Recent advances in the development of HIPK2 inhibitors as anti-renal fibrosis agents.
Chao HaoMeng CaoHanyi OuyangZhuo ChenGaoyun HuQianbin LiPublished in: Future medicinal chemistry (2023)
HIPK2 is a serine/threonine kinase, located in the nucleus, that was initially found to be able to phosphorylate p53 at Ser46 to promote apoptosis; it has been widely studied. It has been reported that HIPK2 can simultaneously regulate TGF-β/Smad3, Wnt/β-catenin, Notch and NF-κB pathways in the kidney to initiate inflammation and fibrosis, resulting in the development of chronic kidney disease (CKD). Therefore, inhibition of HIPK2 is strongly considered an effective method for the treatment of CKD. In brief, this review summarizes the progress of HIPK2 in CKD as well as the reported HIPK2 inhibitors and their role in different CKD models.