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Items: 1 to 20 of 71

1.

Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.

De Schutter JW, Park J, Leung CY, Gormley P, Lin YS, Hu Z, Berghuis AM, Poirier J, Tsantrizos YS.

J Med Chem. 2014 Jul 10;57(13):5764-76. doi: 10.1021/jm500629e. Epub 2014 Jun 23.

PMID:
24911527
2.

Pharmacophore Mapping of Thienopyrimidine-Based Monophosphonate (ThP-MP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase.

Park J, Leung CY, Matralis AN, Lacbay CM, Tsakos M, Fernandez De Troconiz G, Berghuis AM, Tsantrizos YS.

J Med Chem. 2017 Mar 9;60(5):2119-2134. doi: 10.1021/acs.jmedchem.6b01888. Epub 2017 Feb 28.

PMID:
28208018
3.

Thienopyrimidine bisphosphonate (ThPBP) inhibitors of the human farnesyl pyrophosphate synthase: optimization and characterization of the mode of inhibition.

Leung CY, Park J, De Schutter JW, Sebag M, Berghuis AM, Tsantrizos YS.

J Med Chem. 2013 Oct 24;56(20):7939-50. doi: 10.1021/jm400946f. Epub 2013 Oct 3.

PMID:
23998921
4.

Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.

Gritzalis D, Park J, Chiu W, Cho H, Lin YS, De Schutter JW, Lacbay CM, Zielinski M, Berghuis AM, Tsantrizos YS.

Bioorg Med Chem Lett. 2015 Mar 1;25(5):1117-23. doi: 10.1016/j.bmcl.2014.12.089. Epub 2015 Jan 13.

PMID:
25630225
5.

Design of potent bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase via targeted interactions with the active site 'capping' phenyls.

De Schutter JW, Shaw J, Lin YS, Tsantrizos YS.

Bioorg Med Chem. 2012 Sep 15;20(18):5583-91. doi: 10.1016/j.bmc.2012.07.019. Epub 2012 Jul 24.

PMID:
22884353
6.

Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.

Lin YS, Park J, De Schutter JW, Huang XF, Berghuis AM, Sebag M, Tsantrizos YS.

J Med Chem. 2012 Apr 12;55(7):3201-15. doi: 10.1021/jm201657x. Epub 2012 Mar 19.

PMID:
22390415
7.

Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.

Jahnke W, Rondeau JM, Cotesta S, Marzinzik A, Pellé X, Geiser M, Strauss A, Götte M, Bitsch F, Hemmig R, Henry C, Lehmann S, Glickman JF, Roddy TP, Stout SJ, Green JR.

Nat Chem Biol. 2010 Sep;6(9):660-6. doi: 10.1038/nchembio.421. Epub 2010 Aug 15.

PMID:
20711197
8.

Structure of human farnesyl pyrophosphate synthase in complex with an aminopyridine bisphosphonate and two molecules of inorganic phosphate.

Park J, Lin YS, Tsantrizos YS, Berghuis AM.

Acta Crystallogr F Struct Biol Commun. 2014 Mar;70(Pt 3):299-304. doi: 10.1107/S2053230X14002106. Epub 2014 Feb 19.

9.

Mechanistic insights into protonation state as a critical factor in hFPPS enzyme inhibition.

Fernández D, Ortega-Castro J, Mariño L, Perelló J, Frau J.

J Comput Aided Mol Des. 2015 Jul;29(7):667-80. doi: 10.1007/s10822-015-9853-4. Epub 2015 Jun 17.

PMID:
26081258
10.

Discovery of thienopyrimidine-based inhibitors of the human farnesyl pyrophosphate synthase--parallel synthesis of analogs via a trimethylsilyl ylidene intermediate.

Leung CY, Langille AM, Mancuso J, Tsantrizos YS.

Bioorg Med Chem. 2013 Apr 15;21(8):2229-2240. doi: 10.1016/j.bmc.2013.02.006. Epub 2013 Feb 18.

PMID:
23477945
11.

Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding.

Marzinzik AL, Amstutz R, Bold G, Bourgier E, Cotesta S, Glickman JF, Götte M, Henry C, Lehmann S, Hartwieg JC, Ofner S, Pellé X, Roddy TP, Rondeau JM, Stauffer F, Stout SJ, Widmer A, Zimmermann J, Zoller T, Jahnke W.

ChemMedChem. 2015 Nov;10(11):1884-91. doi: 10.1002/cmdc.201500338. Epub 2015 Sep 18.

PMID:
26381451
12.
13.

Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase.

Rodriguez JB, Falcone BN, Szajnman SH.

Expert Opin Drug Discov. 2016;11(3):307-20. doi: 10.1517/17460441.2016.1143814. Epub 2016 Feb 15. Review.

PMID:
26781029
14.

Digeranyl bisphosphonate inhibits geranylgeranyl pyrophosphate synthase.

Wiemer AJ, Tong H, Swanson KM, Hohl RJ.

Biochem Biophys Res Commun. 2007 Feb 23;353(4):921-5. Epub 2006 Dec 21.

PMID:
17208200
15.

The farnesyl-diphosphate/geranylgeranyl-diphosphate synthase of Toxoplasma gondii is a bifunctional enzyme and a molecular target of bisphosphonates.

Ling Y, Li ZH, Miranda K, Oldfield E, Moreno SN.

J Biol Chem. 2007 Oct 19;282(42):30804-16. Epub 2007 Aug 27.

16.

Design, synthesis, calorimetry, and crystallographic analysis of 2-alkylaminoethyl-1,1-bisphosphonates as inhibitors of Trypanosoma cruzi farnesyl diphosphate synthase.

Aripirala S, Szajnman SH, Jakoncic J, Rodriguez JB, Docampo R, Gabelli SB, Amzel LM.

J Med Chem. 2012 Jul 26;55(14):6445-54. doi: 10.1021/jm300425y. Epub 2012 Jul 5.

17.

Syntheses and characterization of non-bisphosphonate quinoline derivatives as new FPPS inhibitors.

Liu J, Liu W, Ge H, Gao J, He Q, Su L, Xu J, Gu LQ, Huang ZS, Li D.

Biochim Biophys Acta. 2014 Mar;1840(3):1051-62. doi: 10.1016/j.bbagen.2013.11.006. Epub 2013 Nov 15.

PMID:
24246954
18.

Human farnesyl pyrophosphate synthase inhibition by nitrogen bisphosphonates: a 3D-QSAR study.

Fernández D, Ortega-Castro J, Frau J.

J Comput Aided Mol Des. 2013 Aug;27(8):739-54. doi: 10.1007/s10822-013-9674-2. Epub 2013 Aug 24.

PMID:
23979193
19.

Farnesyl diphosphate synthase inhibitors from in silico screening.

Lindert S, Zhu W, Liu YL, Pang R, Oldfield E, McCammon JA.

Chem Biol Drug Des. 2013 Jun;81(6):742-8. doi: 10.1111/cbdd.12121.

20.

Development of a cellular tau enzyme-linked immunosorbent assay method for screening GSK-3β inhibitors.

Cho GW, Noh MY, Kang BY, Ku IW, Park J, Hong YH, Kim MH, Kim SH.

Assay Drug Dev Technol. 2011 Oct;9(5):503-13. doi: 10.1089/adt.2010.0343. Epub 2011 May 11.

PMID:
21561378

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