Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 66

1.

Is the Fate of Clinical Candidate Arry-520 Already Sealed? Predicting Resistance in Eg5-Inhibitor Complexes.

Indorato RL, Talapatra SK, Lin F, Haider S, Mackay SP, Kozielski F, Skoufias DA.

Mol Cancer Ther. 2019 Dec;18(12):2394-2406. doi: 10.1158/1535-7163.MCT-19-0154. Epub 2019 Sep 5.

PMID:
31488701
2.

Development and validation of RdRp Screen, a crystallization screen for viral RNA-dependent RNA polymerases.

Riccio F, Talapatra SK, Oxenford S, Angell R, Mazzon M, Kozielski F.

Biol Open. 2019 Jan 2;8(1). pii: bio037663. doi: 10.1242/bio.037663.

3.

Corrigendum to "Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5 [Bioorg Med Chem Lett 28 (17) (2018) 2930-2938]".

Khathi SP, Chandrasekaran B, Karunanidhi S, Tham CL, Kozielski F, Sayyad N, Karpoormath R.

Bioorg Med Chem Lett. 2018 Nov 15;28(21):3489. doi: 10.1016/j.bmcl.2018.08.029. Epub 2018 Sep 29. No abstract available.

PMID:
30279037
4.

Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5.

Khathi SP, Chandrasekaran B, Karunanidhi S, Tham CL, Kozielski F, Sayyad N, Karpoormath R.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2930-2938. doi: 10.1016/j.bmcl.2018.07.007. Epub 2018 Jul 5. Erratum in: Bioorg Med Chem Lett. 2018 Nov 15;28(21):3489.

PMID:
30055887
5.

Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors.

Talapatra SK, Tham CL, Guglielmi P, Cirilli R, Chandrasekaran B, Karpoormath R, Carradori S, Kozielski F.

Eur J Med Chem. 2018 Aug 5;156:641-651. doi: 10.1016/j.ejmech.2018.07.006. Epub 2018 Jul 4.

PMID:
30031975
6.

Modified Peptide Inhibitors of the Keap1-Nrf2 Protein-Protein Interaction Incorporating Unnatural Amino Acids.

Georgakopoulos ND, Talapatra SK, Gatliff J, Kozielski F, Wells G.

Chembiochem. 2018 Sep 4;19(17):1810-1816. doi: 10.1002/cbic.201800170. Epub 2018 Jul 18.

7.

The structure of the binary methyltransferase-SAH complex from Zika virus reveals a novel conformation for the mechanism of mRNA capping.

Chatrin C, Talapatra SK, Canard B, Kozielski F.

Oncotarget. 2017 Dec 14;9(3):3160-3171. doi: 10.18632/oncotarget.23223. eCollection 2018 Jan 9.

8.

Ligand- and structure-based in silico studies to identify kinesin spindle protein (KSP) inhibitors as potential anticancer agents.

Balakumar C, Ramesh M, Tham CL, Khathi SP, Kozielski F, Srinivasulu C, Hampannavar GA, Sayyad N, Soliman ME, Karpoormath R.

J Biomol Struct Dyn. 2018 Nov;36(14):3687-3704. doi: 10.1080/07391102.2017.1396255. Epub 2017 Nov 29.

PMID:
29064326
9.

Depsidones from Lichens as Natural Product Inhibitors of M-Phase Phosphoprotein 1, a Human Kinesin Required for Cytokinesis.

Talapatra SK, Rath O, Clayton E, Tomasi S, Kozielski F.

J Nat Prod. 2016 Jun 24;79(6):1576-85. doi: 10.1021/acs.jnatprod.5b00962. Epub 2016 Jun 14.

PMID:
27300079
10.

New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations.

Labrière C, Talapatra SK, Thoret S, Bougeret C, Kozielski F, Guillou C.

Bioorg Med Chem. 2016 Feb 15;24(4):721-34. doi: 10.1016/j.bmc.2015.12.042. Epub 2015 Dec 24.

PMID:
26778612
11.

The crystal structure and biochemical characterization of Kif15: a bifunctional molecular motor involved in bipolar spindle formation and neuronal development.

Klejnot M, Falnikar A, Ulaganathan V, Cross RA, Baas PW, Kozielski F.

Acta Crystallogr D Biol Crystallogr. 2014 Jan;70(Pt 1):123-33. doi: 10.1107/S1399004713028721. Epub 2013 Dec 24.

