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Items: 25

1.

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.

Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Faram R, Cribbs AP, Halidi N, Li F, Chau I, Greschik H, Velupillai S, Allali-Hassani A, Bennett J, Christott T, Giroud C, Lewis AM, Huber KVM, Athanasou N, Bountra C, Jung M, Schüle R, Vedadi M, Arrowsmith C, Xiong Y, Jin J, Fedorov O, Farnie G, Brennan PE, Oppermann U.

J Med Chem. 2019 Oct 15. doi: 10.1021/acs.jmedchem.9b00562. [Epub ahead of print]

PMID:
31550156
2.

Insights into the full-length SRPK2 structure and its hydrodynamic behavior.

Barbosa ÉAA, Seraphim TV, Gandin CA, Teixeira LF, da Silva RAG, Righetto GL, Goncalves KA, Vasconcellos RS, Almeida MR, Silva Júnior A, Fietto JLR, Kobarg J, Gileadi C, Massirer KB, Borges JC, de Oliveira Neto M, Bressan GC.

Int J Biol Macromol. 2019 Sep 15;137:205-214. doi: 10.1016/j.ijbiomac.2019.06.135. Epub 2019 Jun 20.

PMID:
31229549
3.

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.

Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB.

Cell Rep. 2019 Jan 2;26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023.

4.

Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9.

Christott T, Bennett J, Coxon C, Monteiro O, Giroud C, Beke V, Felce SL, Gamble V, Gileadi C, Poda G, Al-Awar R, Farnie G, Fedorov O.

SLAS Discov. 2019 Feb;24(2):133-141. doi: 10.1177/2472555218809904. Epub 2018 Oct 25.

PMID:
30359161
5.

Discovery of an MLLT1/3 YEATS Domain Chemical Probe.

Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Díaz-Sáez L, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, Chaikuad A, Knapp S, Huber KVM, Farnie G, Heer J, Manevski N, Poda G, Al-Awar R, Dixon DJ, Brennan PE, Fedorov O.

Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. doi: 10.1002/anie.201810617. Epub 2018 Nov 16.

6.

Structural analysis of human KDM5B guides histone demethylase inhibitor development.

Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, Badock V, Munro S, LaThangue NB, Westaway S, Brown J, Athanasou N, Prinjha R, Brennan PE, Oppermann U.

Nat Chem Biol. 2016 Jul;12(7):539-45. doi: 10.1038/nchembio.2087. Epub 2016 May 23.

PMID:
27214403
7.

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.

Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J.

J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7.

8.

Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.

Korczynska M, Le DD, Younger N, Gregori-Puigjané E, Tumber A, Krojer T, Velupillai S, Gileadi C, Nowak RP, Iwasa E, Pollock SB, Ortiz Torres I, Oppermann U, Shoichet BK, Fujimori DG.

J Med Chem. 2016 Feb 25;59(4):1580-98. doi: 10.1021/acs.jmedchem.5b01527. Epub 2015 Dec 23.

9.

Human UTY(KDM6C) is a male-specific Nϵ-methyl lysyl demethylase.

Walport LJ, Hopkinson RJ, Vollmar M, Madden SK, Gileadi C, Oppermann U, Schofield CJ, Johansson C.

J Biol Chem. 2014 Jun 27;289(26):18302-13. doi: 10.1074/jbc.M114.555052. Epub 2014 May 5.

10.

The roles of Jumonji-type oxygenases in human disease.

Johansson C, Tumber A, Che K, Cain P, Nowak R, Gileadi C, Oppermann U.

Epigenomics. 2014 Feb;6(1):89-120. doi: 10.2217/epi.13.79. Review.

11.

Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.

Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A.

J Med Chem. 2012 Jul 26;55(14):6639-43. doi: 10.1021/jm300677j. Epub 2012 Jul 11.

12.

Structural and evolutionary basis for the dual substrate selectivity of human KDM4 histone demethylase family.

Hillringhaus L, Yue WW, Rose NR, Ng SS, Gileadi C, Loenarz C, Bello SH, Bray JE, Schofield CJ, Oppermann U.

J Biol Chem. 2011 Dec 2;286(48):41616-25. doi: 10.1074/jbc.M111.283689. Epub 2011 Sep 13.

13.

Structures of the human GTPase MMAA and vitamin B12-dependent methylmalonyl-CoA mutase and insight into their complex formation.

Froese DS, Kochan G, Muniz JR, Wu X, Gileadi C, Ugochukwu E, Krysztofinska E, Gravel RA, Oppermann U, Yue WW.

J Biol Chem. 2010 Dec 3;285(49):38204-13. doi: 10.1074/jbc.M110.177717. Epub 2010 Sep 28.

14.

Unusual binding interactions in PDZ domain crystal structures help explain binding mechanisms.

Elkins JM, Gileadi C, Shrestha L, Phillips C, Wang J, Muniz JR, Doyle DA.

Protein Sci. 2010 Apr;19(4):731-41. doi: 10.1002/pro.349.

15.

Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits.

Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundström M, Doyle DA, Siderovski DP.

Proc Natl Acad Sci U S A. 2008 Apr 29;105(17):6457-62. doi: 10.1073/pnas.0801508105. Epub 2008 Apr 23.

16.

Structure of PICK1 and other PDZ domains obtained with the help of self-binding C-terminal extensions.

Elkins JM, Papagrigoriou E, Berridge G, Yang X, Phillips C, Gileadi C, Savitsky P, Doyle DA.

Protein Sci. 2007 Apr;16(4):683-94.

17.

Drosophila melanogaster sex peptide stimulates juvenile hormone synthesis and depresses sex pheromone production in Helicoverpa armigera.

Fan Y, Rafaeli A, Gileadi C, Kubli E, Applebaum SW.

J Insect Physiol. 1999 Feb;45(2):127-133.

PMID:
12770380
18.

Activation of octopaminergic receptors by essential oil constituents isolated from aromatic plants: possible mode of action against insect pests.

Kostyukovsky M, Rafaeli A, Gileadi C, Demchenko N, Shaaya E.

Pest Manag Sci. 2002 Nov;58(11):1101-6.

PMID:
12449528
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23.

Modulation of apoptosis in human myeloid leukemic cells by GM-CSF.

Han JH, Gileadi C, Rajapaksa R, Kosek J, Greenberg PL.

Exp Hematol. 1995 Mar;23(3):265-72.

PMID:
7875243
25.

Specific lipid requirements in reconstitution of the delipidated beta-adrenergic receptor with the delipidated regulatory protein.

Schramm M, Kirilovsky J, Eimerl S, Gileadi C.

Adv Second Messenger Phosphoprotein Res. 1988;21:19-24. No abstract available.

PMID:
2843212

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