You are here:Jane Endicott's publications

Jane Endicott's publications
    Shao H., Shi S., Huang S., Hole A., Abbas A.Y., Baumli S., Liu X., Lam F., Foley D.W., Fischer P.M., Noble M., Endicott J.A., Pepper C., Wang S. (2013) Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, x-ray crystal structure, SAR and anti-cancer activities. J. Med. Chem. [Pubmed]
    Hole A., Baumli S., Shao H., Shi S., Pepper C., Fischer P.M., Wang S., Endicott J.A., Noble M. (2012) Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. J. Med. Chem. [Pubmed]
    Baumli S., Hole A.J., Wang L.Z., Noble M.E., Endicott J.A. (2012) The CDK9 tail determines the reaction pathway of positive transcription elongation factor b. Structure 20(10):1788-95. [Pubmed]
    Boehringer J., Riedinger C., Paraskevopoulos K., Johnson E.O., Lowe E.D., Khoudian C., Smith D., Noble M.E., Gordon C., Endicott J.A. (2012) Structural and functional characterization of Rpn12 identifies residues required for Rpn10 proteasome incorporation. Biochem. J. 448(1):55-65. [Pubmed]
    Endicott J.A., Noble M.E., Johnson L.N. (2012) The structural basis for control of eukaryotic protein kinases. Annu. Rev. Biochem. 81:587-613. [Pubmed]
    Baumli S., Hole A.J., Noble M.E., Endicott J.A. (2012) The CDK9 C-helix exhibits conformational plasticity that may explain the selectivity of CAN508. ACS Chem. Biol. 7(5):811-6. [Pubmed]
    Watson A.F., Liu J., Bennaceur K., Drummond C.J., Endicott J.A., Golding B.T., Griffin R.J., Haggerty K., Lu X., McDonnell J.M., Newell D.R., Noble M.E., Revill C.H., Riedinger C., Xu Q., Zhao Y., Lunec J., Hardcastle I.R. (2011) MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. Bioorg. Med. Chem. Lett. 21(19):5916-9. [Pubmed]
    Hardcastle I.R., Liu J., Valeur E., Watson A., Ahmed S.U., Blackburn T.J., Bennaceur K., Clegg W., Drummond C., Endicott J.A., Golding B.T., Griffin R.J., Gruber J., Haggerty K., Harrington R.W., Hutton C., Kemp S., Lu X., McDonnell J.M., Newell D.R., Noble M.E., Payne S.L., Revill C.H., Riedinger C., Xu Q., Lunec J. (2011) Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency. J. Med. Chem. 54(5):1233-43. [Pubmed]
    Riedinger C., Noble M.E., Wright D.J., Mulks F., Hardcastle I.R., Endicott J.A., McDonnell J.M. (2011) Understanding small-molecule binding to MDM2: insights into structural effects of isoindolinone inhibitors from NMR spectroscopy. Chem. Biol. Drug. Des. 77(5):301-8. [Pubmed]
    Trempe J.F., Brown N.R., Noble M.E., Endicott J.A. (2011) A new crystal form of Lys48-linked diubiquitin. Acta Crystallogr. Sect F Struct. Biol. Cryst. Commun. 66(Pt 9):994-8. [Pubmed]
    Baumli S., Endicott J.A., Johnson L.N. (2010) Halogen bonds form the basis for selective P-TEFb inhibition by DRB Chem. Biol. 17(9):931-6. [Pubmed]
    Riedinger C., Boehringer J., Trempe J.F., Lowe E.D., Brown N.R., Gehring K., Noble M.E., Gordon C., Endicott J.A. (2010) Structure of Rpn10 and its interactions with polyubiquitin chains and the proteasome subunit Rpn12. J. Biol. Chem. 285(44):33992-400. [Pubmed]
    Bettayeb K., Baunbæk D., Delehouze C., Loaëc N., Hole A.J., Baumli S., Endicott J.A., Douc-Rasy S., Bénard J., Oumata N., Galons H., Meijer L. (2010) CDK Inhibitors Roscovitine and CR8 Trigger Mcl-1 Down-Regulation and Apoptotic Cell Death in Neuroblastoma Cells. Genes Cancer. (4):369-80. [Pubmed]
    Echalier A., Endicott J.A., Noble M.E. (2010) Recent developments in cyclin-dependent kinase biochemical and structural studies. Biochim. Biophys. Acta. 1804(3):511-9. [Pubmed]
    Takaki T., Echalier A., Brown N.R., Hunt T., Endicott J.A., Noble M.E. (2009) The structure of CDK4/cyclin D3 has implications for models of CDK activation. Proc. Natl. Acad. Sci. U. S. A. 106(11):4171-6. [Pubmed]
