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Molecular Cancer Therapeutics
Molecular Cancer Therapeutics
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About the Cover

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On The Cover

Superposition of the X-ray structures of aminoimidazo[1,2-a]pyridine (green carbons) and ATP (magenta carbons) bound to CDK2 (grey tube). The imidazopyridine moiety within the inhibitor occupies the same site as the ATP adenine. N-1 of the imidazopyridine acts as a hydrogen bond acceptor to the backbone amine NH of Leu83 and the amino group acts as a hydrogen bond donor to the backbone carbonyl of Leu83. The structure-based design approach directed the evolution of a chemical scaffold yielding potent CDK2 inhibitors. These inhibitors selectively inhibited the CDK2 dependent phosphorylation of Rb and induced caspase-3 dependent apoptosis in HCT116 tumor cells. For details, see 1 et al. in this issue.

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Molecular Cancer Therapeutics: 3 (1)
January 2004
Volume 3, Issue 1
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Issue Highlights

  • The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines
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Molecular Cancer Therapeutics
eISSN: 1538-8514
ISSN: 1535-7163

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