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Items: 21

1.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V.

Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17.

2.

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.

Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr HM, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N.

J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.

3.

Assessing histone demethylase inhibitors in cells: lessons learned.

Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S.

Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017.

4.

Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells.

Tumber A, Nuzzi A, Hookway ES, Hatch SB, Velupillai S, Johansson C, Kawamura A, Savitsky P, Yapp C, Szykowska A, Wu N, Bountra C, Strain-Damerell C, Burgess-Brown NA, Ruda GF, Fedorov O, Munro S, England KS, Nowak RP, Schofield CJ, La Thangue NB, Pawlyn C, Davies F, Morgan G, Athanasou N, Müller S, Oppermann U, Brennan PE.

Cell Chem Biol. 2017 Mar 16;24(3):371-380. doi: 10.1016/j.chembiol.2017.02.006. Epub 2017 Mar 2.

5.

Design, Synthesis, Structure-Activity Relationship Studies, and Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Modeling of a Series of O-Biphenyl Carbamates as Dual Modulators of Dopamine D3 Receptor and Fatty Acid Amide Hydrolase.

De Simone A, Russo D, Ruda GF, Micoli A, Ferraro M, Di Martino RM, Ottonello G, Summa M, Armirotti A, Bandiera T, Cavalli A, Bottegoni G.

J Med Chem. 2017 Mar 23;60(6):2287-2304. doi: 10.1021/acs.jmedchem.6b01578. Epub 2017 Mar 2.

PMID:
28182408
6.

Kernel-Based, Partial Least Squares Quantitative Structure-Retention Relationship Model for UPLC Retention Time Prediction: A Useful Tool for Metabolite Identification.

Falchi F, Bertozzi SM, Ottonello G, Ruda GF, Colombano G, Fiorelli C, Martucci C, Bertorelli R, Scarpelli R, Cavalli A, Bandiera T, Armirotti A.

Anal Chem. 2016 Oct 4;88(19):9510-9517. Epub 2016 Sep 14.

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.

K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac.

Dong YY, Pike AC, Mackenzie A, McClenaghan C, Aryal P, Dong L, Quigley A, Grieben M, Goubin S, Mukhopadhyay S, Ruda GF, Clausen MV, Cao L, Brennan PE, Burgess-Brown NA, Sansom MS, Tucker SJ, Carpenter EP.

Science. 2015 Mar 13;347(6227):1256-9. doi: 10.1126/science.1261512.

9.

N-myristoyltransferase is a cell wall target in Aspergillus fumigatus.

Fang W, Robinson DA, Raimi OG, Blair DE, Harrison JR, Lockhart DE, Torrie LS, Ruda GF, Wyatt PG, Gilbert IH, van Aalten DM.

ACS Chem Biol. 2015 Jun 19;10(6):1425-34. doi: 10.1021/cb5008647. Epub 2015 Feb 27.

10.

Development of 3-alkyl-6-methoxy-7-hydroxy-chromones (AMHCs) from natural isoflavones, a new class of fluorescent scaffolds for biological imaging.

Miao J, Cui H, Jin J, Lai F, Wen H, Zhang X, Ruda GF, Chen X, Yin D.

Chem Commun (Camb). 2015 Jan 18;51(5):881-4. doi: 10.1039/c4cc06762b. Epub 2014 Nov 27.

PMID:
25429667
11.

Applying a multitarget rational drug design strategy: the first set of modulators with potent and balanced activity toward dopamine D3 receptor and fatty acid amide hydrolase.

De Simone A, Ruda GF, Albani C, Tarozzo G, Bandiera T, Piomelli D, Cavalli A, Bottegoni G.

Chem Commun (Camb). 2014 May 18;50(38):4904-7. doi: 10.1039/c4cc00967c.

12.

Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.

Moreno-Sanz G, Duranti A, Melzig L, Fiorelli C, Ruda GF, Colombano G, Mestichelli P, Sanchini S, Tontini A, Mor M, Bandiera T, Scarpelli R, Tarzia G, Piomelli D.

J Med Chem. 2013 Jul 25;56(14):5917-30. doi: 10.1021/jm4007017. Epub 2013 Jul 3.

13.

Automated design of ligands to polypharmacological profiles.

Besnard J, Ruda GF, Setola V, Abecassis K, Rodriguiz RM, Huang XP, Norval S, Sassano MF, Shin AI, Webster LA, Simeons FR, Stojanovski L, Prat A, Seidah NG, Constam DB, Bickerton GR, Read KD, Wetsel WC, Gilbert IH, Roth BL, Hopkins AL.

Nature. 2012 Dec 13;492(7428):215-20. doi: 10.1038/nature11691.

14.

Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase.

Recio E, Musso-Buendía A, Vidal AE, Ruda GF, Kasinathan G, Nguyen C, Ruiz-Pérez LM, Gilbert IH, González-Pacanowska D.

Eur J Med Chem. 2011 Aug;46(8):3309-14. doi: 10.1016/j.ejmech.2011.04.052. Epub 2011 Apr 27.

PMID:
21600680
15.

Modified 5'-trityl nucleosides as inhibitors of Plasmodium falciparum dUTPase.

Ruda GF, Nguyen C, Ziemkowski P, Felczak K, Kasinathan G, Musso-Buendia A, Sund C, Zhou XX, Kaiser M, Ruiz-Pérez LM, Brun R, Kulikowski T, Johansson NG, González-Pacanowska D, Gilbert IH.

ChemMedChem. 2011 Feb 7;6(2):309-20. doi: 10.1002/cmdc.201000445. Epub 2011 Jan 18.

PMID:
21246738
16.

Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.

Cui H, Ruda GF, Carrero-Lérida J, Ruiz-Pérez LM, Gilbert IH, González-Pacanowska D.

Eur J Med Chem. 2010 Nov;45(11):5140-9. doi: 10.1016/j.ejmech.2010.08.026. Epub 2010 Aug 14.

PMID:
20817362
17.

Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds.

Ruda GF, Wong PE, Alibu VP, Norval S, Read KD, Barrett MP, Gilbert IH.

J Med Chem. 2010 Aug 26;53(16):6071-8. doi: 10.1021/jm1004754.

18.

Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase.

Ruda GF, Campbell G, Alibu VP, Barrett MP, Brenk R, Gilbert IH.

Bioorg Med Chem. 2010 Jul 15;18(14):5056-62. doi: 10.1016/j.bmc.2010.05.077. Epub 2010 Jun 9.

19.

Synthesis and biological evaluation of phosphate prodrugs of 4-phospho-D-erythronohydroxamic acid, an inhibitor of 6-phosphogluconate dehydrogenase.

Ruda GF, Alibu VP, Mitsos C, Bidet O, Kaiser M, Brun R, Barrett MP, Gilbert IH.

ChemMedChem. 2007 Aug;2(8):1169-80.

20.
21.

Acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase.

Nguyen C, Ruda GF, Schipani A, Kasinathan G, Leal I, Musso-Buendia A, Kaiser M, Brun R, Ruiz-Pérez LM, Sahlberg BL, Johansson NG, Gonzalez-Pacanowska D, Gilbert IH.

J Med Chem. 2006 Jul 13;49(14):4183-95.

PMID:
16821778

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