12.

STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity.

Indorato RL, DeBonis S, Kozielski F, Garcia-Saez I, Skoufias DA.

Biochem Pharmacol. 2013 Nov 15;86(10):1441-51. doi: 10.1016/j.bcp.2013.09.003. Epub 2013 Sep 13.

PMID:
24041742
13.

Analysis of the human cofilin 1 structure reveals conformational changes required for actin binding.

Klejnot M, Gabrielsen M, Cameron J, Mleczak A, Talapatra SK, Kozielski F, Pannifer A, Olson MF.

Acta Crystallogr D Biol Crystallogr. 2013 Sep;69(Pt 9):1780-8. doi: 10.1107/S0907444913014418. Epub 2013 Aug 17.

14.

Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.

Talapatra SK, Anthony NG, Mackay SP, Kozielski F.

J Med Chem. 2013 Aug 22;56(16):6317-29. doi: 10.1021/jm4006274.

PMID:
23875972
15.

"Snapshots" of ispinesib-induced conformational changes in the mitotic kinesin Eg5.

Kaan HY, Major J, Tkocz K, Kozielski F, Rosenfeld SS.

J Biol Chem. 2013 Jun 21;288(25):18588-98. doi: 10.1074/jbc.M113.462648. Epub 2013 May 8.

16.

Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.

Good JA, Wang F, Rath O, Kaan HY, Talapatra SK, Podgórski D, MacKay SP, Kozielski F.

J Med Chem. 2013 Mar 14;56(5):1878-93. doi: 10.1021/jm3014597. Epub 2013 Feb 27.

17.

Structural insights into a unique inhibitor binding pocket in kinesin spindle protein.

Ulaganathan V, Talapatra SK, Rath O, Pannifer A, Hackney DD, Kozielski F.

J Am Chem Soc. 2013 Feb 13;135(6):2263-72. doi: 10.1021/ja310377d. Epub 2013 Feb 4.

PMID:
23305346
18.

The structure of the ternary Eg5-ADP-ispinesib complex.

Talapatra SK, Schüttelkopf AW, Kozielski F.

Acta Crystallogr D Biol Crystallogr. 2012 Oct;68(Pt 10):1311-9. Epub 2012 Sep 13.

19.

Kinesins and cancer.

Rath O, Kozielski F.

Nat Rev Cancer. 2012 Jul 24;12(8):527-39. doi: 10.1038/nrc3310. Review.

PMID:
22825217
20.

Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.

Abualhasan MN, Good JA, Wittayanarakul K, Anthony NG, Berretta G, Rath O, Kozielski F, Sutcliffe OB, Mackay SP.

Eur J Med Chem. 2012 Aug;54:483-98. doi: 10.1016/j.ejmech.2012.05.034. Epub 2012 Jun 7.

PMID:
22749640
21.

Receptor-ligand interaction-based virtual screening for novel Eg5/kinesin spindle protein inhibitors.

Nagarajan S, Skoufias DA, Kozielski F, Pae AN.

J Med Chem. 2012 Mar 22;55(6):2561-73. doi: 10.1021/jm201290v. Epub 2012 Mar 1.

PMID:
22309208
22.

Structural insights into human Kif7, a kinesin involved in Hedgehog signalling.

Klejnot M, Kozielski F.

Acta Crystallogr D Biol Crystallogr. 2012 Feb;68(Pt 2):154-9. doi: 10.1107/S0907444911053042. Epub 2012 Jan 13.

23.

Inhibition of hepatitis C virus NS5B polymerase by S-trityl-L-cysteine derivatives.

Nichols DB, Fournet G, Gurukumar KR, Basu A, Lee JC, Sakamoto N, Kozielski F, Musmuca I, Joseph B, Ragno R, Kaushik-Basu N.

Eur J Med Chem. 2012 Mar;49:191-9. doi: 10.1016/j.ejmech.2012.01.010. Epub 2012 Jan 12.

24.

Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.

Wang F, Good JA, Rath O, Kaan HY, Sutcliffe OB, Mackay SP, Kozielski F.

J Med Chem. 2012 Feb 23;55(4):1511-25. doi: 10.1021/jm201195m. Epub 2012 Feb 13.

25.

Elucidating the functionality of kinesins: an overview of small molecule inhibitors.

Good JA, Skoufias DA, Kozielski F.

