| abstract |
PROBLEM TO BE SOLVED: To provide a therapeutic use of an intracellular kinase inhibitor in a patient having a T cell malignancy, a B cell malignancy, an autoimmune disorder, and a transplanted organ. A protein kinase inhibitor represented by formula (II) that binds to a DKC triad kinase active site, wherein: (a) within the hydrogen bond distance to the amino group of lysine in the catalytic double pair in the kinase active site A proton acceptor located in the kinase active site of (b); (b) an abstractable proton in the hydrogen bond adjacent to the catalytic bipartite aspartate in the kinase active site; (c) β-elimination occurs due to further electron rearrangement; A leaving group that results in the generation of a Michael acceptor in the inhibitor; (d) ATP binding selected from the group consisting of the hinge region of the kinase, several hydrophobic residues, hydrophilic residues, and combinations thereof A protein kinase inhibitor comprising a kinase binding moiety having affinity for a portion of a site. [Selection figure] None |