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

G. Münch; Y. Taneli; E. Schraven; U. Schindler; R. Schinzel; D. Palm; P. Riederer

doi:10.1007/BF02260940

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

G. Münch, Y. Taneli, E. Schraven, U. Schindler, R. Schinzel, D. Palm, P. Riederer

Research output: Contribution to journal › Article › peer-review

77 Citations (Scopus)

Abstract

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

Original language	English
Pages (from-to)	193-208
Number of pages	16
Journal	Journal of Neural Transmission
Volume	8
Issue number	3
DOIs	https://doi.org/10.1007/BF02260940
Publication status	Published - Oct 1994
Externally published	Yes

Keywords

advanced glycosylation
amyloid
dementia of Alzheimer type
Maillard reaction
tenilsetam

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1007/BF02260940

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title = "The cognition-enhancing drug tenilsetam is an inhibitor of protein crosslinking by advanced glycosylation",

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

keywords = "advanced glycosylation, amyloid, dementia of Alzheimer type, Maillard reaction, tenilsetam",

author = "G. M{\"u}nch and Y. Taneli and E. Schraven and U. Schindler and R. Schinzel and D. Palm and P. Riederer",

year = "1994",

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T1 - The cognition-enhancing drug tenilsetam is an inhibitor of protein crosslinking by advanced glycosylation

AU - Münch, G.

AU - Taneli, Y.

AU - Schraven, E.

AU - Schindler, U.

AU - Schinzel, R.

AU - Palm, D.

AU - Riederer, P.

PY - 1994/10

Y1 - 1994/10

N2 - Non-enzymatic glycosylation of proteins, also called Maillard reaction, which occurs at an accelerated rate in diabetes, can lead to the formation of advanced glycosylation endproducts (AGEs). Tenilsetam (®CAS 997: (±)-3-(2-thienyl)-2-piperazinone), a cognition-enhancing drug successfully used for treatment of patients suffering from Alzheimer's disease, when included in the Maillard reaction apparently inhibits protein crosslinking by AGEs in vitro. According to the mechanism proposed, Tenilsetam acts via covalent attachment to glycated proteins, thus blocking the reactive sites for further polymerisation reactions. A beneficial effect of Tenilsetam in Alzheimer's disease could come from the interference with AGE-derived crosslinking of amyloid plaques and a decreased inflammatory response by diminished activation of phagocytosing microglia.

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

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KW - amyloid

KW - dementia of Alzheimer type

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

Abstract

Keywords

UN SDGs

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