[Gamma-secretase inhibitors in Alzheimer's disease therapy].
Neuritic plaques, which are situated in the brain of Alzheimer's disease (AD) patients, are composed mainly of peptides containing 40 or 42 amino acid residues known as ß-amyloid plaques (Aß). The Aß peptide is the result of the enzymatic cleavage of the amyloid precursor protein (APP). In the so-called amyloidogenic pathway, the ß-secretase enzyme releases a protein fragment (C99), which is subsequently metabolized by the enzyme γ-secretase. Monomer forms of Aß are turned into oligomer forms, which are the main cause of cellular neuronal death in AD patients. The following study is focused on γ-secretase inhibitors that can slow down the production or accumulation of pathologic Aß deposits. γ secretase inhibitors that reached different phases of clinical trials are particularly reported as well as other promising groups of these analogues.
Univerzita obrany Hradec Kralove, Katedra Toxikologie.
Spilovská
S
Katarína
Korábečný
K
Jan
Kuča
K
Kamil
Musílek
M
Kamil
D000544:Alzheimer Disease / Q000188:drug therapy* / Q000378:metabolism; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016229:Amyloid beta-Peptides / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D058225:Plaque, Amyloid / Q000378:metabolism
D016229:Amyloid beta-Peptides; D053829:Amyloid Precursor Protein Secretases