A novel approach for the development of selective Cdk4 inhibitors: Library design based on locations of Cdk4 specific amino acid residues

Journal of Medicinal Chemistry

Volumn 44, Issue 26, 2001, Pages 4628-4640

  Honma, T ^a   Yoshizumi, T ^a   Hashimoto, N ^a   Hayashi, K ^a   Kawanishi, N ^a   Fukasawa, K ^a   Takaki, T ^a   Ikeura, C ^a   Ikuta, M ^a   Suzuki Takahashi, I ^a   Hayama, T ^a   Nishimura, S ^a   Morishima, H ^a  

^a TAIHO PHARMACEUTICAL CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ALIPHATIC AMINE; ASPARTIC ACID; CYCLIN DEPENDENT KINASE 4; CYCLIN DEPENDENT KINASE INHIBITOR; GLYCINE; N (5 OXO 2,3,5,9B TETRAHYDRO 1H PYRROLO[2,1 A]ISOINDOL 9 YL) N' (1H PYRAZOL 3 YL)UREA; N (5 OXO 2,3,5,9B TETRAHYDRO 1H PYRROLO[2,1 A]ISOINDOL 9 YL) N' [5 [[(5 CHLORO 2,3 DIHYDRO 1H INDEN 2 YL)AMINO]METHYL] 1H PYRAZOL 3 YL]UREA; PYRAZOLE DERIVATIVE; THREONINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CANCER CELL CULTURE; CELL CYCLE G1 PHASE; DRUG BINDING; DRUG DESIGN; DRUG INHIBITION; DRUG SELECTIVITY; HYDROGEN BOND; HYDROPHILICITY; MITOSIS INHIBITION; MOLECULAR MODEL; NONHUMAN; PROTEIN INTERACTION; STRUCTURE ACTIVITY RELATION;

ADENOSINE TRIPHOSPHATE; AMINO ACID SEQUENCE; COMBINATORIAL CHEMISTRY TECHNIQUES; CRYSTALLOGRAPHY, X-RAY; CYCLIN-DEPENDENT KINASE 4; CYCLIN-DEPENDENT KINASES; DRUG DESIGN; ENZYME INHIBITORS; G1 PHASE; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; PROTEIN BINDING; PROTO-ONCOGENE PROTEINS; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP; TUMOR CELLS, CULTURED; UREA;

EID: 0035924240     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010326y     Document Type: Article

References (44)

1. Cyclins and cyclin-dependent kinases: Take your partners
2. D-type cyclins
3. Cell cycle-dependent phosphorylation of the tumor suppressor RB protein
4. The retinoblastoma protein and a cell cycle control
5. Direct binding of cyclin D to the retinoblastoma gene product (pRB) and pRB phosphorylation by the cyclin D-dependent kinase CDK4
6. Cyclin D1 is nuclear protein required for cell cycle progression in G1
7. Cell-cycle regulators and cancer
8. Inhibitors of cyclin-dependent kinases as therapeutic agents for the treatment of cancer
9. Structure-based generation of a new class of potent Cdk4 inhibitors: New de novo design strategy and library design
10. Structural basis of cyclin-dependent kinase activation by phosphorylation
11. Crystallographic approach to identification of cyclin dependent kinase 4 (CDK4) specific inhibitors by using CDK4 mimic CDK2 protein
12. Universal control mechanism regulating onset of M-phase
13. Cyclins and cell cycle check-points
14. A restriction point for control of normal animal cell proliferation
15. Animal cell cycle
16. Structure-based design of a novel, potent, and selective inhibitor for MMP-13 utilizing NMR spectroscopy and computer-aided molecular design
17. Structure-based design of a low molecular weight, nonphosphorus, nonpeptide, and highly selective inhibitor of protein-tyrosine phosphatase 1B
18. Structure-based design of COX-2 selectivity into flurbiprofen
19. Structural basis for selective inhibition of cyclooxygenase-2 by antiinflammatory agents
20. The protein kinase family: Conserved features and deduced phylogeny of the catalytic domains
21. Protein kinase catalytic domain sequence database: Identification of conserved features of primary structure and classification of family members
22. Protein kinases. 6. The eukaryotic protein kinase superfamily: Kinase (catalytic) domain structure and classification
23. The structure-based design of ATP-site directed protein kinase inhibitors
24. Mechanisms of p38cdc2 regulation
25. Structural basis for inhibition of the cyclin-dependent kinase Cdk6 by the tumor suppressor p16INK4a
26. Structural basis of inhibition of CDK-cyclin complexes by INK4 inhibitors
27. Crystal structure of the complex of the cyclin D-dependent kinase Cdk6 bound to the cell-cycle inhibitor p19INK4d
28. Retinoblastoma-protein-dependent cell-cycle inhibition by the tumor suppressor p16
29. Tumor-derived p16 encoding proteins defective in cell-cycle inhibition
30. An introduction to de novo ligand design
31. The computer program LUDI: A new method for the de novo design of enzyme inhibitors
32. LUDI: Rule-based automatic design of new substituents for enzyme inhibitor leads
33. Recent developments in the chemistry of 3(5)-aminopyrazoles
34. Aminopyrazole; II. C-Unsubstituierte 1-alkyl-3-aminopyrazole aus 2-chloroacrylnitril bzw. 2,3-dichloropropannitril und alkylhydrazinen
35. 3:5-Dioxo-1:2-diphenylpyrazolidines. The 4-hydroxy- and certain 4-alkoxy- and 4-alkylamino-analogues
36. Butyrolactone I, a selective inhibitor of cdk2 and cdc2 kinase
37. The consensus motif for phosphorylation by cyclin D1-Cdk4 is different from that for phosphorylation by cyclin A/E-Cdk2
38. Homogeneous proximity tyrosine kinase assays: Scintillation proximity assay versus homogeneous time-resolved fluorescence