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Items: 36


Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy.

Gomes B, Driessens G, Bartlett D, Cai D, Cauwenberghs S, Crosignani S, Dalvie D, Denies S, Dillon CP, Fantin VR, Guo J, Letellier MC, Li W, Maegley K, Marillier R, Miller N, Pirson R, Rabolli V, Ray C, Streiner N, Torti VR, Tsaparikos K, Van den Eynde BJ, Wythes M, Yao LC, Zheng X, Tumang J, Kraus M.

Mol Cancer Ther. 2018 Dec;17(12):2530-2542. doi: 10.1158/1535-7163.MCT-17-1104. Epub 2018 Sep 19.


Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).

Kung PP, Bingham P, Brooun A, Collins M, Deng YL, Dinh D, Fan C, Gajiwala KS, Grantner R, Gukasyan HJ, Hu W, Huang B, Kania R, Kephart SE, Krivacic C, Kumpf RA, Khamphavong P, Kraus M, Liu W, Maegley KA, Nguyen L, Ren S, Richter D, Rollins RA, Sach N, Sharma S, Sherrill J, Spangler J, Stewart AE, Sutton S, Uryu S, Verhelle D, Wang H, Wang S, Wythes M, Xin S, Yamazaki S, Zhu H, Zhu J, Zehnder L, Edwards M.

J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27.


Conserved RNA-binding specificity of polycomb repressive complex 2 is achieved by dispersed amino acid patches in EZH2.

Long Y, Bolanos B, Gong L, Liu W, Goodrich KJ, Yang X, Chen S, Gooding AR, Maegley KA, Gajiwala KS, Brooun A, Cech TR, Liu X.

Elife. 2017 Nov 29;6. pii: e31558. doi: 10.7554/eLife.31558.


Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.

Crosignani S, Bingham P, Bottemanne P, Cannelle H, Cauwenberghs S, Cordonnier M, Dalvie D, Deroose F, Feng JL, Gomes B, Greasley S, Kaiser SE, Kraus M, Négrerie M, Maegley K, Miller N, Murray BW, Schneider M, Soloweij J, Stewart AE, Tumang J, Torti VR, Van Den Eynde B, Wythes M.

J Med Chem. 2017 Dec 14;60(23):9617-9629. doi: 10.1021/acs.jmedchem.7b00974. Epub 2017 Nov 21.


Strategies Employed for the Development of PARP Inhibitors.

Canan S, Maegley K, Curtin NJ.

Methods Mol Biol. 2017;1608:271-297. doi: 10.1007/978-1-4939-6993-7_18.


Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M.

J Med Chem. 2016 Dec 22;59(24):11196. doi: 10.1021/acs.jmedchem.6b01747. Epub 2016 Dec 12. No abstract available.


Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M.

J Med Chem. 2016 Sep 22;59(18):8306-25. doi: 10.1021/acs.jmedchem.6b00515. Epub 2016 Sep 6. Erratum in: J Med Chem. 2016 Dec 22;59(24):11196.


Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance.

Brooun A, Gajiwala KS, Deng YL, Liu W, Bolaños B, Bingham P, He YA, Diehl W, Grable N, Kung PP, Sutton S, Maegley KA, Yu X, Stewart AE.

Nat Commun. 2016 Apr 28;7:11384. doi: 10.1038/ncomms11384.


Comparison of a High-Throughput Mass Spectrometry Method and Radioactive Filter Binding to Assay the Protein Methyltransferase PRMT5.

Maegley KA, Krivacic C, Bingham P, Liu W, Brooun A.

Assay Drug Dev Technol. 2015 May;13(4):235-40. doi: 10.1089/adt.2015.640.


SAH derived potent and selective EZH2 inhibitors.

Kung PP, Huang B, Zehnder L, Tatlock J, Bingham P, Krivacic C, Gajiwala K, Diehl W, Yu X, Maegley KA.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1532-7. doi: 10.1016/j.bmcl.2015.02.017. Epub 2015 Feb 17.


Challenges and opportunities in epigenetic drug discovery.

Cummings RT, Maegley K, Hill WA, Sims R, Mohin S.

