Schering Corporation

Wenyan Wang

Vincent Stewart Madison

Shahriar Shane Taremi

Winifred W Prosise

Corey Strickland

Paul Reichert

Brian M Beyer

Bruce A Malcolm

Jun Zou

Eileen Wilson

Li Xiao

Charles A Lesburg

Hung V Le

Kuo-Chi Cheng

Jian-Jun Liu

Peter Orth

The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of &#x3b2;-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Refolded recombinant &#x3b2;-secretase crystals and methods for preparing and using the same

The present invention relates to Pregnane X receptor (PXR) polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.

Crystal of pregnane X receptor fused to steroid receptor coactivator-1

The present invention relates, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.

Pregnane X receptor compositions, crystals and uses thereof

The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of &#x3b2;-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding human BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Method for making &#x3b2;-secretase co-crystals complexed with a ligand

The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure-based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.

Catalytic domain of ADAM33 and methods of use thereof

The present invention discloses purified polypeptides that comprise an active human ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human ADAM33 catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human ADAM33. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human ADAM33 in structure based drug design to identify compounds that can modulate the enzymatic activity of human ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the human ADAMS33 catalytic domain.

Crystalline form of an n231 mutant catalytic domain of ADAM33 and methods of use thereof

The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of &#x3b2;-secretase (BACE) polypeptide. Polypeptides used herein are derived from human BACE which is also known by the synonyms 'mamapsin 2', 'human &#x3b2;-site APP-cleaving enzyme, and Asp2'. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

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Edison, NJ, United States of America

Wenyan Wang