I owned Athena before Elan took them out, another random piece of the puzzle.....
J Med Chem 2002 Jan 17;45(2):259-62
Design of Substrate-Based Inhibitors of Human beta-Secretase.
Tung JS, Davis DL, Anderson JP, Walker DE, Mamo S, Jewett N, Hom RK, Sinha S, Thorsett ED, John V.
Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, California 94080.
By use of the effectively cleaved beta-secretase (BACE) substrate (1), incorporation of a statine in P(1) resulted in a weak inhibitor 13 of the enzyme. Further substitution of P(1)'-Asp by P(1)'-Val in 13 results in a potent inhibitor 22 of BACE. Removal of the P(10)-P(5) residues on the N-terminal part of inhibitor 22 resulted in no loss of potency (23). C-terminal truncations of inhibitor 22 generally led to significant loss of potency. |
