Advances in a novel class of hypoglycemic agents: glucokinase activators

doi:10.5246/jcps.2026.02.008

Abstract

Abstract:

Type 2 diabetes mellitus (T2DM) is a complex metabolic disorder characterized by multifactorial pathogenesis, in which therapies targeting a single mechanism often fail to achieve optimal glycemic control. In recent years, glucokinase (GK), a key regulatory enzyme in glucose homeostasis, has emerged as a promising anti-diabetic target, attracting considerable attention from researchers. Acting as a glucose sensor, GK initiates counter-regulatory responses in response to fluctuations in blood glucose, thereby contributing to the restoration and maintenance of normoglycemia. Activation of GK enhances glucose metabolism and lowers blood glucose levels, representing a potential therapeutic strategy for the management of type 2 diabetes. GK activators (GKAs), a novel class of anti-diabetic agents, have therefore garnered significant interest. This article provides a comprehensive review of the functional role of GK in diabetes, elucidates the mechanistic action of GKAs at the protein level, and summarizes current research progress, emerging trends, and prospects regarding the clinical application of GKAs.

Key words: Type 2 diabetes mellitus, Glucokinase, Glucokinase activators

Supporting:

Wenxi Li, Gong Fang, Jie Zhang, Juan Bai. Advances in a novel class of hypoglycemic agents: glucokinase activators[J]. Journal of Chinese Pharmaceutical Sciences, 2026, 35(2): 115-130.

Figures/Tables 4

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