Beta secretase: Difference between revisions
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{{STRUCTURE_1w51 | PDB=1w51 | SCENE=Beta_secretase/Default3/1 }} | |||
<scene name='Beta_secretase/Default3/1'>β-Secretase</scene>, also known as '''BACE''' ('''β'''-site of '''A'''myloid precursor protein '''C'''leaving '''E'''nzyme) and '''Memapsin 2''', is an aspartyl protease found in humans. β-Secretase plays an important role in the development of Alzheimer's disease. This has made β-secretase a therapeutic target for pharmacological intervention. | <scene name='Beta_secretase/Default3/1'>β-Secretase</scene>, also known as '''BACE''' ('''β'''-site of '''A'''myloid precursor protein '''C'''leaving '''E'''nzyme) and '''Memapsin 2''', is an aspartyl protease found in humans. β-Secretase plays an important role in the development of Alzheimer's disease. This has made β-secretase a therapeutic target for pharmacological intervention. | ||
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[[Image:Om99 reaction.PNG|center]] | [[Image:Om99 reaction.PNG|center]] | ||
OM99-2 remains stabilized in the pocket by binding to the other pockets of β-secretase (S1, S2, S2', and S3). Additionally, OM99-2 is able to interact with other residues in β-secretase (in this case Gly34 and Thr232), though this is not the case for all inhibitors. | OM99-2 remains stabilized in the pocket by binding to the other pockets of β-secretase (S1, S2, S2', and S3). OM99-2 complexed with β-secretase shows the hydrophobic nature of the S1 and S3 pockets. Additionally, OM99-2 is able to interact with other residues in β-secretase (in this case Gly34 and Thr232), though this is not the case for all inhibitors. | ||
Numerous tests have been conducted with OM99-2 as an inhibitor, the results have been mainly positive. However, there have occurred a substantial number of times results where the flap only partially closes and the 10s loop closes off the S3 pocket. While the inhibitor works well when it is stabilized within β-secretase, the fact that it does not always stabilize keeps the inhibitor from being consumed by humans. | Numerous tests have been conducted with OM99-2 as an inhibitor, the results have been mainly positive. However, there have occurred a substantial number of times results where the flap only partially closes and the 10s loop closes off the S3 pocket. While the inhibitor works well when it is stabilized within β-secretase, the fact that it does not always stabilize keeps the inhibitor from being consumed by humans. | ||
