Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 54

1.

The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.

Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, Plant MH, Shaffer PL, Teffera Y, Yi S, Zhang M, Gingras J, DiMauro EF.

J Med Chem. 2017 Feb 9;60(3):1105-1125. doi: 10.1021/acs.jmedchem.6b01496. Epub 2016 Dec 21.

PMID:
28001399
2.

Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators.

Huang X, Shaffer PL, Ayube S, Bregman H, Chen H, Lehto SG, Luther JA, Matson DJ, McDonough SI, Michelsen K, Plant MH, Schneider S, Simard JR, Teffera Y, Yi S, Zhang M, DiMauro EF, Gingras J.

Nat Struct Mol Biol. 2017 Feb;24(2):108-113. doi: 10.1038/nsmb.3329. Epub 2016 Dec 19.

PMID:
27991902
3.

Selective antagonism of TRPA1 produces limited efficacy in models of inflammatory- and neuropathic-induced mechanical hypersensitivity in rats.

Lehto SG, Weyer AD, Youngblood BD, Zhang M, Yin R, Wang W, Teffera Y, Cooke M, Stucky CL, Schenkel L, Geuns-Meyer S, Moyer BD, Wild KD, Gavva NR.

Mol Pain. 2016 Nov 29;12. pii: 1744806916677761. Print 2016.

4.

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.

Schenkel LB, Olivieri PR, Boezio AA, Deak HL, Emkey R, Graceffa RF, Gunaydin H, Guzman-Perez A, Lee JH, Teffera Y, Wang W, Youngblood BD, Yu VL, Zhang M, Gavva NR, Lehto SG, Geuns-Meyer S.

J Med Chem. 2016 Mar 24;59(6):2794-809. doi: 10.1021/acs.jmedchem.6b00039. Epub 2016 Mar 4.

PMID:
26942860
5.

Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.

Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11.

PMID:
26812066
6.

Correction to Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors.

Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2015 May 14;58(9):4087. doi: 10.1021/acs.jmedchem.5b00591. Epub 2015 Apr 22. No abstract available.

PMID:
25901648
7.

Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.

Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.

J Med Chem. 2015 Mar 12;58(5):2417-30. doi: 10.1021/jm501913a. Epub 2015 Mar 3. Erratum in: J Med Chem. 2015 May 14;58(9):4087.

PMID:
25699405
8.

Species difference in glucuronidation formation kinetics with a selective mTOR inhibitor.

Berry LM, Liu J, Colletti A, Krolikowski P, Zhao Z, Teffera Y.

Drug Metab Dispos. 2014 Apr;42(4):707-17. doi: 10.1124/dmd.113.054809. Epub 2014 Jan 14.

9.

Whole-body tissue distribution study of drugs in neonate mice using desorption electrospray ionization mass spectrometry imaging.

Liu J, Gingras J, Ganley KP, Vismeh R, Teffera Y, Zhao Z.

Rapid Commun Mass Spectrom. 2014 Jan 30;28(2):185-90. doi: 10.1002/rcm.6775.

PMID:
24338966
10.

Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.

Hua Z, Bregman H, Buchanan JL, Chakka N, Guzman-Perez A, Gunaydin H, Huang X, Gu Y, Berry V, Liu J, Teffera Y, Huang L, Egge B, Emkey R, Mullady EL, Schneider S, Andrews PS, Acquaviva L, Dovey J, Mishra A, Newcomb J, Saffran D, Serafino R, Strathdee CA, Turci SM, Stanton M, Wilson C, Dimauro EF.

J Med Chem. 2013 Dec 27;56(24):10003-15. doi: 10.1021/jm401317z. Epub 2013 Dec 11.

PMID:
24294969
11.

Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.

Bregman H, Chakka N, Guzman-Perez A, Gunaydin H, Gu Y, Huang X, Berry V, Liu J, Teffera Y, Huang L, Egge B, Mullady EL, Schneider S, Andrews PS, Mishra A, Newcomb J, Serafino R, Strathdee CA, Turci SM, Wilson C, DiMauro EF.

J Med Chem. 2013 Jun 13;56(11):4320-42. doi: 10.1021/jm4000038. Epub 2013 May 23.

PMID:
23701517
12.

Ratios of biliary glutathione disulfide (GSSG) to glutathione (GSH): a potential index to screen drug-induced hepatic oxidative stress in rats and mice.

Cao L, Waldon D, Teffera Y, Roberts J, Wells M, Langley M, Zhao Z.

