Recent advances in the development of HIPK2 inhibitors as anti-renal fibrosis agents

Author:

Hao Chao123,Cao Meng123,Ouyang Hanyi123,Chen Zhuo123,Hu Gaoyun123,Li Qianbin123ORCID

Affiliation:

1. Department of Medicinal Chemistry, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, 410013, China

2. Hunan Key Laboratory of Small Molecules for Diagnosis & Treatment of Chronic Disease, Changsha, Hunan, 410013, China

3. Hunan Key Laboratory of Organ Fibrosis, Changsha, Hunan, 410013, China

Abstract

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.

Funder

Chinese Pharmaceutical Association Biomedical Innovation Fund Project of Yiling

Fundamental Research Funds for the Central University of Central South University

National Natural Science Foundation of China

Natural Science Foundation of Hunan Province

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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