Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.

Substituted guanines and pyrimidines were tested as inhibitors of cyclin B1/CDK1 and cyclin A3/CDK2 and soaked into crystals of monomeric CDK2. O6-Cyclohexylmethylguanine (NU2058) was a competitive inhibitor of CDK1 and CDK2 with respect to ATP (Ki values: CDK1, 5 +/- 1 microM; CDK2, 12 +/- 3 microM...

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Main Authors: Arris, C, Boyle, F, Calvert, A, Curtin, N, Endicott, J, Garman, E, Gibson, A, Golding, B, Grant, S, Griffin, R, Jewsbury, P, Johnson, L, Lawrie, A, Newell, DR, Noble, M, Sausville, E, Schultz, R, Yu, W
Format: Journal article
Language:English
Published: 2000