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Items: 26


Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors.

Iglesias J, Lamontagne J, Erb H, Gezzar S, Zhao S, Joly E, Truong VL, Skorey K, Crane S, Madiraju SR, Prentki M.

J Lipid Res. 2016 Jan;57(1):131-41. doi: 10.1194/jlr.D058438. Epub 2015 Sep 30.


Broadening the spectrum of β-lactam antibiotics through inhibition of signal peptidase type I.

Therien AG, Huber JL, Wilson KE, Beaulieu P, Caron A, Claveau D, Deschamps K, Donald RG, Galgoci AM, Gallant M, Gu X, Kevin NJ, Lafleur J, Leavitt PS, Lebeau-Jacob C, Lee SS, Lin MM, Michels AA, Ogawa AM, Painter RE, Parish CA, Park YW, Benton-Perdomo L, Petcu M, Phillips JW, Powles MA, Skorey KI, Tam J, Tan CM, Young K, Wong S, Waddell ST, Miesel L.

Antimicrob Agents Chemother. 2012 Sep;56(9):4662-70. doi: 10.1128/AAC.00726-12. Epub 2012 Jun 18.


Restoring methicillin-resistant Staphylococcus aureus susceptibility to β-lactam antibiotics.

Tan CM, Therien AG, Lu J, Lee SH, Caron A, Gill CJ, Lebeau-Jacob C, Benton-Perdomo L, Monteiro JM, Pereira PM, Elsen NL, Wu J, Deschamps K, Petcu M, Wong S, Daigneault E, Kramer S, Liang L, Maxwell E, Claveau D, Vaillancourt J, Skorey K, Tam J, Wang H, Meredith TC, Sillaots S, Wang-Jarantow L, Ramtohul Y, Langlois E, Landry F, Reid JC, Parthasarathy G, Sharma S, Baryshnikova A, Lumb KJ, Pinho MG, Soisson SM, Roemer T.

Sci Transl Med. 2012 Mar 21;4(126):126ra35. doi: 10.1126/scitranslmed.3003592.


Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors.

Leclerc JP, Falgueyret JP, Girardin M, Guay J, Guiral S, Huang Z, Li CS, Oballa R, Ramtohul YK, Skorey K, Tawa P, Wang H, Zhang L.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6505-9. doi: 10.1016/j.bmcl.2011.08.073. Epub 2011 Aug 25.


Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods.

Hamel M, Henault M, Hyjazie H, Morin N, Bayly C, Skorey K, Therien AG, Mancini J, Brideau C, Kargman S.

J Biomol Screen. 2011 Oct;16(9):1098-105. doi: 10.1177/1087057111415525. Epub 2011 Aug 5.


Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.

Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L.

J Med Chem. 2011 Jul 28;54(14):5082-96. doi: 10.1021/jm200319u. Epub 2011 Jun 28.


High-throughput scintillation proximity assay for stearoyl-CoA desaturase-1.

Tawa P, Falgueyret JP, Guiral S, Isabel E, Powell DA, Zuck P, Skorey K.

J Biomol Screen. 2011 Jun;16(5):506-17. doi: 10.1177/1087057111399436. Epub 2011 Mar 15.


Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors.

Isabel E, Powell DA, Black WC, Chan CC, Crane S, Gordon R, Guay J, Guiral S, Huang Z, Robichaud J, Skorey K, Tawa P, Xu L, Zhang L, Oballa R.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):479-83. doi: 10.1016/j.bmcl.2010.10.107. Epub 2010 Oct 26.


2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors.

Powell DA, Ramtohul Y, Lebrun ME, Oballa R, Bhat S, Falgueyret JP, Guiral S, Huang Z, Skorey K, Tawa P, Zhang L.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6366-9. doi: 10.1016/j.bmcl.2010.09.094. Epub 2010 Sep 19.


Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor.

Han Y, Belley M, Bayly CI, Colucci J, Dufresne C, Giroux A, Lau CK, Leblanc Y, McKay D, Therien M, Wilson MC, Skorey K, Chan CC, Scapin G, Kennedy BP.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5. doi: 10.1016/j.bmcl.2008.04.064. Epub 2008 Apr 29.


