Abstract:
The present invention relates to polypeptides which comprise the ligand binding domain of Lck, crystalline forms of these polypeptides, and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Lck. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain. The invention also relates to the use of the three dimensional structure of the Lck catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential selective inhibitors of Lck activity, for example, compounds which inhibit the binding of a native substrate to the Lck catalytic domain selectively.
Abstract:
The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
Abstract:
Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.
Abstract:
The present invention provides antibodies, and antigen-binding portions thereof, that bind to epitopes comprising at least one amino acid residues from residues 1-197 of the p40 subunit of IL-12 and/or IL-23. The invention further provides nucleic acids encoding the antibodies, compositions, vectors and host cells comprising the antibodies, and methods of making and using the same.
Abstract:
The present invention relates to a batch crystallization method for crystallizing anti-human TNFalpha (hTNFalpha) antibody and antibody fragments which allows the production of said antibody on an industrial scale; a method of controlling the size of antibody crystals, for example, crystals of anti-hTNFalpha antibody fragments, compositions containing said crystals as well as methods of use of said crystals and compositions.
Abstract:
The invention relates to batch crystallization methods for crystallizing an anti-hIL-12 antibody that allows the production of the antibody on an industrial scale, antibody crystals obtained according to the methods, compositions containing the crystals, and methods of using the crystals and the compositions.
Abstract:
La presente invención proporciona métodos para cristalizar anticuerpos y fragmentos de los mismos, así como cristales producidos de esta manera. Más particularmente la presente invención proporciona métodos para cristalizar fragmentos de anticuerpos Fab humanos y no humanos, ya sea solos o como co-cristales con su ligando objetivo. Por ejemplo, se proporciona un cristal que comprende un fragmento de múrido Fab del anticuerpo 125-2H o un fragmento Fab de humano del anticuerpo ABT-325, que enlaza a IL-18, así como un co-cristal de un fragmento Fab de múrido enlazado a IL-18. ABT-325 y 125-2H difieren significativamente en el carácter del sitio de combinación y en la arquitectura, explicando de esta forma su capacidad para enlazar a IL-18 en forma simultánea en epítopes distintos.