Schering Corporation

Merck Sharp + Dohme Corp.

Brian M Beyer

Richard N Ingram

Corey Strickland

Peter Orth

Bruce A Malcolm

Leonard G Presta

Andrew Joseph Prongay

Wenyan Wang

Yan-Hui Liu

Eileen Wilson

Vincent Stewart Madison

Paul Reichert

Alan W Hruza

F George Njoroge

Hung V Le

Rumin Zhang

William T Windsor

Thomas E Hesson

Krishna Kalghatgi

James P Durkin

Jennifer Joanne Gesell

Michael R Ziebell

Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.

Engineered anti-IL-23p19 antibodies

The present invention relates to factor IXa complexes and crystals thereof as well as methods for identifying inhibitors of factor IXa.

Factor IXa crystals, related complexes and methods

The present invention provides methods for identifying modulators of PCSK9, for example, using a variety of assay formats. Inhibitors of PCSK9 can be used for example, to treat diseases such as hyperlipidemia and related disorders.

Assay for PCSK9 inhibitors

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 discloses a modified tumor necrosis factor-alpha converting enzyme (TACE) catalytic domain, that unlike the native TACE catalytic domain, is stable at high protein concentrations. The present invention further discloses methods for generating crystals of the modified TACE protein in protein-ligand complexes with a number of inhibitors. In addition, the present invention discloses methods of using the proteins, crystals and/or three-dimensional structures obtained to identify compounds that can modulate the enzymatic activity of TACE.

Modified tumor necrosis factor-alpha converting enzyme and methods of use thereof

Engineered anti-IL-23 antibodies

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

Methods for identifying modified tumor necrosis factor-alpha converting enzyme inhibitors

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.

Codon-optimized &#x3b2;-secretase and methods of refolding and processing

Novel chromogenic, fluorogenic and fluorescence polarization substrates which are useful in HCV NS3 protease and inhibitor assays.

Peptide substrates for HCV NS3 protease assays

Growing community of inventors

Lincroft, NJ, United States of America

Brian M Beyer