Structural biology in drug design: Selective protein kinase inhibitors

Drug Discovery Today

Volumn 7, Issue 11, 2002, Pages 601-611

  Scapin, Giovanna ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 PHENYLAMINO PYRROLO[2,3 D]PYRIMIDINE; 4 PHENYLAMINOPYRAZOLO[2,3 D]PYRIMIDINE; 9 NITROPAULLONE; ADAPTOR PROTEIN; ADENOSINE TRIPHOSPHATE; CYCLIC AMP DEPENDENT PROTEIN KINASE; CYCLIN DEPENDENT KINASE; CYCLINE; DIMETHOXYQUINAZOLINE; EPIDERMAL GROWTH FACTOR RECEPTOR; FLAVOPIRIDOL; GUANOSINE TRIPHOSPHATASE; IMATINIB; INSULIN RECEPTOR KINASE; ISOFLAVONE DERIVATIVE; JANUS KINASE; LEFLUNOMIDE; MITOGEN ACTIVATED PROTEIN KINASE; MYOSIN LIGHT CHAIN KINASE; OLOMOUCINE; PAULLONE DERIVATIVE; PROTEIN KINASE (CALCIUM,CALMODULIN); PROTEIN KINASE INHIBITOR; PROTEIN TYROSINE KINASE; PYRIMIDINE DERIVATIVE; QUINAZOLINE DERIVATIVE; QUINOLONE DERIVATIVE; SOMATOMEDIN C; STAT PROTEIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; CDKN1A PROTEIN, HUMAN; CYCLIN DEPENDENT KINASE INHIBITOR 1A; ENZYME INHIBITOR; JAK3 PROTEIN, HUMAN; JANUS KINASE 3; PROTEIN KINASE; PROTEIN KINASE C;

BINDING SITE; CARBOXY TERMINAL SEQUENCE; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; IC 50; NONHUMAN; PROTEIN DOMAIN; PROTEIN PHOSPHORYLATION; PROTEIN STRUCTURE; REVIEW; SEQUENCE HOMOLOGY; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMISTRY; DRUG ANTAGONISM; DRUG EFFECT; METABOLISM; SRC HOMOLOGY DOMAIN;

ADENOSINE TRIPHOSPHATE; ANIMAL; BINDING SITES; CYCLINS; DRUG DESIGN; ENZYME INHIBITORS; HUMAN; PROTEIN KINASE C; PROTEIN KINASES; PROTEIN-TYROSINE KINASE; RECEPTOR, EPIDERMAL GROWTH FACTOR; SRC HOMOLOGY DOMAINS; ANIMALS; CYCLIN-DEPENDENT KINASE INHIBITOR P21; HUMANS; JANUS KINASE 3; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES;

EID: 0036591874     PISSN: 13596446     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1359-6446(02)02290-0     Document Type: Review

References (72)

