Donald Coen - Medfield MA, US James Hogle - Newton MA, US Carl Elkin - Cambridge MA, US Harmon J. Zuccola - Brookline MA, US Kristie Grove Bridges - Maynard MA, US Scott Lokey - Santa Cruz CA, US
Assignee:
President and Fellows of Harvard College - Cambridge MA
A method for the structure-based identification and selection of inhibitors of processivity factor binding to protein is disclosed herein. Characterization of the protein/processivity factor interface is given. Methods for the structure-based inhibition of processivity factor binding to protein are also given. One embodiment includes a class of peptidomimetics that mimic helical portions of proteins. In addition, methods of treatment of various diseases are given, using the inhibitors of the invention.
Crystal Structure Of Human Jak3 Kinase Domain Complex And Binding Pockets Thereof
The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexed with AMP-PNP.
Crystal Structure Of Human Jak3 Kinase Domain Complex And Binding Pockets Thereof
Harmon Zuccola - Westwood MA, US Marc Jacobs - Boston MA, US Lovorka Swenson - Belmont MA, US Kumkum Saxena - Framingham MA, US
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
International Classification:
C12N 9/00 C12N 9/10
US Classification:
435183, 435194
Abstract:
The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexed with AMP-PNP.
This invention relates to HDAg peptides, including mutants, derivatives fragments and fusion molecules, including fusion proteins, coiled-coil oligomers, nucleic acid molecules, vectors comprising HDAg nucleic acid molecules, cells comprising said molecules, methods of multivalent expression and association of binding moieties of HDAg fusion molecules, and methods of use involving the molecules. The molecules are particularly useful as a framework for multivalent display via formation of C-terminal and/or N-terminal fusion proteins or via chemical coupling to chemically reactive sidechains, e.g. cysteine residues.
Structure-Based Approach To Design Of Protein-Processivity Factor Interactions
Donald Coen - Medfield MA, US James Hogle - Newton MA, US Carl Elkin - Cambridge MA, US Harmon Zuccola - Brookline MA, US Kristie Bridges - Arlington MA, US Scott Lokey - Santa Cruz CA, US
International Classification:
C40B 30/02 C40B 30/06 G06F 19/00
US Classification:
702019000
Abstract:
A method for the structure-based identification and selection of inhibitors of processivity factor binding to protein is disclosed herein. Characterization of the protein/processivity factor interface is given. Methods for the structure-based inhibition of processivity factor binding to protein are also given. One embodiment includes a class of peptidomimetics that mimic helical portions of proteins. In addition, methods of treatment of various diseases are given, using the inhibitors of the invention.
Structure-Based Approach To Design Of Inhibitors Of Protein-Processivity Factor Interactions
Donald Coen - Medfield MA, US James Hogle - Newton MA, US Carl Elkin - Cambridge MA, US Harmon J. Zuccola - Brookline MA, US Kristie Grove Bridges - Maynard MA, US Scott Lokey - Santa Cruz CA, US
International Classification:
C40B 30/04
US Classification:
506 9
Abstract:
A method for the structure-based identification and selection of inhibitors of processivity factor binding to protein is disclosed herein. Characterization of the protein/processivity factor interface is given. Methods for the structure-based inhibition of processivity factor binding to protein are also given. One embodiment includes a class of peptidomimetics that mimic helical portions of proteins. In addition, methods of treatment of various diseases are given, using the inhibitors of the invention.
Crystal Structure Of Human Jak3 Kinase Domain Complex And Binding Pockets Thereof
Harmon Zuccola - Westwood MA, US Marc Jacobs - Boston MA, US Lovorka Swenson - Belmont MA, US Kumkum Saxena - Framingham MA, US
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED - CAMBRIDGE MA
International Classification:
C12Q 1/48
US Classification:
435 15, 435194
Abstract:
The present invention relates to human Janus Kinase 3 (JAK3) and JAK3-like binding pockets. The present invention provides a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. This invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention relates to methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to JAK3 protein or JAK3 protein homologues, or complexes thereof. The invention also relates to crystallizable compositions and crystals comprising JAK3 kinase domain and JAK3 kinase domain complexes with AMP-PNP.
James M. Hogle - Newton MA, US Harmon J. Zuccola - Brookline MA, US David Filman - Auburndale MA, US Carl Elkin - Cambridge MA, US
Assignee:
President and Fellows of Harvard College - Cambridge MA
International Classification:
C12P 2102
US Classification:
435 697, 435 5, 435 41, 435 693, 530350
Abstract:
This invention relates to HDAg peptides, including mutants, derivatives fragments and fusion molecules, including fusion proteins, coiled-coil oligomers, nucleic acid molecules, vectors comprising HDAg nucleic acid molecules, cells comprising said molecules, methods of multivalent expression and association of binding moieties of HDAg fusion molecules, and methods of use involving the molecules. The molecules are particularly useful as a framework for multivalent display via formation of C-terminal and/or N-terminal fusion proteins or via chemical coupling to chemically reactive sidechains, e. g. cysteine residues.
Vertex Pharmaceuticals
Research Fellow I
Harvard Medical School 2000 - 2001
Co-director Structural Genomics of Cancer Initiative
Harvard Medical School 1992 - 2000
Postdoctoral Fellow
Education:
Harvard Medical School 1992 - 2000
Postgraduate, Structural Biology
Georgia Institute of Technology 1986 - 1992
Ph.D., Biochemistry
University of Florida 1982 - 1986
B.S., Chemistry
Skills:
Structural Biology Drug Design Protein Chemistry Drug Discovery X Ray Crystallography Crystallography Biochemistry Biotechnology Drug Development Life Sciences In Vivo Lead Optimization Biophysics