Modulators and inhibitors of gamma- and beta-secretases.
Most gene mutations associated with Alzheimer's disease point to the metabolism of amyloid precursor protein as a potential cause. The beta- and gamma-secretases are two executioners of amyloid precursor protein processing resulting in amyloid-beta. Significant progress has been made in the selective inhibition of both proteases, regardless of structural information for gamma-secretase. Several peptidic and nonpeptidic leads were identified for both targets.
Schmidt
Boris
B
Clemens Schöpf Institute for Organic Chemistry and Biochemistry, TU Darmstadt, Darmstadt, Germany. Schmidt_Boris@t-online.de
Baumann
Stefanie
S
Narlawar
Rajeshwar
R
Braun
Hannes A
HA
Larbig
Gregor
G
D053829:Amyloid Precursor Protein Secretases / Q000187:drug effects* / Q000378:metabolism*; D016564:Amyloid beta-Protein Precursor / Q000378:metabolism; D000818:Animals; D015195:Drug Design; D006801:Humans; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D016564:Amyloid beta-Protein Precursor; D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases