The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Identification of Novel Purine and Pyrimidine Cyclin-Dependent Kinase Inhibitors with Distinct Molecular Interactions and Tumor Cell Growth Inhibition Profiles
Open accessAbstract
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) and formed a triplet of hydrogen bonds (i.e., NH-9 to Glu 81, N-3 to Leu 83, and 2-NH2 to Leu 83). The triplet of hydrogen bonding and CDK inhibition was reproduced by 2,6-diamino-4-cyclohexylmethyloxy-5-nitrosopyrimidine (NU6027, Ki values: CDK1, 2.5 +/- 0.4 microM; CDK2, 1.3 +/- 0.2 microM). Against human tumor cells, NU2058 and NU6027 were growth inhibitory in vitro (mean GI50 values of 13 +/- 7 microM and 10 +/- 6 microM, respectively), with a pattern of sensitivity distinct from flavopiridol and olomoucine. These CDK inhibition and chemosensitivity data indicate that the distinct mode of binding of NU2058 and NU6027 has direct consequences for enzyme and cell growth inhibition.
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Sherr, C. J. (1996) · Science · doi:10.1126/science.274.5293.1672 · Cited by 5,379
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Knockaert, M., Greengard, P., & Meijer, L. (2002) · Trends in Pharmacological Sciences · doi:10.1016/s0165-6147(02)02071-0 · Cited by 537
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Mazanetz, M. P., & Fischer, P. M. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2111 · Cited by 459
Targeting Cyclin-Dependent Kinases in Human Cancers: From Small Molecules to Peptide Inhibitors
Peyressatre, M., Prével, C., Pellerano, M., & Morris, M. (2015) · Cancers · doi:10.3390/cancers7010179 · Cited by 344
KLIFS: A Knowledge-Based Structural Database To Navigate Kinase–Ligand Interaction Space
van Linden, O. P. J., Kooistra, A. J., Leurs, R., de Esch, I. J. P., & de Graaf, C. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm400378w · Cited by 298
Metadata
- Authors
- Arris, C. E., Boyle, F. T., Calvert, A. H., Curtin, N. J., Endicott, J. A., Garman, E. F., Gibson, A. E., Golding, B. T., Grant, S., Griffin, R. J., Jewsbury, P., Johnson, L. N., Lawrie, A. M., Newell, D. R., Noble, M. E. M., Sausville, E. A., Schultz, R., & Yu, W.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2000-07-01
- Volume
- 43
- Issue
- 15
- Pages
- 2797-2804
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2073275756
- Cited by
- 215
- References
- 1
- FWCI
- 12.78
- Type
- journal article
- Language
- en
- Open access
- green
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