Discovery of a new molecular probe ML228: An activator of the hypoxia inducible factor (HIF) pathway

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 76-81

  Theriault, Jimmy R ^a   Felts, Andrew S ^b   Bates, Brittney S ^b   Perez, Jose R ^a   Palmer, Michelle ^a   Gilbert, Shawn R ^c   Dawson, Eric S ^b   Engers, Julie L ^b   Lindsley, Craig W ^b   Emmitte, Kyle A ^b  

^a BROAD INSTITUTE OF MIT AND HARVARD   (United States)

^b VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^c University of Alabama at Birmingham   (United States)

Author keywords

Angiogenesis; HIF; Hypoxia; Ischemia; Triazine; VEGF

Indexed keywords

HYPOXIA INDUCIBLE FACTOR; OXYGENASE INHIBITOR; TRIAZINE DERIVATIVE;

ARTICLE; CELL HYPOXIA; CONTROLLED STUDY; GENE ACTIVATION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; MOLECULAR PROBE; MOLECULAR PROBE ML228; REAL TIME POLYMERASE CHAIN REACTION; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANOXIA; CHEMISTRY, PHARMACEUTICAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; HUMANS; HYPOXIA-INDUCIBLE FACTOR 1; MODELS, CHEMICAL; MOLECULAR CONFORMATION; MOLECULAR PROBES; NEOVASCULARIZATION, PATHOLOGIC; PROTEIN STRUCTURE, TERTIARY; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZINES; VASCULAR ENDOTHELIAL GROWTH FACTOR A;

EID: 84655167719     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.077     Document Type: Article

References (33)

1. G.L. Semenza Curr. Opin. Cell. Biol. 13 2001 167
2. L.E. Huang, Z. Arany, D.M. Livingston, and H.F. Bunn J. Biol. Chem. 271 1996 32253
3. L.E. Huang, J. Gu, M. Schau, and H.F. Bunn Proc. Natl. Acad. Sci. U.S.A. 95 1998 7987
4. P.J. Kallio, W.J. Wilson, S. O'Brien, Y. Makino, and L. Poellinger J. Biol. Chem. 274 1999 6519
5. C.H. Sutter, E. Laughner, and G.L. Semenza Proc. Natl. Acad. Sci. U.S.A. 97 2000 4748
6. M. Ivan, K. Kondo, H. Yang, W. Kim, J. Valiando, M. Ohh, A. Salic, J.M. Asara, W.S. Lane, and W.G. Kaelin Jr. Science 292 2001 464
7. P. Jaakkola, D.R. Mole, Y.M. Tian, M.I. Wilson, J. Gielbert, S.J. Gaskell, A. Kriegsheim, H.F. Hebestreit, M. Mukherji, C.J. Schofield, P.H. Maxwell, C.W. Pugh, and P.J. Ratcliffe Science 292 2001 468
8. E. Berra, E. Benizri, A. Ginouves, V. Volmat, D. Roux, and J. Pouyssegur EMBO J. 22 2003 4082
9. J.H. Marxsen, P. Stengel, K. Doege, P. Heikkinen, T. Jokilehto, T. Wagner, W. Jelkmann, P. Jaakkola, and E. Metzen Biochem. J. 381 2004 761
10. E. Metzen, D.P. Stiehl, K. Doege, J.H. Marxsen, T. Hellwig-Burgel, and W. Jelkmann Biochem. J. 387 2005 711
11. P.J. Kallio, K. Okamoto, S. O'Brien, P. Carrero, Y. Makino, H. Tanaka, and L. Poellinger EMBO J. 17 1998 6573
12. A. Giaccia, B.G. Siim, and R.S. Johnson Nat. Rev. Drug Disc. 2 2003 803
13. K.S. Hewitson, L.A. McNeill, and C.J. Schofield Curr. Pharm. Des. 10 2004 821
14. E.J. Yeo, Y.S. Chun, and J.W. Park Biochem. Pharmacol. 68 2004 1061
15. V.S. Chekanov, V. Nikolaychik, M.A. Maternowski, R. Mehran, M.B. Leon, M. Adamian, J. Moses, G. Dangas, N. Kipshidze, and M. Akhtar Ann. Thorac. Surg. 75 2003 184
16. M. Hirsila, P. Koivunen, L. Xu, T. Seeley, K.I. Kivirikko, and J. Myllyharju FASEB J. 19 2005 1308
17. L. Xi, M. Taher, C. Yin, F. Salloum, and R.C. Kukreja Am. J. Physiol. Heart Circ. Physiol. 287 2004 H2369
18. Y. Yuan, G. Hilliard, T. Ferguson, and D.E. Millhorn J. Biol. Chem. 278 2003 15911
19. Y. Bentur, M. McGuigan, and G. Koren Drug Saf. 6 1991 37
20. M.H. Rabinowitz, T.D. Barrett, M.D. Rosen, and H. Venkatesan Ann. Rep. Med. Chem. 45 2010 123
21. Allen, J. R.; Burli, R.; Bryan, M. C.; Cao, G.-Q.; Neira, S. C.; Reed, A. B. PCT Int. Patent Appl. WO2008/130600, 2008.
22. Guiadeen, D.; Hale, J. J.; Kothandaraman, S. PCT Int. Patent Appl. WO2008/130527, 2008.
23. M.D. Rosen, H. Venkatesan, H.M. Peltier, S.D. Bembenek, K.C. Kanelakis, L.X. Zhao, B.E. Leonard, F.M. Hocutt, X. Wu, H.L. Palomino, T.I. Brondstetter, P.V. Haugh, L. Cagnon, W. Yan, L.A. Liotta, A. Young, T. Mirzadegan, N.P. Shankley, T.D. Barrett, and M.H. Rabinowitz ACS Med. Chem. Lett. 1 2010 526
24. N.C. Warshakoon, S. Wu, A. Boyer, R. Kawamoto, J. Sheville, S. Renock, K. Xu, M. Pokross, S. Zhou, C. Winter, R. Walter, M. Mekel, and A.G. Evdokimov Bioorg. Med. Chem. Lett. 16 2006 5517
25. Clements, M. J.; Debenham, J. S.; Hale, J. J.; Madsen-Duggan, C. B.; Walsh, T. F. PCT Int. Patent Appl. WO2009/117269, 2009.
26. N.M. Chau, P. Rogers, W. Aherne, V. Carroll, I. Collins, E. McDonald, P. Workman, and M. Ashcroft Cancer Res. 65 2005 4918
27. Y. Wang, C. Wan, L. Deng, X. Liu, X. Cao, S.R. Gilbert, M.L. Bouxsein, M.C. Faugere, R.E. Guldberg, L.C. Gerstenfeld, V.H. Haase, R.S. Johnson, E. Schipani, and T.L. Clemens J. Clin. Invest. 117 2007 1616
28. C. Wan, S.R. Gilbert, Y. Wang, X. Cao, X. Shen, G. Ramaswamy, K.A. Jacobsen, Z.S. Alaql, A.W. Eberhardt, L.C. Gerstenfeld, T.A. Einhorn, L. Deng, and T.L. Clemens Proc. Natl. Acad. Sci. U.S.A. 105 2008 686
29. Proteasome-Glo™ Chymotrypsin, www.promega.com.
30. J.L. Johansen, T.N. Sager, J. Lotharius, L. Witten, A. Mork, J. Egebjerg, and K. Thirstrup J. Neurochem. 115 2010 209
31. LeadProfilerScreen®, www.ricerca.com.
32. CellTiter-Glo®, www.promega.com.
33. A.N. Jain J. Med. Chem. 47 2004 947