Variants that differed in frequency between GDM and controls have been identified in genes coding for the (a) islet specific promoter of
glucokinase, said to be important for glucose sensing by the [beta] cells; (b) Calpain 10, a gene associated with type 2 diabetes in some ethnic groups; and (c) the sulfonylurea receptor-1 that is involved in glucose-stimulated secretion (39-41).
Matschinsky, "Assessing the potential of
glucokinase activators in diabetes therapy," Nature Reviews Drug Discovery, vol.
Glucokinase diabetes in 103 families from a country-based study in the Czech Republic: geographically restricted distribution of two prevalent GCK mutations.
Glucokinase (EC2.7.1.2) activity was measured using the glucose-6-phosphate dehydrogenase (G6PDH) coupling method (Tranulis et al., 1996; Panserat et al., 2000a).
Three dimensional structures of
glucokinase (PDB ID: 1V4S) (Kamata et al.
[5] Human genes: LPL, lipoprotein lipase; CRP, C-reactive protein, pentraxin-related; TRIB1, tribbles pseudokinase 1; GCKR,
glucokinase (hexokinase 4) regulator; APAA5, apolipoprotein A-V; APOC3, apolipoprotein C-III.
Also, it has a strong potential to restore
glucokinase activity and inhibit lipogenesis resulting in activation of glycolysis.
The significance of GCK in sensing ambient glucose has led to the hypothesis that pharmaceutical manipulation of this physiological mechanism in the form of
glucokinase activators could present an effective method of treating hyperglycaemia as a result of type 2 diabetes [63].
The genetic variants examined included PNPLA3 (patatin-like phospholipase domain-containing protein 3), NCAN (neurocan), LYPLAL1 (lysophospholipase-like 1), GCKR (
glucokinase regulatory protein), and PPP1R3B (protein phosphatase 1), regulatory subunit 3b.
29 December 2011 - Chinese Hua Medicine said last week it had licensed Swiss Roche's (VTX:ROG)
Glucokinase Activator (GKA) programme.