Sept. 10, 2009 INBRE Steering Committee. Development and Screening of Transition Metal Complexes as CXCR4 Antagonists. Dr. Tim Hubin Department of Chemistry and Physics. Important role in embryonic development: Organogenesis (liver , heart) Stem cell movement
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Dr. Tim Hubin
Department of Chemistry and Physics
Organogenesis (liver, heart)
Stem cell movement
Cerebellar neuron migration (formation of brain)
Seven transmembrane G-protein-coupled receptor
27% of amino acids are Asp, His or Tyr.
Expressed on :
Neuronal cellsCXCR4 chemokine receptor
Khan, A.; Greenman, J.; Archibald, S. J. Curr. Med. Chem. 2007, 14, 2257.
Mol. Pharm., 1999, 55, 67.
J. Med. Chem., 1995, 38, 366.
Biochemistry, 2003, 42, 715.
Bosnich, B.; Poon, C. K.; Tobe, M. L. Inorg. Chem.,1965, 4,1102
Only cis V
Reagents: (a) acetonitrile, RT, 24 h (89%); (b) NaBH4, EtOH reflux, 1 h (65%).
Lewis, E. A.; Hubin, T. J.; Archibald, S. J. European Patent 1765826A2 .
Cross bridged (CB)
Cu-O1 2.28(1) Å
Cu-O1 1.95(1) Å
+ Control 717.019
FL1-HBinding by flow cytometry
Receptor specific antibody
Summary of mAb 12G5 binding to CXCR4 in the presence of bound antagonists.
G. McRobbie, A. Khan, G. Nicholson, L. Madden, J. Greenman C. Pannecouque, E. De Clercq, T. J. Hubin and S. J. Archibald, J. Am. Chem. Soc, 2009, 3416.
ANTI-CANCER ACTIVITY bound antagonists.Invasion assays
CXCL12 bound antagonists.
Drug + CXCL12
Current research group bound antagonists.:
Courtney Garcia (Pre-Med)
Josh Priddle (Pre-Med)
Desiray Cannon (Pre-Med)
Brooke Shockey (Pre-Med)
Katherine Coats (Chemistry)
Robert Ullom—University of Kansas (Medicine)
TauLyn Snell—Wichita State University (PA)
Joe Blas—Creighton (Medicine)
Danny Maples—OSU (Chemistry)
Randall Maples—OSU (Chemistry)
Dallas Matz—Arizona State University (Chemistry)
Mike McClain—OU (Chemistry)
Amy Cain—U. British Columbia (Chemistry)
Neil Funwie—OU (Petroleum Engineering)
Orry Birdsong—UT Galveston (Medicine)
Kimberly Roewe—OSU (Chemistry)
Kiet Ngyuen—SWOSU (Pharmacy)Acknowledgements