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).
Familial hyperglycemia due to mutations in glucokinase
: definition of a subtype of diabetes mellitus.
Matschinsky, "Assessing the potential of glucokinase
activators in diabetes therapy," Nature Reviews Drug Discovery, vol.
diabetes in 103 families from a country-based study in the Czech Republic: geographically restricted distribution of two prevalent GCK mutations.
Blood glucose (i) Increases circulating insulin to reduce regulation glucose back to normal; improvement (ii) Increases relevant enzyme activities including glucokinase
, hexokinase, and glucose-6-phosphate dehydrogenase to increase glucose metabolic rate.
(EC184.108.40.206) 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.
 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 .
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.