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Items: 1 to 20 of 56


Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.

Matralis AN, Xanthopoulos D, Huot G, Lopes-Paciencia S, Cole C, de Vries H, Ferbeyre G, Tsantrizos YS.

Bioorg Med Chem. 2018 Nov 1;26(20):5547-5554. doi: 10.1016/j.bmc.2018.10.001. Epub 2018 Oct 4.


Unraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors.

Lacbay CM, Waller DD, Park J, Gómez Palou M, Vincent F, Huang XF, Ta V, Berghuis AM, Sebag M, Tsantrizos YS.

J Med Chem. 2018 Aug 9;61(15):6904-6917. doi: 10.1021/acs.jmedchem.8b00886. Epub 2018 Jul 25.


Pharmacophore requirements for HIV-1 reverse transcriptase inhibitors that selectively "Freeze" the pre-translocated complex during the polymerization catalytic cycle.

Lacbay CM, Menni M, Bernatchez JA, Götte M, Tsantrizos YS.

Bioorg Med Chem. 2018 May 1;26(8):1713-1726. doi: 10.1016/j.bmc.2018.02.017. Epub 2018 Feb 14.


Isoprenoids and tau pathology in sporadic Alzheimer's disease.

Pelleieux S, Picard C, Lamarre-Théroux L, Dea D, Leduc V, Tsantrizos YS, Poirier J.

Neurobiol Aging. 2018 May;65:132-139. doi: 10.1016/j.neurobiolaging.2018.01.012. Epub 2018 Feb 2.


Crystallographic and thermodynamic characterization of phenylaminopyridine bisphosphonates binding to human farnesyl pyrophosphate synthase.

Park J, Rodionov D, De Schutter JW, Lin YS, Tsantrizos YS, Berghuis AM.

PLoS One. 2017 Oct 16;12(10):e0186447. doi: 10.1371/journal.pone.0186447. eCollection 2017.


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.


Metal-Free Cycloetherification by in Situ Generated P-Stereogenic α-Diazanium Intermediates: A Convergent Synthesis of Enantiomerically Pure Dihydrobenzooxaphospholes.

Li SG, Han ZS, Viereck P, Lee H, Kurouski D, Senanayake CH, Tsantrizos YS.

Org Lett. 2017 Feb 17;19(4):894-897. doi: 10.1021/acs.orglett.7b00051. Epub 2017 Feb 3.


Human farnesyl pyrophosphate synthase is allosterically inhibited by its own product.

Park J, Zielinski M, Magder A, Tsantrizos YS, Berghuis AM.

Nat Commun. 2017 Jan 18;8:14132. doi: 10.1038/ncomms14132.


Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.

Fader LD, Bailey M, Beaulieu E, Bilodeau F, Bonneau P, Bousquet Y, Carson RJ, Chabot C, Coulombe R, Duan J, Fenwick C, Garneau M, Halmos T, Jakalian A, James C, Kawai SH, Landry S, LaPlante SR, Mason SW, Morin S, Rioux N, Simoneau B, Surprenant S, Thavonekham B, Thibeault C, Trinh T, Tsantrizos Y, Tsoung J, Yoakim C, Wernic D.

ACS Med Chem Lett. 2016 Jun 9;7(8):797-801. doi: 10.1021/acsmedchemlett.6b00194. eCollection 2016 Aug 11.


A Covalent Cysteine-Targeting Kinase Inhibitor of Ire1 Permits Allosteric Control of Endoribonuclease Activity.

Waller DD, Jansen G, Golizeh M, Martel-Lorion C, Dejgaard K, Shiao TC, Mancuso J, Tsantrizos YS, Roy R, Sebag M, Sleno L, Thomas DY.

Chembiochem. 2016 May 3;17(9):843-51. doi: 10.1002/cbic.201500485. Epub 2016 Mar 7.


Mutant lamin A links prophase to a p53 independent senescence program.

Moiseeva O, Lessard F, Acevedo-Aquino M, Vernier M, Tsantrizos YS, Ferbeyre G.

