Structure of human methionine aminopeptidase-2 complexed with fumagillin

Science

Volumn 282, Issue 5392, 1998, Pages 1324-1327

  Liu, Shenping ^a   Widom, Joanne ^a   Kemp, Christopher W ^b   Crews, Craig M ^c   Clardy, Jon ^a  

^a Cornell University ^*  (United States)

^b Kemp Biotechnologies Inc   (United States)

^c YALE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINOPEPTIDASE; FUMAGILLIN; METHIONINE DERIVATIVE;

ANGIOGENESIS; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER; COMPLEX FORMATION; DRUG DESIGN; DRUG STRUCTURE; ENZYME STRUCTURE; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION;

EID: 0032515029     PISSN: 00368075     EISSN: None     Source Type: Journal    
DOI: 10.1126/science.282.5392.1324     Document Type: Article

References (31)

1. J. Folkman, Nature Med. 1, 27 (1995).
2. M. McCowen, M. Callender, J. F. Lawlis Jr., Science 113, 202 (1951); F. R. Hanson and T. E. Eble, J. Bacteriol. 58, 527 (1949).
3. M. McCowen, M. Callender, J. F. Lawlis Jr., Science 113, 202 (1951); F. R. Hanson and T. E. Eble, J. Bacteriol. 58, 527 (1949).
4. D. Ingber et al., Nature 348, 555 (1990).
5. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
6. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
7. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
8. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
9. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
10. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
11. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
12. B. J. Dezube et al., J. Clin. Oncol. 16, 1444 (1998); Y. Kawarada et al., Pancreas 15, 251 (1997); H. Konno et al., Cancer 77, 1736 (1996); Y. Ohta et al., Br. J. Cancer 75, 512 (1997); Y. Singh et al., Breast Cancer Res. Treat. 45, 15 (1997); E. Wassberg and R. Christofferson, Eur. J. Cancer 33, 2020 (1997); J. L. Xia et al., J. Cancer Res. Clin. Oncol. 123, 383 (1997); P. Twardowski and W. J. Gradishar, Curr. Opin. Oncol. 9, 584 (1997).
13. N. Sin et al., Proc. Natl. Acad. Sci. U.S.A. 94, 6099 (1997).
14. E. C. Griffith et ai, Chem. Biol. 4, 461 (1997).
15. J. Wang, N. Quan, J. Henkin, Proc. Am. Assoc. Cancer Res. 39, 98 (abstr.) (1998).
16. S. M. Arfin et al., Proc. Natl. Acad. Sci. U.S.A. 92, 7714 (1995).
17. 2.
18. Crystals of HsMetAP-2 were grown in 1 to 2 weeks at 4°C from sitting drops, with a protein concentration of 12 mg/ml in 10 mM Hepes (pH 7.2), 10% glycerol, and 100 mM NaCl. The reservoir solution contained 15 to 30% t-butanol in 33 to 100 mM sodium citrate buffer, pH 5.2 to 5.6. The crystals belong to the orthorhombic space group C222, with a = 90.49 Å, b = 99.38 Å, and c = 101.59 Å and contain one molecule in the asymmetric unit. HsMetAP-2-fumagillin complex crystals were prepared by adding 1 μl of 50 mM fumagillin (ethanol) directly into a crystallization drop and equilibrated for 12 hours before mounting.
19. free). The root mean square deviations from ideal bond lengths and bond angles are 0.012 Å and 2.2°.
20. free). The root mean square deviations from ideal bond lengths and bond angles are 0.012 Å and 2.2°.
21. free). The root mean square deviations from ideal bond lengths and bond angles are 0.012 Å and 2.2°.
22. free). The root mean square deviations from ideal bond lengths and bond angles are 0.012 Å and 2.2°.
23. S. L. Roderick and B. W. Matthews, Biochemistry 32, 3907 (1993).
24. T. H. Tahirov et al. J. Struct. Biol. 121, 68 (1998).
25. J. Kraut, Annu. Rev. Biochem. 46, 331 (1977).
26. R. L. Kendall and R. A. Bradshaw, J. Biol. Chem. 267, 20667 (1992).
27. X. Li and Y.-H. Chang, Proc. Natl. Acad. Sci. U.S.A. 92, 12357 (1995).
28. C. J. Barton, Protein Eng. 6, 37 (1993).
29. P. J. Kraulis, J. Appl. Cryst. 24, 946 (1991).
30. A. C. Wallace, R. Laskowski, J. Thornton, Protein Eng. 8, 127 (1995).
31. We thank R. Gillilan for graphics, the MacCHESS staff for help with data collection, J. Liu for helpful discussions, and Y.-H. Chang for the HsMetAP-2 pBluescript plasmid. The Cornell work was funded in part by U.S. Public Health Service grants CA59021 and CA24487 (to J.C.). C.M.C. is a Donaghue Foundation New Investigator. Atomic coordinates have been deposited in the Protein Data Bank under accession numbers 1BN5 (HsMetAP-2) and 1BOA (HsMetAP-2-fumagillin).