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Publikationer i urvalet

50 träffar

Bibliografisk träff 2020-09-29

Aryloxy Diester Phosphonamidate Prodrugs of Phosphoantigens (ProPAgens) as Potent Activators of Vγ9/Vδ2 T-Cell Immune Responses.

Kadri H, Taher TE, Xu Q, Sharif M, Ashby E, Bryan RT, Willcox BE, Mehellou Y.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.0c01232

Bibliografisk träff 2020-09-23

A guanidinium-based inhibitor of a type I isopentenyl diphosphate isomerase.

Abdelmagid WM, Mahmoodi N, Tanner ME.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2020.127577

Bibliografisk träff 2019-10-31

Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.

Bhuiyan NH, Varney ML, Wiemer DF, Holstein SA.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2019.126757

Bibliografisk träff 2018-08-18

Novel bisphosphonates with antiresorptive effect in bone mineralization and osteoclastogenesis.

Savino S, Toscano A, Purgatorio R, Profilo E, Laghezza A, Tortorella P, Angelelli M, Cellamare S, Scala R, Tricarico D, Marobbio CMT, Perna F, Vitale P, Agamennone M, Dimiccoli V, Tolomeo A, Scilimati A.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.08.044

Bibliografisk träff 2016-03-03

DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.

Chen M, Suzuki A, Thakkar S, Yu K, Hu C, Tong W.

Drug Discov Today · review; journal article · DOI 10.1016/j.drudis.2016.02.015

Bibliografisk träff 2015-09-04

Protonation State and Hydration of Bisphosphonate Bound to Farnesyl Pyrophosphate Synthase.

Yokoyama T, Mizuguchi M, Ostermann A, Kusaka K, Niimura N, Schrader TE, Tanaka I.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01147

Bibliografisk träff 2015-04-17

N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.

Zhou X, Born EJ, Allen C, Holstein SA, Wiemer DF.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2015.04.021

Bibliografisk träff 2015-01-29

Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.

Liu YL, Cao R, Wang Y, Oldfield E.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml500528x

Bibliografisk träff 2015-01-13

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 · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2014.12.089

Bibliografisk träff 2014-06-23

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 · research support, non-u.s. gov't; journal article · DOI 10.1021/jm500629e

Bibliografisk träff 2013-11-13

New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.

Ferrer-Casal M, Li C, Galizzi M, Stortz CA, Szajnman SH, Docampo R, Moreno SN, Rodriguez JB.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2013.11.010

Bibliografisk träff 2013-10-03

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 · research support, non-u.s. gov't; journal article · DOI 10.1021/jm400946f

Bibliografisk träff 2012-12-20

Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.

Recher M, Barboza AP, Li ZH, Galizzi M, Ferrer-Casal M, Szajnman SH, Docampo R, Moreno SN, Rodriguez JB.

Eur J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.ejmech.2012.12.015

Bibliografisk träff 2012-12-01

Triazole-based inhibitors of geranylgeranyltransferase II.

Zhou X, Hartman SV, Born EJ, Smits JP, Holstein SA, Wiemer DF.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.bmcl.2012.11.089

Bibliografisk träff 2012-09-19

Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.

Sakatis MZ, Reese MJ, Harrell AW, Taylor MA, Baines IA, Chen L, Bloomer JC, Yang EY, Ellens HM, Ambroso JL, Lovatt CA, Ayrton AD, Clarke SE.

Chem Res Toxicol · journal article · DOI 10.1021/tx300075j

Bibliografisk träff 2012-07-24

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 · journal article · DOI 10.1016/j.bmc.2012.07.019

Bibliografisk träff 2012-03-19

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 · research support, non-u.s. gov't; journal article · DOI 10.1021/jm201657x

Bibliografisk träff 2011-12-15

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

Liu Z, Shi Q, Ding D, Kelly R, Fang H, Tong W.

PLoS Comput Biol · research support, u.s. gov't, p.h.s.; research-article; journal article · DOI 10.1371/journal.pcbi.1002310

Bibliografisk träff 2011-08-05

Remarkable potential of the α-aminophosphonate/phosphinate structural motif in medicinal chemistry.

Mucha A, Kafarski P, Berlicki Ł.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm200587f

Bibliografisk träff 2011-04-01

Synthesis and biological evaluation of new 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.

Rosso VS, Szajnman SH, Malayil L, Galizzi M, Moreno SN, Docampo R, Rodriguez JB.

Bioorg Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2011.02.037

Bibliografisk träff 2010-11-09

Prediction of drug intestinal absorption by new linear and non-linear QSPR.

Talevi A, Goodarzi M, Ortiz EV, Duchowicz PR, Bellera CL, Pesce G, Castro EA, Bruno-Blanch LE.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2010.11.005

Bibliografisk träff 2010-08-11

Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.

De Schutter JW, Zaretsky S, Welbourn S, Pause A, Tsantrizos YS.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.07.133

Bibliografisk träff 2010-05-10

Lipophilic bisphosphonates are potent inhibitors of Plasmodium liver-stage growth.

Singh AP, Zhang Y, No JH, Docampo R, Nussenzweig V, Oldfield E.

Antimicrob Agents Chemother · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1128/aac.00198-10

Bibliografisk träff 2010-05-01

Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.

McKenna CE, Kashemirov BA, Błazewska KM, Mallard-Favier I, Stewart CA, Rojas J, Lundy MW, Ebetino FH, Baron RA, Dunford JE, Kirsten ML, Seabra MC, Bala JL, Marma MS, Rogers MJ, Coxon FP.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm900232u

Bibliografisk träff 2010-05-01

Inhibition of the Fe(4)S(4)-cluster-containing protein IspH (LytB): electron paramagnetic resonance, metallacycles, and mechanisms.

Wang K, Wang W, No JH, Zhang Y, Zhang Y, Oldfield E.

J Am Chem Soc · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/ja909664j

Bibliografisk träff 2010-02-06

Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.

Prado-Prado FJ, García-Mera X, González-Díaz H.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2010.01.068

Bibliografisk träff 2010-02-01

Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.

Varma MV, Obach RS, Rotter C, Miller HR, Chang G, Steyn SJ, El-Kattan A, Troutman MD.

J Med Chem · journal article · DOI 10.1021/jm901371v

Bibliografisk träff 2009-08-01

Physicochemical determinants of human renal clearance.

Varma MV, Feng B, Obach RS, Troutman MD, Chupka J, Miller HR, El-Kattan A.

J Med Chem · journal article · DOI 10.1021/jm900403j

Bibliografisk träff 2008-12-01

Bisphosphonate inhibition of a Plasmodium farnesyl diphosphate synthase and a general method for predicting cell-based activity from enzyme data.

Mukkamala D, No JH, Cass LM, Chang TK, Oldfield E.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm8009074

Bibliografisk träff 2008-07-01

Determination of the microscopic equilibrium dissociation constants for risedronate and its analogues reveals two distinct roles for the nitrogen atom in nitrogen-containing bisphosphonate drugs.

Hounslow AM, Carran J, Brown RJ, Rejman D, Blackburn GM, Watts DJ.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm7015792