Semin Cell Dev Biol. 2011 Dec;22(9):935-45. doi: 10.1016/j.semcdb.2011.09.023. Epub 2011 Oct 6. Review.

PMID:
22001111
26.

The structure of the kinesin-1 motor-tail complex reveals the mechanism of autoinhibition.

Kaan HY, Hackney DD, Kozielski F.

Science. 2011 Aug 12;333(6044):883-5. doi: 10.1126/science.1204824.

27.

Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.

Kaan HY, Weiss J, Menger D, Ulaganathan V, Tkocz K, Laggner C, Popowycz F, Joseph B, Kozielski F.

J Med Chem. 2011 Mar 24;54(6):1576-86. doi: 10.1021/jm100991m. Epub 2011 Feb 23.

PMID:
21344920
28.

Kinesin-12, a mitotic microtubule-associated motor protein, impacts axonal growth, navigation, and branching.

Liu M, Nadar VC, Kozielski F, Kozlowska M, Yu W, Baas PW.

J Neurosci. 2010 Nov 3;30(44):14896-906. doi: 10.1523/JNEUROSCI.3739-10.2010.

29.

Relocation of Aurora B and survivin from centromeres to the central spindle impaired by a kinesin-specific MKLP-2 inhibitor.

Tcherniuk S, Skoufias DA, Labriere C, Rath O, Gueritte F, Guillou C, Kozielski F.

Angew Chem Int Ed Engl. 2010 Oct 25;49(44):8228-31. doi: 10.1002/anie.201003254. No abstract available.

PMID:
20857469
30.

Structure-activity relationships and molecular docking of novel dihydropyrimidine-based mitotic Eg5 inhibitors.

Prokopcová H, Dallinger D, Uray G, Kaan HY, Ulaganathan V, Kozielski F, Laggner C, Kappe CO.

ChemMedChem. 2010 Oct 4;5(10):1760-9. doi: 10.1002/cmdc.201000252.

PMID:
20737530
31.

Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol.

Kaan HY, Ulaganathan V, Rath O, Prokopcová H, Dallinger D, Kappe CO, Kozielski F.

J Med Chem. 2010 Aug 12;53(15):5676-83. doi: 10.1021/jm100421n.

PMID:
20597485
32.

Proteome analysis of microtubule-associated proteins and their interacting partners from mammalian brain.

Kozielski F, Riaz T, DeBonis S, Koehler CJ, Kroening M, Panse I, Strozynski M, Donaldson IM, Thiede B.

Amino Acids. 2011 Jul;41(2):363-85. doi: 10.1007/s00726-010-0649-5. Epub 2010 Jun 22.

PMID:
20567863
33.

Docetaxel-resistant prostate cancer cells remain sensitive to S-trityl-L-cysteine-mediated Eg5 inhibition.

Wiltshire C, Singh BL, Stockley J, Fleming J, Doyle B, Barnetson R, Robson CN, Kozielski F, Leung HY.

Mol Cancer Ther. 2010 Jun;9(6):1730-9. doi: 10.1158/1535-7163.MCT-09-1103. Epub 2010 Jun 1.

34.

Mutations in the human kinesin Eg5 that confer resistance to monastrol and S-trityl-L-cysteine in tumor derived cell lines.

Tcherniuk S, van Lis R, Kozielski F, Skoufias DA.

Biochem Pharmacol. 2010 Mar 15;79(6):864-72. doi: 10.1016/j.bcp.2009.11.001. Epub 2009 Nov 6.

PMID:
19896928
35.

An allosteric transition trapped in an intermediate state of a new kinesin-inhibitor complex.

Kaan HY, Ulaganathan V, Hackney DD, Kozielski F.

Biochem J. 2009 Dec 14;425(1):55-60. doi: 10.1042/BJ20091207.

PMID:
19793049
36.

Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.

Putey A, Popowycz F, Do QT, Bernard P, Talapatra SK, Kozielski F, Galmarini CM, Joseph B.

J Med Chem. 2009 Oct 8;52(19):5916-25. doi: 10.1021/jm900476c.

PMID:
19743863
37.

Isobaric peptide termini labeling for MS/MS-based quantitative proteomics.

Koehler CJ, Strozynski M, Kozielski F, Treumann A, Thiede B.

J Proteome Res. 2009 Sep;8(9):4333-41. doi: 10.1021/pr900425n.

PMID:
19655813
38.

Motor-dependent microtubule disassembly driven by tubulin tyrosination.

