Biography
Education and qualifications
1997: PhD, University of Hamburg, Supervisor Christian Betzel
1978: BSc, Chemistry (First Class Honours), University of Hamburg
Appointments
2007-present: Group Leader, Beatson Institute for Cancer Research
2005-2007: Group Leader, French Atomic Commission, CEA/IBS, Grenoble, France
2001-2005: Team Leader, CEA/IBS, Grenoble, France
1999-2001: Research Scientist (tenured) with Richard Wade, CEA/IBS, Grenoble, France
1997-1999: Postdoctoral Fellow with Richard Wade, IBS, Grenoble, France
Committee membership
2006-present: French Society for Therapeutic Chemistry
Recent Publications
Kaan HY, Ulaganathan V, Hackney DD, Kozielski F (2009). An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex. Biochem J., in press.
Tcherniuk S, van Lis R, Kozielski F, Skoufias DA (2009). Mutations in the human kinesin Eg5 confer resistance to monastrol and STLC in tumour derived cell lines. Biochem Pharmacol., in press.
Putey A, Popowycz F, Do QT, Bernard P, Talapatra SK, Kozielski F, Galmarini CM, Joseph B (2009). Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure-activity relationship studies. J Med Chem. 52, 5916-5925.
Koehler CJ, Strozynski M, Kozielski F, Treumann A, Thiede B (2009). Isobaric peptide termini labeling for MS/MS-based quantitative proteomics. J Proteome Res. 8, 4333-41.
Comas H, Buisson D-A, Najman R, Kozielski F, Roussequ B, Lopez R (2009). Synthesis of 5-acyl-3,4-dihydropyrimidine-2-thiones via solvent-free solution phase and solid phase Biginelli procedures. Synlett 11, 1737-40.
Peris L, Wagenbach M, Lafanechère L, Brocard J, Moore AT, Kozielski F, Job D, Wordeman L, Andrieux A (2009). Motor-dependent microtubule disassembly driven by tubulin tyrosination. J Cell Biol. 185, 1159-66.
Popowycz F, Schneider C, Debonis S, Skoufias DA, Kozielski F, Galmarini CM, Joseph B (2009). Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine mtoseverin derivatives. Bioorg Med Chem. 17, 3471-8.
Wade RH, Garcia-Saez I, Kozielski F (2009). Structural variations in protein superfamilies: actin and tubulin. Mol. Biotechnol. 42, 49-60.
Debonis S, Skoufias DA, Indorato RL, Liger F, Marquet B, Laggner C, Joseph B, Kozielski F (2008). Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5. J Med Chem. 51, 1115-25.
Kozielski F, Skoufias DA, Indorato RL, Saoudi Y, Jungblut PR, Hustoft HK, Strozynski M, Thiede B (2008). Proteome analysis of apoptosis signaling by S-trityl-L-cysteine, a potent reversible inhibitor of human mitotic kinesin Eg5. Proteomics 8, 289-300.
Garcia-Saez I, DeBonis S, Lopez R, Fernando Trucco F, Rousseau B, Thuery P, Kozielski F (2007). Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration. J Biol Chem. 282, 9740-7.
Kozielski F, DeBonis S, Skoufias DA (2007). Screening for inhibitors of microtubule-associated motor proteins. Methods in Mol Med. 13, 189-207.
Klein E, DeBonis S, Skoufias DA, Kozielski F, Lebeau L (2007). New chemical tools for investigating human mitotic kinesin Eg5. Bioorg Med Chem. 15, 6474-88.
Brier S, Carletti E, DeBonis S, Hewat E, Lemaire D, Kozielski F (2006). The marine natural product adociasulfate-2 as a tool to identify the MT-binding region of kinesins. Biochem. 45, 15644-53.
Skoufias DA, DeBonis S, Lebeau L, Crevel I, Saoudi Y, Cross R, Wade RH, Hackney D, Kozielski F (2006). S-trityl-L-cysteine is a reversible, tight-binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression. J Biol.Chem. 281, 17559-69.
Brier S, Lemaire D, DeBonis S, Forest E, Kozielski F (2006). Molecular dissection of the inhibitor binding pocket of human mitotic Eg5 reveals mutants that confer resistance to antimitotic agents. J Mol Biol. 360, 360-76.
Neumann E, Garcia-Saez I, DeBonis S, Wade RH, Kozielski F, Conway JF (2006). Human kinetochore-associated kinesin CENP-E visualized at 17 Å resolution bound to microtubules. J Mol Biol. 362, 203-11.
Banci L, Bertini I, Cusack S, de Jong RN, Heinemann U, Jones EY, Kozielski F, Maskos K, Messerschmidt A, Owens R, Perrakis A, Potersman A, Schneider G, Siebold C, Silman I, Sisma T, Stewart-Jones G, Sussman JL, Thierry J-C, Moras D (2006). First steps towards effective methods in exploiting high-throughput technologies for the determination of human protein structures of high biomedical value. Acta Cryst. D 62, 1208-17.
Garcia-Saez I, Tcherniuk S, Kozielski F (2006). The structure of human neuronal Rab6B in the active and inactive form. Acta Cryst. D 62, 725-73.