    Riedinger C., Endicott J.A. (2009) All change: protein conformation and the ubiquitination reaction cascade. F1000 Biol. Rep. 1:19. [Pubmed]
    Riedinger C., Endicott J.A., Kemp S.J., Smyth L.A., Watson A., Valeur E., Golding B.T., Griffin R.J., Hardcastle I.R., Noble M.E., McDonnell J.M. (2008) Analysis of chemical shift changes reveals the binding modes of isoindolinone inhibitors of the MDM2-p53 interaction. J. Am. Chem. Soc. 130(47):16038-44. [Pubmed]
    Bettayeb K., Oumata N., Echalier A., Ferandin Y., Endicott J.A., Galons H., Meijer L. (2008) CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 27(44):5797-807. [Pubmed]
    Echalier A., Bettayeb K., Ferandin Y., Lozach O., Clément M., Valette A., Liger F., Marquet B., Morris J.C., Endicott J.A., Joseph B., Meijer L. (2008) Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex. J. Med. Chem. 51(4):737-51. [Pubmed]
    Alier K.A., Endicott J.A., Stemkowski P.L., Cenac N., Cellars L., Chapman K., Andrade-Gordon P., Vergnolle N., Smith P.A. (2008) Intrathecal administration of proteinase-activated receptor-2 agonists produces hyperalgesia by exciting the cell bodies of primary sensory neurons. J. Pharmacol. Exp. Ther. 324(1):224-33. [Pubmed]
    Bettayeb K., Tirado O.M., Marionneau-Lambot S., Ferandin Y., Lozach O., Morris J.C., Mateo-Lozano S., Drueckes P., Schächtele C., Kubbutat M.H., Liger F., Marquet B., Joseph B., Echalier A., Endicott J.A., Notario V., Meijer L. (2007) Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases. Cancer Res. 67(17):8325-34. [Pubmed]
    Marchetti F., Sayle K.L., Bentley J., Clegg W., Curtin N.J., Endicott J.A., Golding B.T., Griffin R.J., Haggerty K., Harrington R.W., Mesguiche V., Newell D.R., Noble M.E., Parsons R.J., Pratt D.J., Wang L.Z., Hardcastle I.R. (2007) Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2. Org. Biomol. Chem. 5(10):1577-85. [Pubmed]
    Trempe J.F., Endicott J.A. (2007) Structural biology: pass the protein. Nature 445(7126):375-6. [Pubmed]
    Welburn J.P., Tucker J.A., Johnson T., Lindert L., Morgan M., Willis A., Noble M.E., Endicott J.A. (2007) How tyrosine 15 phosphorylation inhibits the activity of cyclin-dependent kinase 2-cyclin A. J. Biol. Chem. 282(5):3173-81. [Pubmed]
    Pratt D.J., Bentley J., Jewsbury P., Boyle F.T., Endicott J.A., Noble M.E. (2006) Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. J. Med. Chem. 49(18):5470-7. [Pubmed]
    Griffin R.J., Henderson A., Curtin N.J., Echalier A., Endicott J.A., Hardcastle I.R., Newell D.R., Noble M.E., Wang L.Z., Golding B.T. (2006) Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination. J. Am. Chem. Soc. 128(18):6012-3. [Pubmed]
    Lowe E.D., Hasan N., Trempe J.F., Fonso L., Noble M.E., Endicott J.A., Johnson L.N., Brown N.R. (2006) Structures of the Dsk2 UBL and UBA domains and their complex. Acta Crystallogr. D Biol. Crystallogr. 62(Pt 2):177-88. [Pubmed]
    Macdonald N., Welburn J.P., Noble M.E., Nguyen A., Yaffe M.B., Clynes D., Moggs J.G., Orphanides G., Thomson S., Edmunds J.W., Clayton A.L., Endicott J.A., Mahadevan L.C. (2005) Molecular basis for the recognition of phosphorylated and phosphoacetylated histone h3 by 14-3-3. Mol. Cell. 20(2):199-211. [Pubmed]
    Sasaki T., Funakoshi M., Endicott J.A., Kobayashi H. (2005) Budding yeast Dsk2 protein forms a homodimer via its C-terminal UBA domain. Biochem. Biophys. Res. Commun. 336(2):530-5. [Pubmed]
    Trempe J.F., Brown N.R., Lowe E.D., Gordon C., Campbell I.D., Noble M.E., Endicott J.A. (2005) Mechanism of Lys48-linked polyubiquitin chain recognition by the Mud1 UBA domain. EMBO J. 2005 24(18):3178-89. [Pubmed]