Peris L, Wagenbach M, Lafanechère L, Brocard J, Moore AT, Kozielski F, Job D, Wordeman L, Andrieux A.

J Cell Biol. 2009 Jun 29;185(7):1159-66. doi: 10.1083/jcb.200902142.

39.

Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives.

Popowycz F, Schneider C, Debonis S, Skoufias DA, Kozielski F, Galmarini CM, Joseph B.

Bioorg Med Chem. 2009 May 1;17(9):3471-8. doi: 10.1016/j.bmc.2009.03.007. Epub 2009 Mar 10.

PMID:
19349183
40.

Structural variations in protein superfamilies: actin and tubulin.

Wade RH, Garcia-Saez I, Kozielski F.

Mol Biotechnol. 2009 May;42(1):49-60. doi: 10.1007/s12033-008-9128-6. Epub 2009 Jan 8.

PMID:
19130318
41.

Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.

Debonis S, Skoufias DA, Indorato RL, Liger F, Marquet B, Laggner C, Joseph B, Kozielski F.

J Med Chem. 2008 Mar 13;51(5):1115-25. doi: 10.1021/jm070606z. Epub 2008 Feb 12.

PMID:
18266314
42.

Proteome analysis of apoptosis signaling by S-trityl-L-cysteine, a potent reversible inhibitor of human mitotic kinesin Eg5.

Kozielski F, Skoufias DA, Indorato RL, Saoudi Y, Jungblut PR, Hustoft HK, Strozynski M, Thiede B.

Proteomics. 2008 Jan;8(2):289-300. doi: 10.1002/pmic.200700534.

PMID:
18186019
43.

Screening for inhibitors of microtubule-associated motor proteins.

Kozielski F, DeBonis S, Skoufias DA.

Methods Mol Med. 2007;137:189-207.

PMID:
18085231
44.

New chemical tools for investigating human mitotic kinesin Eg5.

Klein E, DeBonis S, Thiede B, Skoufias DA, Kozielski F, Lebeau L.

Bioorg Med Chem. 2007 Oct 1;15(19):6474-88. Epub 2007 Jun 10.

PMID:
17587586
45.

Structure of human Eg5 in complex with a new monastrol-based inhibitor bound in the R configuration.

Garcia-Saez I, DeBonis S, Lopez R, Trucco F, Rousseau B, Thuéry P, Kozielski F.

J Biol Chem. 2007 Mar 30;282(13):9740-7. Epub 2007 Jan 23.

46.

The marine natural product adociasulfate-2 as a tool to identify the MT-binding region of kinesins.

Brier S, Carletti E, DeBonis S, Hewat E, Lemaire D, Kozielski F.

Biochemistry. 2006 Dec 26;45(51):15644-53. Epub 2006 Dec 1.

PMID:
17176086
47.

First steps towards effective methods in exploiting high-throughput technologies for the determination of human protein structures of high biomedical value.

Banci L, Bertini I, Cusack S, de Jong RN, Heinemann U, Jones EY, Kozielski F, Maskos K, Messerschmidt A, Owens R, Perrakis A, Poterszman A, Schneider G, Siebold C, Silman I, Sixma T, Stewart-Jones G, Sussman JL, Thierry JC, Moras D.

Acta Crystallogr D Biol Crystallogr. 2006 Oct;62(Pt 10):1208-17. Epub 2006 Sep 19. Review.

PMID:
17001097
48.

Human kinetochore-associated kinesin CENP-E visualized at 17 A resolution bound to microtubules.

Neumann E, Garcia-Saez I, DeBonis S, Wade RH, Kozielski F, Conway JF.

J Mol Biol. 2006 Sep 15;362(2):203-11. Epub 2006 Jul 27.

PMID:
16926026
49.

The structure of human neuronal Rab6B in the active and inactive form.

Garcia-Saez I, Tcherniuk S, Kozielski F.

Acta Crystallogr D Biol Crystallogr. 2006 Jul;62(Pt 7):725-33. Epub 2006 Jun 20.

PMID:
16790928
50.

Molecular dissection of the inhibitor binding pocket of mitotic kinesin Eg5 reveals mutants that confer resistance to antimitotic agents.

Brier S, Lemaire D, DeBonis S, Forest E, Kozielski F.

J Mol Biol. 2006 Jul 7;360(2):360-76. Epub 2006 May 15.

PMID:
16780877

Supplemental Content

Loading ...
Support Center