Cell Cycle. 2015 Aug 3;14(15):2408-21. doi: 10.1080/15384101.2015.1053671. Epub 2015 Jun 1.


Concise and Practical Asymmetric Synthesis of a Challenging Atropisomeric HIV Integrase Inhibitor.

Fandrick KR, Li W, Zhang Y, Tang W, Gao J, Rodriguez S, Patel ND, Reeves DC, Wu JP, Sanyal S, Gonnella N, Qu B, Haddad N, Lorenz JC, Sidhu K, Wang J, Ma S, Grinberg N, Lee H, Tsantrizos Y, Poupart MA, Busacca CA, Yee NK, Lu BZ, Senanayake CH.

Angew Chem Int Ed Engl. 2015 Jun 8;54(24):7144-8. doi: 10.1002/anie.201501575. Epub 2015 May 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.


Modular assembly of purine-like bisphosphonates as inhibitors of HIV-1 reverse transcriptase.

Lacbay CM, Mancuso J, Lin YS, Bennett N, Götte M, Tsantrizos YS.

J Med Chem. 2014 Sep 11;57(17):7435-49. doi: 10.1021/jm501010f. Epub 2014 Aug 29.


A highly concise and convergent synthesis of HCV polymerase inhibitor Deleobuvir (BI 207127): application of a one-pot borylation-Suzuki coupling reaction.

Zhang Y, Lu BZ, Li G, Rodriguez S, Tan J, Wei HX, Liu J, Roschangar F, Ding F, Zhao W, Qu B, Reeves D, Grinberg N, Lee H, Heckmann G, Niemeier O, Brenner M, Tsantrizos Y, Beaulieu PL, Hossain A, Yee N, Farina V, Senanayake CH.

Org Lett. 2014 Sep 5;16(17):4558-61. doi: 10.1021/ol5021114. Epub 2014 Aug 8.


Human isoprenoid synthase enzymes as therapeutic targets.

Park J, Matralis AN, Berghuis AM, Tsantrizos YS.

Front Chem. 2014 Jul 22;2:50. doi: 10.3389/fchem.2014.00050. eCollection 2014. Review.


Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.

Fader LD, Carson R, Morin S, Bilodeau F, Chabot C, Halmos T, Bailey MD, Kawai SH, Coulombe R, Laplante S, Mekhssian K, Jakalian A, Garneau M, Duan J, Mason SW, Simoneau B, Fenwick C, Tsantrizos Y, Yoakim C.

ACS Med Chem Lett. 2014 Apr 16;5(6):711-6. doi: 10.1021/ml500110j. eCollection 2014 Jun 12.


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.


Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.

Fader LD, Malenfant E, Parisien M, Carson R, Bilodeau F, Landry S, Pesant M, Brochu C, Morin S, Chabot C, Halmos T, Bousquet Y, Bailey MD, Kawai SH, Coulombe R, LaPlante S, Jakalian A, Bhardwaj PK, Wernic D, Schroeder P, Amad M, Edwards P, Garneau M, Duan J, Cordingley M, Bethell R, Mason SW, Bös M, Bonneau P, Poupart MA, Faucher AM, Simoneau B, Fenwick C, Yoakim C, Tsantrizos Y.

ACS Med Chem Lett. 2014 Jan 22;5(4):422-7. doi: 10.1021/ml500002n. eCollection 2014 Apr 10.


Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.

Fenwick C, Amad M, Bailey MD, Bethell R, Bös M, Bonneau P, Cordingley M, Coulombe R, Duan J, Edwards P, Fader LD, Faucher AM, Garneau M, Jakalian A, Kawai S, Lamorte L, LaPlante S, Luo L, Mason S, Poupart MA, Rioux N, Schroeder P, Simoneau B, Tremblay S, Tsantrizos Y, Witvrouw M, Yoakim C.

Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44. doi: 10.1128/AAC.02719-13. Epub 2014 Mar 24.

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