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Design and Synthesis of a Heterocyclic Compound Collection for Probing the Spatial Charactistics of ATP Binding Sites Presented at the CSIR Conference.

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Presentation on theme: "Design and Synthesis of a Heterocyclic Compound Collection for Probing the Spatial Charactistics of ATP Binding Sites Presented at the CSIR Conference."— Presentation transcript:

1 Design and Synthesis of a Heterocyclic Compound Collection for Probing the Spatial Charactistics of ATP Binding Sites Presented at the CSIR Conference Centre CSIR Biosciences C.P. Kenyon, P.M. Matlaba, C.J. Parkinson, A.L. Rousseau and C.W. van der Westhuyzen February 28, 2006

2 Slide 2 © CSIR 2006 www.csir.co.za The kinases The nature of the ATP site A basis for selectivity Types of potential guest molecules Methodology for preparation

3 Slide 3 © CSIR 2006 www.csir.co.za The Kinases Proteins which transfer phosphoryl residues Utilise ATP as phosphate source All have an ATP site Why are kinases attractive targets?

4 Slide 4 © CSIR 2006 www.csir.co.za Basic Structural Characteristics of the ATP Site

5 Slide 5 © CSIR 2006 www.csir.co.za Pharmaceutical example: Interactions of SB203580 in the p38 MAP Kinase

6 Slide 6 © CSIR 2006 www.csir.co.za Rational Basis of Design

7 Slide 7 © CSIR 2006 www.csir.co.za Scaffold Selection Pyrimidines PurinesImidazopyridines

8 Slide 8 © CSIR 2006 www.csir.co.za Spatial Comparison of Scaffolds

9 Slide 9 © CSIR 2006 www.csir.co.za Pyrimidines and Purines

10 Slide 10 © CSIR 2006 www.csir.co.za Synthesis of Pyrimidines and Purines

11 Slide 11 © CSIR 2006 www.csir.co.za

12 Slide 12 © CSIR 2006 www.csir.co.za Imidazopyridines

13 Slide 13 © CSIR 2006 www.csir.co.za The Classical Approach

14 Slide 14 © CSIR 2006 www.csir.co.za Diversity Orientated Approach

15 Slide 15 © CSIR 2006 www.csir.co.za

16 Slide 16 © CSIR 2006 www.csir.co.za

17 Slide 17 © CSIR 2006 www.csir.co.za The Way Ahead Explore the untapped dimension Kinase and ATP –ase studies

18 Thanks To……… CSIR Thematic Programmes Department of Science and Technology

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