By Lorenzo A. Pinna, Patricia T.W. Cohen
The goals of this volume are to spotlight the great pharmacological strength of protein kinase and protein phosphatase inhibitors, to supply a radical assessment of the main amazing achievements within the box and to demonstrate how helpful those experiences might be for the development of either uncomplicated wisdom on organic legislation and deregulation and for the scientific therapy of a large spectrum of illnesses. This goal is attained by means of contributions of chief investigators within the box, who address the problem from assorted angles.
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Extra info for Inhibitors of Protein Kinases and Protein Phosphates
J Med Chem 41:2252–60 Ando S, Tsujimura K, et al (1993) Phosphorylation of synthetic vimentin peptides by cdc2 kinase. Biochem Biophys Res Commun 195:837–43 Ando S, Ikuhara T, et al (1997) Role of the pyrrolidine ring of proline in determining the substrate specificity of cdc2 kinase or cdk5. J Biochem [Tokyo] 122:409–14 Beaulieu PL, Cameron DR, et al (1999) Ligands for the tyrosine kinase p56lck SH2 domain: discovery of potent dipeptide derivatives with monocharged, nonhydrolyzable phosphate replacements.
2 CDKs and GSK-3 as Kinase Screening Targets . . . . . . . . . Kinase Purification and Assay . . . . . . . . . . . . . Pharmacological Inhibitors of CDKs and GSK-3 . . . . . . . . 2 . . . . . . 5 Paullones as CDK and GSK-3 Inhibitors. . . . . . . . Discovery of Paullones . . . . . . . . . . . . . Molecular Mechanism of Interaction of Paullones with Kinases— Structure/Activity Relationship Studies . . . . . . . . Selectivity of Paullones .
Nat Struct Biol 8:37–41 Pellicena P, Stowell KR, et al (1998) Enhanced phosphorylation of Src family kinase substrates containing SH2 domain binding sites. J Biol Chem 273:15325–8 Pinna LA, Ruzzene M (1996) How do protein kinases recognize their substrates? Biochim Biophys Acta 1314:191–225 Pluskey S, Wandless TJ, et al (1995) Potent stimulation of SH-PTP2 phosphatase activity by simultaneous occupancy of both SH2 domains. J Biol Chem 270:2897–900 Profit AA, Lee TR, et al (1999) Bivalent inhibitors of protein tyrosine kinases.
Inhibitors of Protein Kinases and Protein Phosphates by Lorenzo A. Pinna, Patricia T.W. Cohen