Volume 16, Issue 5 e13544
REVIEW ARTICLE
Open Access

Clinical investigation of glucokinase activators for the restoration of glucose homeostasis in diabetes

Ping Li

Corresponding Author

Ping Li

Department of Endocrinology, Drum Tower Hospital Affiliated to Nanjing University Medical School, Nanjing, China

Correspondence

Dalong Zhu and Ping Li, Department of Endocrinology, Drum Tower Hospital Affiliated to Nanjing University Medical School, 321 Zhongshan Road, Nanjing, Jiangsu, CN 210012, China.

Email: [email protected] and [email protected]

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Dalong Zhu

Corresponding Author

Dalong Zhu

Department of Endocrinology, Drum Tower Hospital Affiliated to Nanjing University Medical School, Nanjing, China

Correspondence

Dalong Zhu and Ping Li, Department of Endocrinology, Drum Tower Hospital Affiliated to Nanjing University Medical School, 321 Zhongshan Road, Nanjing, Jiangsu, CN 210012, China.

Email: [email protected] and [email protected]

Search for more papers by this author
First published: 25 April 2024

Abstract

As a sensor, glucokinase (GK) controls glucose homeostasis, which progressively declines in patients with diabetes. GK maintains the equilibrium of glucose levels and regulates the homeostatic system set points. Endocrine and hepatic cells can both respond to glucose cooperatively when GK is activated. GK has been under study as a therapeutic target for decades due to the possibility that cellular GK expression and function can be recovered, hence restoring glucose homeostasis in patients with type 2 diabetes. Five therapeutic compounds targeting GK are being investigated globally at the moment. They all have distinctive molecular structures and have been clinically shown to have strong antihyperglycemia effects. The mechanics, classification, and clinical development of GK activators are illustrated in this review. With the recent approval and marketing of the first GK activator (GKA), dorzagliatin, GKA's critical role in treating glucose homeostasis disorder and its long-term benefits in diabetes will eventually become clear.

Video Abstract

Clinical investigation of glucokinase activators for the restoration of glucose homeostasis in diabetes

by Ping Li and Dalong Zhu

DISCLOSURE

Zhu Dalong is an editorial board member of the Journal of Diabetes and a coauthor of this article. To minimize bias, they were excluded from all editorial decision-making related to the acceptance of this article for publication.

The full text of this article hosted at iucr.org is unavailable due to technical difficulties.