Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving transferase
Patent
1998-02-18
2000-12-19
Nashed, Nashaat T.
Chemistry: molecular biology and microbiology
Measuring or testing process involving enzymes or...
Involving transferase
435194, 702 19, C12Q 148, G06F 1900
Patent
active
061626139
ABSTRACT:
The invention relates to methods for designing inhibitors of serine/threonine kinases and tyrosine kinases, particularly MAP kinases, through the use of ATP-binding site mutants of those kinases. The methods of this invention take advantage of the fact that the mutant kinases are capable of binding inhibitory compounds of other kinases with greater affinity than the corresponding wild-type kinase. The invention further relates to the mutant kinases themselves and crystallizable co-complexes of the mutant kinase and the inhibitory compound.
REFERENCES:
Singh et al., "Structure-Based Design of a Potent, Selective, and Irreversible Inhibitor of the Catalytic Domain of the erbB Receptor Subfamily of Protein Tyrosine Kinases," J. Med. Chem. 40, 1130-1135 (1997).
Wilson et al., "The Structural Basis for the Specificity of Pyridinylimidazole Inhibitors of p38 MAP Kinase," Chem. & Biol. 4, 423-431 (1997).
Gum et al., "Acquisition of Sensitivity of Stress-Activated Protein Kinases to the p38 Inhibitor, SB 203580, by Alteration of One or More Amino acids within the ATP Binding Pocket," J. Biol. Chem. 273, 15605-15610 (1998).
Goldsmith et al., "Protein Kinases," Curr. Opin. Struct. Biol. 4, 833-840 (1994).
Johnson et al., "Active and Inactive Protein Kinases: Structural Basis for Regulation," Cell 85, 149-158 (1996).
Taylor et al., "Three Protein Kinase Structures Define a Common Motif," Structure 2, 345-355 (1994).
Fox et al. "A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazol inhibitors of p38 MAP kinase" Protein Scince 7, 2249-2255, Nov. 1998.
Fox Ted
Germann Ursula A.
Su Michael Shin-San
Wilson Keith Philip
Brown Karen E.
Haley James F.
Nashed Nashaat T.
Vertex Pharmaceuticals Inc.
LandOfFree
Methods for designing inhibitors of serine/threonine-kinases and does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Methods for designing inhibitors of serine/threonine-kinases and, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Methods for designing inhibitors of serine/threonine-kinases and will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-270104