The cognition-enhancing drug tenilsetam is an inhibitor of protein crosslinking by advanced glycosylation

作者: G Münch , Y Taneli , E Schraven , U Schindler , R Schinzel

DOI: 10.1007/BF02260940

关键词:

摘要: Non-enzymatic glycosylation of proteins, also called Maillard reaction, which occurs at an accelerated rate in diabetes, can lead to the formation advanced endproducts (AGEs). Tenilsetam (®CAS 997: (±)-3-(2-thienyl)-2-piperazinone), a cognition-enhancing drug successfully used for treatment patients suffering from Alzheimer's disease, when included reaction apparently inhibits protein crosslinking by AGEs vitro. According mechanism proposed, acts via covalent attachment glycated thus blocking reactive sites further polymerisation reactions. A beneficial effect disease could come interference with AGE-derived amyloid plaques and decreased inflammatory response diminished activation phagocytosing microglia.

参考文章(51)
Stalinska K, Guzdek A, Glycated proteins as inducers of acute phase cytokines. Folia Histochemica Et Cytobiologica. ,vol. 30, pp. 167- ,(1992)
Brownlee M, Vlassara H, Cerami A, Role of advanced glycosylation products in complications of diabetes. Diabetes Care. ,vol. 11, pp. 73- 79 ,(1988)
J-P. Brion, M. E. Cheetham, M. Coleman, G. Dale, J-M. Gallo, D. P. Hanger, A. Probst, D. C. Smith, B. H. Anderton, Molecular and cellular changes associated with neurofibrillary tangles and senile plaques Alzheimer's disease: Epidemiology, Neuropathology, Neurochemistry, Clinics.. pp. 131- 139 ,(1990) , 10.1007/978-3-7091-3396-5_13
Richard Bucala, Anthony Cerami, None, Advanced glycosylation: chemistry, biology, and implications for diabetes and aging. Advances in pharmacology (San Diego). ,vol. 23, pp. 1- 34 ,(1992) , 10.1016/S1054-3589(08)60961-8
Giancarlo Pepeu, Giacomo Spignoli, Nootropic drugs and brain cholinergic mechanisms Progress in Neuro-psychopharmacology & Biological Psychiatry. ,vol. 13, ,(1989) , 10.1016/0278-5846(89)90112-7
Ursula Schindler, Pre-clinical evaluation of cognition enhancing drugs Progress in Neuro-psychopharmacology & Biological Psychiatry. ,vol. 13, ,(1989) , 10.1016/0278-5846(89)90114-0
Martinus A.M. van Boekel, Paul J.P.C. van den Bergh, Herman J. Hoenders, Glycation of human serum albumin: inhibition by Diclofenac. Biochimica et Biophysica Acta. ,vol. 1120, pp. 201- 204 ,(1992) , 10.1016/0167-4838(92)90270-N
Detlef Schlondorff, Cellular mechanisms of lipid injury in the glomerulus. American Journal of Kidney Diseases. ,vol. 22, pp. 72- 82 ,(1993) , 10.1016/S0272-6386(12)70171-3