Memapsin 2, a drug target for Alzheimer's disease.
Mempasin 2, a beta-secretase, is the membrane-anchored aspartic protease that initiates the cleavage of amyloid precursor protein leading to the production of beta-amyloid and the onset of Alzheimer's disease. Thus memapsin 2 is a major therapeutic target for the development of inhibitor drugs for the disease. Many biochemical tools, such as the specificity and crystal structure, have been established and have led to the design of potent and relatively small transition-state inhibitors. Although developing a clinically viable mempasin 2 inhibitor remains challenging, progress to date renders hope that memapsin 2 inhibitors may ultimately be useful for therapeutic reduction of beta-amyloid.
Protein Studies Program, Oklahoma Medical Research Foundation, University of Oklahoma Medical Center, Oklahoma City, OK 73104, USA.
Gerald
G
Koelsch
Robert T
RT
Turner
Lin
L
Hong
Arun K
AK
Ghosh
Jordan
J
Tang
D000544:Alzheimer Disease / Q000188:drug therapy*; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D021381:Protein Transport; D013379:Substrate Specificity
D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases