Medical use of inhibitors of serine/threonine protein phosphatase, for treatment or prevention of e.g. arteriosclerosis, cystic fibrosis and diabetes mellitus

摘要

Use of inhibitors (I) of serine/threonine protein phosphatase for treatment or prevention of e.g. arteriosclerotic diseases is new. Use of inhibitors (I) of serine/threonine protein phosphatase for treatment or prevention of arteriosclerotic diseases, high-density lipoprotein (HDL) deficiency syndrome, syndromes caused by apolipoprotein A1 (ApoA1) synthesis defects or mutations, lecithin:cholesterol acyltransferase deficiency, fish eye disease, lipoprotein lipase deficiency, defects in ATP (adenosine triphosphate)-cassette transporters, diabetes mellitus, benign growths, malignant tumors, cystic fibrosis, adrenoleukodystrophy, retinitis pigmentosa, sideroblast anemia, ataxia, Stargardt disease and inherited intrahepatic cholestasis is new. ACTIVITY : Antiarteriosclerotic; Ophthalmological; Antidiabetic; Cytostatic; Antianemic; Cardiant; Cerebroprotective. MECHANISM OF ACTION : Serine/threonine-specific protein phosphatase inhibitor. Normal human fibroblasts were incubated with ApoA1 (A) (10 Microg/ml) or cantharidine (B) (1 MicroM), in presence of 1 mg/ml albumin, then the total amount of cholesterol in the culture supernatant determined by gas chromatography. The mean cholesterol efflux (relative to 100% in presence of albumin only) for (A) and (B) was 114 % and 176 % respectively.