Anal Bioanal Chem. 2013 Mar;405(8):2635-42. doi: 10.1007/s00216-012-6661-8. Epub 2013 Feb 3.

PMID:
23377112
13.

Impact of hydrolysis-mediated clearance on the pharmacokinetics of novel anaplastic lymphoma kinase inhibitors.

Teffera Y, Berry LM, Brake RL, Lewis RT, Saffran DC, Moore E, Liu J, Zhao Z.

Drug Metab Dispos. 2013 Jan;41(1):238-47. doi: 10.1124/dmd.112.047993. Epub 2012 Nov 1.

14.

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.

Peterson EA, Boezio AA, Andrews PS, Boezio CM, Bush TL, Cheng AC, Choquette D, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Kim JL, Lewis RT, Liu J, Mullady EL, Potashman MH, Romero K, Shaffer PL, Stanton MK, Stellwagen JC, Teffera Y, Yi S, Cai T, La DS.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4967-74. doi: 10.1016/j.bmcl.2012.06.033. Epub 2012 Jun 16.

PMID:
22765895
15.

The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.

Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H, Epstein LF, Emkey R, Andrews PS, Yu VL, Saffran DC, Xu M, Drew A, Merkel P, Szilvassy S, Brake RL.

J Med Chem. 2012 Jul 26;55(14):6523-40. doi: 10.1021/jm3005866. Epub 2012 Jul 10.

PMID:
22734674
16.

Localization and quantification of drugs in animal tissues by use of desorption electrospray ionization mass spectrometry imaging.

Vismeh R, Waldon DJ, Teffera Y, Zhao Z.

Anal Chem. 2012 Jun 19;84(12):5439-45. doi: 10.1021/ac3011654. Epub 2012 Jun 11.

PMID:
22663341
17.

Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.

Henne KR, Tran TB, VandenBrink BM, Rock DA, Aidasani DK, Subramanian R, Mason AK, Stresser DM, Teffera Y, Wong SG, Johnson MG, Chen X, Tonn GR, Wong BK.

Drug Metab Dispos. 2012 Jul;40(7):1429-40. doi: 10.1124/dmd.112.045708. Epub 2012 Apr 19.

18.

Application of on-line nano-liquid chromatography/mass spectrometry in metabolite identification studies.

Liu J, Zhao Z, Teffera Y.

Rapid Commun Mass Spectrom. 2012 Feb 15;26(3):320-6. doi: 10.1002/rcm.5332.

PMID:
22223319
19.

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.

Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2064-70. doi: 10.1016/j.bmcl.2011.02.007. Epub 2011 Feb 12.

PMID:
21376583
20.

Identification of quinone imine containing glutathione conjugates of diclofenac in rat bile.

Waldon DJ, Teffera Y, Colletti AE, Liu J, Zurcher D, Copeland KW, Zhao Z.

Chem Res Toxicol. 2010 Dec 20;23(12):1947-53. doi: 10.1021/tx100296v.

PMID:
21053927
21.

Bioactivation of isothiazoles: minimizing the risk of potential toxicity in drug discovery.

Teffera Y, Choquette D, Liu J, Colletti AE, Hollis LS, Lin MH, Zhao Z.

Chem Res Toxicol. 2010 Nov 15;23(11):1743-52. doi: 10.1021/tx100208k. Epub 2010 Sep 8.

PMID:
20825217
22.

Desorption electrospray ionization tissue imaging using heated nebulizing gas and high-resolution accurate mass spectra.

Waldon DJ, Zhao Z, Teffera Y.

Rapid Commun Mass Spectrom. 2010 Aug 30;24(16):2352-6. doi: 10.1002/rcm.4652.

PMID:
20635324
23.

Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.

Boezio AA, Berry L, Albrecht BK, Bauer D, Bellon SF, Bode C, Chen A, Choquette D, Dussault I, Fang M, Hirai S, Kaplan-Lefko P, Larrow JF, Lin MH, Lohman J, Potashman MH, Qu Y, Rex K, Santostefano M, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Harmange JC.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. doi: 10.1016/j.bmcl.2009.09.096. Epub 2009 Sep 27. Erratum in: Bioorg Med Chem Lett. 2010 Jan 15;20(2):773. Fang, Mei [added]; Qu, Yusheng [added].

PMID:
19819693
24.

Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo.