Enzyme occupancy measurement of intracellular protein tyrosine phosphatase 1B using photoaffinity probes.

Skorey K, Waddleton D, Therien M, Leriche T.

Anal Biochem. 2006 Feb 1;349(1):49-61. Epub 2005 Dec 1.


Residues distant from the active site influence protein-tyrosine phosphatase 1B inhibitor binding.

Montalibet J, Skorey K, McKay D, Scapin G, Asante-Appiah E, Kennedy BP.

J Biol Chem. 2006 Feb 24;281(8):5258-66. Epub 2005 Dec 6.


Protein tyrosine phosphatase: enzymatic assays.

Montalibet J, Skorey KI, Kennedy BP.

Methods. 2005 Jan;35(1):2-8. Review.


Synthesis of a novel peptidic photoaffinity probe for the PTP-1B enzyme.

Thérien M, Skorey K, Zamboni R, Li CS, Lau CK, LeRiche T, Linh Truong V, Waddleton D, Ramachandran C.

Bioorg Med Chem Lett. 2004 May 3;14(9):2319-22.


Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.

Lau CK, Bayly CI, Gauthier JY, Li CS, Therien M, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Payette P, Ramachandran C, Kennedy BP, Scapin G.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1043-8.


The development of potent non-peptidic PTP-1B inhibitors.

Dufresne C, Roy P, Wang Z, Asante-Appiah E, Cromlish W, Boie Y, Forghani F, Desmarais S, Wang Q, Skorey K, Waddleton D, Ramachandran C, Kennedy BP, Xu L, Gordon R, Chan CC, Leblanc Y.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1039-42.


The structural basis for the selectivity of benzotriazole inhibitors of PTP1B.

Scapin G, Patel SB, Becker JW, Wang Q, Desponts C, Waddleton D, Skorey K, Cromlish W, Bayly C, Therien M, Gauthier JY, Li CS, Lau CK, Ramachandran C, Kennedy BP, Asante-Appiah E.

Biochemistry. 2003 Oct 7;42(39):11451-9.


Development of a robust scintillation proximity assay for protein tyrosine phosphatase 1B using the catalytically inactive (C215S) mutant.

Skorey KI, Kennedy BP, Friesen RW, Ramachandran C.

Anal Biochem. 2001 Apr 15;291(2):269-78.


The YRD motif is a major determinant of substrate and inhibitor specificity in T-cell protein-tyrosine phosphatase.

Asante-Appiah E, Ball K, Bateman K, Skorey K, Friesen R, Desponts C, Payette P, Bayly C, Zamboni R, Scapin G, Ramachandran C, Kennedy BP.

J Biol Chem. 2001 Jul 13;276(28):26036-43. Epub 2001 May 14.


A two-component affinity chromatography purification of Helix pomatia arylsulfatase by tyrosine vanadate.

Skorey KI, Johnson NA, Huyer G, Gresser MJ.

Protein Expr Purif. 1999 Mar;15(2):178-87.


How does alendronate inhibit protein-tyrosine phosphatases?

Skorey K, Ly HD, Kelly J, Hammond M, Ramachandran C, Huang Z, Gresser MJ, Wang Q.

J Biol Chem. 1997 Sep 5;272(36):22472-80.


Characterization of autocrine inducible prostaglandin H synthase-2 (PGHS-2) in human osteosarcoma cells.

Wong E, DeLuca C, Boily C, Charleson S, Cromlish W, Denis D, Kargman S, Kennedy BP, Ouellet M, Skorey K, O'Neill GP, Vickers PJ, Riendeau D.

Inflamm Res. 1997 Feb;46(2):51-9.


From indomethacin to a selective COX-2 inhibitor. Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors.

Lau CK, Black WC, Belley M, Chan C, Charleson S, Denis D, Gauthier JY, Gordon R, Guay D, Hamel P, Kargman S, Leblanc Y, Mancini J, Ouellet M, Percival D, Prasit P, Roy P, Skorey K, Tagari P, Vickers P, Wong E.

Adv Exp Med Biol. 1997;407:73-8. No abstract available.


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