而细胞重塑是许多毁灭性纤维化疾病的核心现象。最近不仅强调了器官纤维化，而且还指出了肌成纤维细胞在肿瘤进展，侵袭和转移中的关键作用。为了抑制不可治愈的纤维化疾病的进展，或限制成肌纤维细胞诱导的肿瘤进展和转移，成肌纤维细胞的靶向已经引起了极大的关注。在这篇综述中，我们概述了肌成纤维细胞的起源，它们在三个主要器官（肝，肾，肺和癌症）纤维化进展过程中的一般特征和功能。然后，我们将在上述器官和肿瘤微环境的背景下讨论针对成肌纤维细胞的最先进药物靶向技术。