    Welburn J.P., Endicott J.A. (2005) Inhibition of the cell cycle with chemical inhibitors: a targeted approach. Semin. Cell. Dev. Biol. 16(3):369-81. [Pubmed]
    Pratt D.J., Endicott J.A., Noble M.E. (2004) The role of structure in kinase-targeted inhibitor design. Curr. Opin. Drug Discov. Devel. 7(4):428-36. [Pubmed]
    Hardcastle I.R., Arris C.E., Bentley J., Boyle F.T., Chen Y., Curtin N.J., Endicott J.A., Gibson A.E., Golding B.T., Griffin R.J., Jewsbury P., Menyerol J., Mesguiche V., Newell D.R., Noble M.E., Pratt D.J., Wang L.Z., Whitfield H.J. (2004) N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2. J. Med. Chem. 47(15):3710-22. [Pubmed]
    Noble M.E., Endicott J.A., Johnson L.N. (2004) Protein kinase inhibitors: insights into drug design from structure. Science. 303(5665):1800-5. [Pubmed]
    Sayle K.L., Bentley J., Boyle F.T., Calvert A.H., Cheng Y., Curtin N.J., Endicott J.A., Golding B.T., Hardcastle I.R., Jewsbury P., Mesguiche V., Newell D.R., Noble M.E., Parsons R.J., Pratt D.J., Wang L.Z., Griffin R.J. (2003) Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. Bioorg. Med. Chem. Lett. 13(18):3079-82. [Pubmed]
    Mesguiche V., Parsons R.J., Arris C.E., Bentley J., Boyle F.T., Curtin N.J., Davies T.G., Endicott J.A., Gibson A.E., Golding B.T., Griffin R.J., Jewsbury P., Johnson L.N., Newell D.R., Noble M.E., Wang L.Z., Hardcastle I.R. (2003) 4-Alkoxy-2,6-diaminopyrimidine derivatives: inhibitors of cyclin dependent kinases 1 and 2. Bioorg. Med. Chem. Lett. 13(2):217-22. [Pubmed]
    Davies T.G., Bentley J., Arris C.E., Boyle F.T., Curtin N.J., Endicott J.A., Gibson A.E., Golding B.T., Griffin R.J., Hardcastle I.R., Jewsbury P., Johnson L.N., Mesguiche V., Newell D.R., Noble M.E., Tucker J.A., Wang L., Whitfield H.J. (2002) Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor. Nat. Struct. Biol. 9(10):745-9. [Pubmed]
    Davies T.G., Pratt D.J., Endicott J.A., Johnson L.N., Noble M.E. (2002) Structure-based design of cyclin-dependent kinase inhibitors. Pharmacol. Ther. 93(2-3):125-33. [Pubmed]
    Johnson L.N., De Moliner E., Brown N.R., Song H., Barford D., Endicott J.A., Noble M.E. (2002) Structural studies with inhibitors of the cell cycle regulatory kinase cyclin-dependent protein kinase 2. Pharmacol. Ther. 93(2-3):113-24. [Pubmed]
    Gibson A.E., Arris C.E., Bentley J., Boyle F.T., Curtin N.J., Davies T.G., Endicott J.A., Golding B.T., Grant S., Griffin R.J., Jewsbury P., Johnson L.N., Mesguiche V., Newell D.R., Noble M.E., Tucker J.A., Whitfield H.J. (2002) Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives. J. Med. Chem. 45(16):3381-93. [Pubmed]
    Lawrie A.M., Tito P., Hernandez H., Brown N.R., Robinson C.V., Endicott J.A., Noble M.E., Johnson L.N. (2001) Xenopus phospho-CDK7/cyclin H expressed in baculoviral-infected insect cells. Protein Expr. Purif. 23(2):252-60. [Pubmed]
    Davies T.G., Tunnah P., Meijer L., Marko D., Eisenbrand G., Endicott J.A., Noble M.E. (2001) Inhibitor binding to active and inactive CDK2: the crystal structure of CDK2-cyclin A/indirubin-5-sulphonate. Structure 9(5):389-97. [Pubmed]
    Arris C.E., Boyle F.T., Calvert A.H., Curtin N.J., Endicott J.A., Garman E.F., Gibson A.E., Golding B.T., Grant S., Griffin R.J., Jewsbury P., Johnson L.N., Lawrie A.M., Newell D.R., Noble M.E., Sausville E.A., Schultz R., Yu W. (2000) Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J. Med. Chem. 43(15):2797-804. [Pubmed]
    Endicott J.A., Noble M.E., Tucker J.A. (1999) Cyclin-dependent kinases: inhibition and substrate recognition. Curr. Opin. Struct. Biol. 9(6):738-44. [Pubmed]