1. Protein kinases and phosphatases: The yin and yang of protein phosphorylation and signaling
2. Structural basis for control by phosphorylation
3. Protein tyrosine phosphatases in signal transduction
4. Protein phosphatases - A phylogenetic perspective
5. Molecular reactions of protein phosphatases - Insights from structure and chemistry
6. Histidine phosphorylation and two-component signaling in eukaryotic cells
7. Growth factor signaling by receptor tyrosine kinases
8. Protein tyrosine kinase structure and function
9. MAP kinases
10. Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase
11. Protein kinases 6. The eukaryotic protein kinase superfamily: Kinase (catalytic) domain structure and classification
12. Active and inactive protein kinases: Structural basis for regulation
13. Kinetic and catalytic mechanisms of protein kinases
14. RTK mutations and human syndromes: When good receptors turn bad
15. Molecular and cellular interactions in rheumatoid synovium
16. Protein kinase inhibition: Natural and synthetic variations on a theme
17. Chemical inhibitors of protein kinases
18. The structure-based design of ATP-site directed protein kinases inhibitors
19. Protein tyrosine kinase inhibitors in cancer treatment
20. Protein tyrosine kinase inhibitors in cancer treatment (part II)
21. Protein kinase inhibitors: The tyrosine-specific protein kinases
22. Protein kinase inhibitors: Emerging pharmacophores 1997-2000
23. The Src homology-2 domains (SH2 domains) of the protein tyrosine kinase p56lck: Structure, mechanism and drug design
24. Recent advances in the design and synthesis of SH2 inhibitors of Src, Grb2 and ZAP-70
25. Progress in the development of inhibitors of SH2 domains
26. From consensus sequence peptide to high affinity ligand, a 'library scan' strategy
27. Substrate competitive inhibitors of IGF-1 receptor kinase
28. Mechanism-based design of a protein kinase inhibitor
29. Inhibitors of the JNK signaling pathway
30. P38 MAP kinase: Molecular target for the inhibition of pro-inflammatory cytokines
31. Protein kinase antagonists: Interim challenges and issues
32. Structural basis of inhibitor selectivity in MAP kinases
33. Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor
34. Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors
35. Structural basis for selective inhibition of Src family kinases by PP1
36. The cell cycle and drug discovery: The promise and the hope
37. Therapeutic potential of targeting the cell cycle
38. Phase I trial of continuous infusion flavopiridol, a novel cyclin-dependent kinase inhibitor, in patients with refractory neoplasms
39. Multiple modes of ligand recognition: Crystal structures of cyclin-dependent protein kinase 2 in complex with ATP and two inhibitors, olomoucine and isopentenyladenine
40. Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase
41. Structure-based design of potent CDK1 inhibitors derived from olomoucine
42. Identification of cyclin-dependent kinase 1 inhibitors of a new chemical type by structure-based drug design and database searching
43. Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition
44. Exploiting chemical libraries, structure and genomics in the search for kinase inhibitors
45. Structure-based inhibitor design for CDK2, a cell cycle controlling protein kinase
46. Crystallographic approach to identification of cyclin-dependent kinase 4 (CDK4)-specific inhibitors by using CDK4 mimic CDK2 protein
47. Antibodies to growth factors and receptors
48. Modeling study of protein kinase inhibitors:binding mode of staurosporine - Origin of the selectivity of CGP52411
49. Strategies toward the design of novel and selective protein tyrosine kinase inhibitors
50. Structure-based design of potent inhibitors of EGF-receptor tyrosine kinase as anti-cancer agents
51. Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methy-N-(2, 5-dibromophenyl)propenamide]
52. Structure-based design of a potent, selective and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases
53. The Janus protein tyrosine kinase family and its role in cytokine signaling
54. Differential substrate recognition capabilities of Janus family protein tyrosine kinases within the interleukin 2 receptor (IL2R) system: Jak3 as a potential molecular target for treatment of leukemias with a hyperactive Jak-Stat signaling machinery
55. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents
56. Structural mechanism for STI-571 inhibition of abelson tyrosine kinase
57. The protein kinase C family: Heterogeneity and its implications
58. Modular peptide recognition domains in eukaryotic signaling
59. Phosphoryltyrosyl mimetics in the design of peptide-based signal transduction inhibitors
60. Rational design, synthesis and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth
61. SH3 domains and drug design: Ligands, structure and biological function
62. Protein structure-based combinatorial chemistry: Discovery of non-peptide binding elements to Src SH3 domain
63. Exploiting the basis of proline recognition by SH3 and WW domains: Design of N-substituted inhibitors
64. Src homology-2 domains: Structure, mechanisms and drug discovery
65. Structure-based design of a novel series of nonpeptide ligands that bind to the pp60src SH2 domain
66. Structure-based design and synthesis of a novel class of SRC SH2 inhibitors
67. Structure-based design of novel bicyclic nonpeptide inhibitors for the Src SH2 domain
68. Structure-based design of an osteoclast-selective, nonpeptide Src homology 2 inhibitor with in vivo antiresorptive activity
69. Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain
70. Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic
71. Protein kinase Cα: A novel target for the therapy of androgen-independent prostate cancer?
72. Crystal structure of the cys2 activator-binding domain of protein kinase C δ in complex with phorbol ester