CDK8 inhibitor KY-065 rescues skeletal abnormalities in achondroplasia model mice.

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Tác giả: Kazuya Fukasawa, Eiichi Hinoi, Hironori Hojo, Tetsuhiro Horie, Takuya Kadota, Tatsuya Kitao, Takuya Kubo, Koki Sadamori, Yui Shibata, Hiroaki Shirahase, Nobutada Tanaka, Kazuya Tokumura, Ryotaro Yamakawa, Megumi Yamamoto, Tomoki Yoshida

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: Netherlands : Biochimica et biophysica acta. Molecular basis of disease , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 188894

Cyclin-dependent kinase 8 (CDK8) is a transcription-related CDK family member implicated in the regulation of bone homeostasis, and we recently demonstrated that our internally developed CDK8 inhibitor KY-065 can prevent postmenopausal osteoporosis in a mouse model. Achondroplasia (ACH), the most common form of genetic dwarfism in humans, is caused by a gain-of-function mutation in fibroblast growth factor receptor 3 (FGFR3), a receptor tyrosine kinase that activates downstream mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) signaling pathways. The first precision drug approved for the treatment of ACH in children, the C-type natriuretic peptide analog vosoritide, antagonizes the MAPK pathway, while there are currently no effective and safe medications targeting the STAT1 pathway. Here, we demonstrate that KY-065 rescues impaired chondrogenesis and stunted long bone growth in the Fgfr3
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