    Brown N.R., Noble M.E., Endicott J.A., Johnson L.N. (1999) The structural basis for specificity of substrate and recruitment peptides for cyclin-dependent kinases. Nat. Cell. Biol. 1(7):438-43. [Pubmed]
    Hoessel R., Leclerc S., Endicott J.A., Nobel M.E., Lawrie A., Tunnah P., Leost M., Damiens E., Marie D., Marko D., Niederberger E., Tang W., Eisenbrand G., Meijer L. (1999) Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases. Nat. Cell. Biol. 1(1):60-7. [Pubmed]
    Noble M.E., Endicott J.A. (1999) Chemical inhibitors of cyclin-dependent kinases: insights into design from X-ray crystallographic studies. Pharmacol. Ther. 82(2-3):269-78. [Pubmed]
    Owen D.J., Vallis Y., Noble M.E., Hunter J.B., Dafforn T.R., Evans P.R., McMahon H.T. (1999) A structural explanation for the binding of multiple ligands by the alpha-adaptin appendage domain. Cell 97(6):805-15. [Pubmed]
    Brown N.R., Noble M.E., Lawrie A.M., Morris M.C., Tunnah P., Divita G., Johnson L.N., Endicott J.A. (1999) Effects of phosphorylation of threonine 160 on cyclin-dependent kinase 2 structure and activity. J. Biol. Chem. 274(13):8746-56. [Pubmed]
    Endicott J.A., Noble M.E. (1998) Structural principles in cell-cycle control: beyond the CDKs. Structure 6(5):535-41. [Pubmed]
    Noble M.E., Endicott J.A., Brown N.R., Johnson L.N. (1997) The cyclin box fold: protein recognition in cell-cycle and transcription control.Trends Biochem. Sci. 22(12):482-7. [Pubmed]
    Lawrie A.M., Noble M.E., Tunnah P., Brown N.R., Johnson L.N., Endicott J.A. (1997) Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2. Nat. Struct. Biol. 4(10):796-801. [Pubmed]
    Brown N.R., Noble M.E., Endicott J.A., Garman E.F., Wakatsuki S., Mitchell E., Rasmussen B., Hunt T., Johnson L.N. (1995) The crystal structure of cyclin A. Structure 3(11):1235-47. [Pubmed]
    Bourne Y., Arvai A.S., Bernstein S.L., Watson M.H., Reed S.I., Endicott J.E., Noble M.E., Johnson L.N., Tainer J.A. (1995) Crystal structure of the cell cycle-regulatory protein suc1 reveals a beta-hinge conformational switch. Proc. Natl. Acad. Sci. U. S. A. 92(22):10232-6. [Pubmed]
    Endicott J.A., Noble M.E., Garman E.F., Brown N., Rasmussen B., Nurse P., Johnson L.N. (1995) The crystal structure of p13suc1, a p34cdc2-interacting cell cycle control protein. EMBO J. 14(5):1004-14. [Pubmed]
    Endicott J.A., Nurse P. (1995) The cell cycle and suc1: from structure to function? Structure 3(4):321-5.[Pubmed]
    Endicott J.A., Nurse P., Johnson L.N. (1994) Mutational analysis supports a structural model for the cell cycle protein kinase p34. Protein Eng. 7(2):243-53. [Pubmed]
    Endicott J.A., Sarangi F., Ling V. (1991) Complete cDNA sequences encoding the Chinese hamster P-glycoprotein gene family. DNA Seq. 2(2):89-101. [Pubmed]
    Endicott J.A., Ling V. (1989) The biochemistry of P-glycoprotein-mediated multidrug resistance. Annu. Rev. Biochem. 58:137-71. [Pubmed]
    Endicott J.A., Juranka P.F., Sarangi F., Gerlach J.H., Deuchars K.L., Ling V. (1987) Simultaneous expression of two P-glycoprotein genes in drug-sensitive Chinese hamster ovary cells. Mol. Cell. Biol. 7(11):4075-81. [Pubmed]
    Gerlach J.H., Endicott J.A., Juranka P.F., Henderson G., Sarangi F., Deuchars K.L., Ling V. (1986) Homology between P-glycoprotein and a bacterial haemolysin transport protein suggests a model for multidrug resistance. Nature. 324(6096):485-9. [Pubmed]
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February 2014
JBC Best paper of the year 2013 awarded to Pr. Rick Lewis
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2014 is the year of Crystallography
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