DYRK1A Inhibitors as Potential Therapeutics for β-Cell Regeneration for Diabetes
Year: 2021
Type: article
Abstract: According to the World Health Organization (WHO), 422 million people are suffering from diabetes worldwide. Current diabetes therapies are focused on optimizing blood glucose control to prevent long-term diabetes complications. Unfortunately, current therapies have failed to achieve glycemic targets in the majority of people with diabetes. In this context, regeneration of functional insulin-producing human β-cells in people with diabetes through the use of DYRK1A inhibitor drugs has recently received special attention. Several small molecule DYRK1A inhibitors have been identified that induce human β-cell proliferation in vitro and in vivo. Furthermore, DYRK1A inhibitors have also been shown to synergize β-cell proliferation with other classes of drugs, such as TGFβ inhibitors and GLP-1 receptor agonists. In this perspective, we review the status of DYRK1A as a therapeutic target for β-cell proliferation and provide perspectives on technical and scientific challenges for future translational development.
Source: Journal of Medicinal Chemistry
Authors: Kunal Kumar, Chalada Suebsuwong, Peng Wang, Adolfo Garcia-Ocana, Andrew F. Stewart, Robert J. DeVita
Institution: Icahn School of Medicine at Mount Sinai
Language: English
Subfield: Surgery
Field: Medicine
Domain: Health Sciences
Open Access status: green
Awards: G113413678, G1193134389, G3358720692, DYRK Inhibitors for Human Beta Cell Expansion, Dextran Sulfate, Beta Cell Preservation and Immune Regulation in Type 1 Diabetes, Biological and Medicinal Chemistry Approaches to Human Beta Cell Regeneration, Novel Selective Type II kinase Inhibitors to treat Diabetes, G7863164370, G836681807, NYR-Diabetes Research Center (NYR-DRC)
OpenAlex ID: W3135826760