Elan Pharmaceuticals, Inc.

D Danielle Woods

Timothy Earl Benson

Donald Bryan Prince

Methods of using monoclinic crystals of human beta-secretase (BACE) having unit cell dimensions of a, b, and c, wherein a is about 81&#xb1;20 &#x212b; to about 101 &#x212b;, b is 103&#xb1;20 &#x212b;, c is 100&#xb1;20 &#x212b;, and &#x3b1;=&#x3b3;=90&#xb0;, and &#x3b2; is 105&#xb0;&#xb1;10&#xb0; for crystals of symmetry P2and a=73.1, b=105.1, c=50.5 &#x212b; and &#x3b2; is 94.8&#xb0; for crystals of C2 symmetry in drug screening assays comprising selecting a potential modifier by adding the potential modifiers to an aqueous mixture of the crystal and detecting a measure of binding, such that the potential modifier that binds is selected as a potential drug.

Methods of using crystals of beta amyloid cleaving enzyme (BACE)

The present invention provides a crystal of human beta-secretase (BACE) having monoclinic space group symmetry C2, in a representative example, comprising a unit cell having dimensions of a, b, and c, wherein a is about 53 &#x212b; to about 103 &#x212b;, b is about 85 &#x212b; to about 125 &#x212b;, c is about 40 &#x212b; to about 60 &#x212b;, and &#x3b1;=&#x3b3;=90&#xb0;, and &#x3b2; is about 85&#xb0; to about 105&#xb0;, and in a preferred example, comprising unit cell dimensions as follows: a is 73.1 &#x212b;, b is 105.1 &#x212b;, c is 50.5 &#x212b;, and &#x3b1;=&#x3b3;=90&#xb0;, and &#x3b2; is 94.8, wherein the Matthews coefficient of said crystal is 2.1 &#x212b;/Da with 42% solvent, and wherein said crystal diffracts to 1.7 &#x212b; resolution.

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Kalamazoo, MI, United States of America

D Danielle Woods