Assay Drug Dev Technol. 2014 Oct;12(8):452-6. doi: 10.1089/adt.2014.1502. Epub 2014 Aug 15. No abstract available.


Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as novel PKM2 activators.

Guo C, Linton A, Jalaie M, Kephart S, Ornelas M, Pairish M, Greasley S, Richardson P, Maegley K, Hickey M, Li J, Wu X, Ji X, Xie Z.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3358-63. doi: 10.1016/j.bmcl.2013.03.090. Epub 2013 Apr 1.


Ack1: activation and regulation by allostery.

Gajiwala KS, Maegley K, Ferre R, He YA, Yu X.

PLoS One. 2013;8(1):e53994. doi: 10.1371/journal.pone.0053994. Epub 2013 Jan 14.


Strategies employed for the development of PARP inhibitors.

Canan S, Maegley K, Curtin N.

Methods Mol Biol. 2011;780:463-89. doi: 10.1007/978-1-61779-270-0_28.


Development of hepatitis C virus chimeric replicons for identifying broad spectrum NS3 protease inhibitors.

Binder J, Tetangco S, Weinshank M, Maegley K, Lingardo L, Diehl W, Love R, Patick AK, Smith GJ 3rd.

Antiviral Res. 2011 Aug;91(2):102-11. doi: 10.1016/j.antiviral.2011.05.007. Epub 2011 May 19.


Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone.

Kung PP, Sinnema PJ, Richardson P, Hickey MJ, Gajiwala KS, Wang F, Huang B, McClellan G, Wang J, Maegley K, Bergqvist S, Mehta PP, Kania R.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3557-62. doi: 10.1016/j.bmcl.2011.04.130. Epub 2011 May 5.


Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide.

Zehnder L, Bennett M, Meng J, Huang B, Ninkovic S, Wang F, Braganza J, Tatlock J, Jewell T, Zhou JZ, Burke B, Wang J, Maegley K, Mehta PP, Yin MJ, Gajiwala KS, Hickey MJ, Yamazaki S, Smith E, Kang P, Sistla A, Dovalsantos E, Gehring MR, Kania R, Wythes M, Kung PP.

J Med Chem. 2011 May 12;54(9):3368-85. doi: 10.1021/jm200128m. Epub 2011 Apr 20.


Structure of HIV-1 reverse transcriptase with the inhibitor beta-Thujaplicinol bound at the RNase H active site.

Himmel DM, Maegley KA, Pauly TA, Bauman JD, Das K, Dharia C, Clark AD Jr, Ryan K, Hickey MJ, Love RA, Hughes SH, Bergqvist S, Arnold E.

Structure. 2009 Dec 9;17(12):1625-1635. doi: 10.1016/j.str.2009.09.016.


Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.

Kung PP, Funk L, Meng J, Collins M, Zhou JZ, Johnson MC, Ekker A, Wang J, Mehta P, Yin MJ, Rodgers C, Davies JF 2nd, Bayman E, Smeal T, Maegley KA, Gehring MR.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6273-8. doi: 10.1016/j.bmcl.2008.09.081. Epub 2008 Sep 26.


Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.

Thomas HD, Calabrese CR, Batey MA, Canan S, Hostomsky Z, Kyle S, Maegley KA, Newell DR, Skalitzky D, Wang LZ, Webber SE, Curtin NJ.

Mol Cancer Ther. 2007 Mar;6(3):945-56.


A fluorescence polarization assay for screening inhibitors against the ribonuclease H activity of HIV-1 reverse transcriptase.

Nakayama GR, Bingham P, Tan D, Maegley KA.

Anal Biochem. 2006 Apr 15;351(2):260-5. Epub 2006 Feb 17.


Design, synthesis, and biological evaluation of novel human 5'-deoxy-5'-methylthioadenosine phosphorylase (MTAP) substrates.

Kung PP, Zehnder LR, Meng JJ, Kupchinsky SW, Skalitzky DJ, Johnson MC, Maegley KA, Ekker A, Kuhn LA, Rose PW, Bloom LA.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2829-33.


Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.

Tikhe JG, Webber SE, Hostomsky Z, Maegley KA, Ekkers A, Li J, Yu XH, Almassy RJ, Kumpf RA, Boritzki TJ, Zhang C, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR.

J Med Chem. 2004 Oct 21;47(22):5467-81.


The crystal structure of the RNA-dependent RNA polymerase from human rhinovirus: a dual function target for common cold antiviral therapy.

Love RA, Maegley KA, Yu X, Ferre RA, Lingardo LK, Diehl W, Parge HE, Dragovich PS, Fuhrman SA.

Structure. 2004 Aug;12(8):1533-44.


Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.

White AW, Curtin NJ, Eastman BW, Golding BT, Hostomsky Z, Kyle S, Li J, Maegley KA, Skalitzky DJ, Webber SE, Yu XH, Griffin RJ.

Bioorg Med Chem Lett. 2004 May 17;14(10):2433-7.


Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.

Calabrese CR, Almassy R, Barton S, Batey MA, Calvert AH, Canan-Koch S, Durkacz BW, Hostomsky Z, Kumpf RA, Kyle S, Li J, Maegley K, Newell DR, Notarianni E, Stratford IJ, Skalitzky D, Thomas HD, Wang LZ, Webber SE, Williams KJ, Curtin NJ.

J Natl Cancer Inst. 2004 Jan 7;96(1):56-67.


Identification of potent nontoxic poly(ADP-Ribose) polymerase-1 inhibitors: chemopotentiation and pharmacological studies.

Calabrese CR, Batey MA, Thomas HD, Durkacz BW, Wang LZ, Kyle S, Skalitzky D, Li J, Zhang C, Boritzki T, Maegley K, Calvert AH, Hostomsky Z, Newell DR, Curtin NJ.

Clin Cancer Res. 2003 Jul;9(7):2711-8.


Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.

Skalitzky DJ, Marakovits JT, Maegley KA, Ekker A, Yu XH, Hostomsky Z, Webber SE, Eastman BW, Almassy R, Li J, Curtin NJ, Newell DR, Calvert AH, Griffin RJ, Golding BT.

J Med Chem. 2003 Jan 16;46(2):210-3.


Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.

Canan Koch SS, Thoresen LH, Tikhe JG, Maegley KA, Almassy RJ, Li J, Yu XH, Zook SE, Kumpf RA, Zhang C, Boritzki TJ, Mansour RN, Zhang KE, Ekker A, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR, Webber SE, Hostomsky Z.

J Med Chem. 2002 Nov 7;45(23):4961-74.


Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.

White AW, Almassy R, Calvert AH, Curtin NJ, Griffin RJ, Hostomsky Z, Maegley K, Newell DR, Srinivasan S, Golding BT.

J Med Chem. 2000 Nov 2;43(22):4084-97.


DNA bending by EcoRI DNA methyltransferase accelerates base flipping but compromises specificity.

Allan BW, Garcia R, Maegley K, Mort J, Wong D, Lindstrom W, Beechem JM, Reich NO.

J Biol Chem. 1999 Jul 2;274(27):19269-75.


Ras-catalyzed hydrolysis of GTP: a new perspective from model studies.

Maegley KA, Admiraal SJ, Herschlag D.

Proc Natl Acad Sci U S A. 1996 Aug 6;93(16):8160-6. Review.


Spectroscopic studies of arsenic(III) binding to Escherichia coli RI methyltransferase and to two mutants, C223S and W183F.

Lam WC, Tsao DH, Maki AH, Maegley KA, Reich NO.

Biochemistry. 1992 Nov 3;31(43):10438-42.


Structural and functional analysis of EcoRI DNA methyltransferase by proteolysis.

Reich NO, Maegley KA, Shoemaker DD, Everett E.

Biochemistry. 1991 Mar 19;30(11):2940-6.


Chitin-chitosan membranes. Separations of amino acids and polypeptides.

Pellegrino JJ, Geer S, Maegley K, Rivera R, Steward D, Ko M.

Ann N Y Acad Sci. 1990;589:229-44. No abstract available.


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