New York University

Sugen Incorporated

Stevan R Hubbard

Joseph Schlessinger

Moosa Mohammadi

Xiang-peng Kong

Zhongtao Zhang

Alexander Plotnikov

The determination and use of three dimensional structures of receptor protein tyrosine kinases and/or their ligands are described. One particular group of such structures includes three dimensional structures of the extracellular domain of RPTKs. The three dimensional structures of RPTKs can faciliate the design and identification of modulators of RPTK function. Other such structures can include of RPTK ligands, such as stem cell factor or a fragment thereof. Modulators of RPTK function can be used to treat diseases that are mediated by inappropriate RPTK activity.

Crystal of fibroblast growth factor receptor 1 in complex with fibroblast growth factor

Crystals of the tyrosine kinase domain of cytoplasmic tyrosine kinases and receptor tyrosine kinases that undergo ligand-mediated receptor dimerization are provided. In particular, crystals of a mutant of the tyrosine kinase domain of fibroblast growth factor receptor 1 (FLGK), alone and in complex with a non-hydrolyzable adenosine triphosphate analogue, are provided. Also provided are the high resolution three dimensional structures of crystalline FLGK, both alone and in co-complex with the adenosine triphosphate analogue, as determined by X-ray diffraction.

Crystals of the tyrosine kinase domain of non-insulin receptor tyrosine kinases

Crystals of the tyrosine kinase domain of non-insulin receptor tyrosine

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Riverside, NY, United States of America

Stevan R Hubbard