Teffera Y, Colletti AE, Harmange JC, Hollis LS, Albrecht BK, Boezio AA, Liu J, Zhao Z.

Chem Res Toxicol. 2008 Nov;21(11):2216-22. doi: 10.1021/tx800307n.

PMID:
18837519
25.

Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: synthesis, SAR, and pharmacokinetic properties.

Choquette D, Teffera Y, Polverino A, Harmange JC.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4054-8. doi: 10.1016/j.bmcl.2008.05.114. Epub 2008 Jun 4.

PMID:
18573658
26.

Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).

Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, Lin J, Moriguchi J, Berry L, Huang L, Teffera Y, Yang Y, Zhang Y, Bellon SF, Lee M, Shimanovich R, Bak A, Dominguez C, Norman MH, Harmange JC, Dussault I, Kim TS.

J Med Chem. 2008 Jul 10;51(13):3688-91. doi: 10.1021/jm800401t. Epub 2008 Jun 14.

PMID:
18553959
27.

A novel bioactivation pathway for 2-[2-(2,6-dichlorophenyl)aminophenyl]ethanoic acid (diclofenac) initiated by cytochrome P450-mediated oxidative decarboxylation.

Grillo MP, Ma J, Teffera Y, Waldon DJ.

Drug Metab Dispos. 2008 Sep;36(9):1740-4. doi: 10.1124/dmd.108.021287. Epub 2008 Jun 9.

28.

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.

Albrecht BK, Harmange JC, Bauer D, Berry L, Bode C, Boezio AA, Chen A, Choquette D, Dussault I, Fridrich C, Hirai S, Hoffman D, Larrow JF, Kaplan-Lefko P, Lin J, Lohman J, Long AM, Moriguchi J, O'Connor A, Potashman MH, Reese M, Rex K, Siegmund A, Shah K, Shimanovich R, Springer SK, Teffera Y, Yang Y, Zhang Y, Bellon SF.

J Med Chem. 2008 May 22;51(10):2879-82. doi: 10.1021/jm800043g. Epub 2008 Apr 22.

PMID:
18426196
29.

Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.

Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R.

J Med Chem. 2008 Mar 27;51(6):1649-67. doi: 10.1021/jm701097z. Epub 2008 Mar 7.

PMID:
18324761
30.

Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.

Weiss MM, Harmange JC, Polverino AJ, Bauer D, Berry L, Berry V, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Whittington DA, Zanon R.

J Med Chem. 2008 Mar 27;51(6):1668-80. doi: 10.1021/jm701098w. Epub 2008 Mar 7.

PMID:
18324759
31.

Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.

La DS, Belzile J, Bready JV, Coxon A, DeMelfi T, Doerr N, Estrada J, Flynn JC, Flynn SR, Graceffa RF, Harriman SP, Larrow JF, Long AM, Martin MW, Morrison MJ, Patel VF, Roveto PM, Wang L, Weiss MM, Whittington DA, Teffera Y, Zhao Z, Polverino AJ, Harmange JC.

J Med Chem. 2008 Mar 27;51(6):1695-705. doi: 10.1021/jm701129j. Epub 2008 Feb 27.

PMID:
18311900
32.

Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats.

Tang W, Stearns RA, Chen Q, Bleasby K, Teffera Y, Colletti A, Hafey M, Evers R, Dean DC, Magriotis PA, Lanza TJ, Lin LS, Hagmann WK, Baillie TA.

Xenobiotica. 2008 Feb;38(2):223-37. doi: 10.1080/00498250701744682 .

PMID:
18197560
33.

Identification of a novel glutathione conjugate of diclofenac by LTQ-Orbitrap.

Teffera Y, Waldon DJ, Colletti AE, Albrecht BK, Zhao Z.

Drug Metab Lett. 2008 Jan;2(1):35-40.

PMID:
19356068
34.

Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs.

Beconi MG, Reed JR, Teffera Y, Xia YQ, Kochansky CJ, Liu DQ, Xu S, Elmore CS, Ciccotto S, Hora DF, Stearns RA, Vincent SH.

Drug Metab Dispos. 2007 Apr;35(4):525-32. Epub 2007 Jan 12.

35.

Species differences in metabolism and pharmacokinetics of a sphingosine-1-phosphate receptor agonist in rats and dogs: formation of a unique glutathione adduct in the rat.

Anari MR, Creighton MD, Ngui JS, Tschirret-Guth RA, Teffera Y, Doss GA, Tang W, Yu NX, Ciccotto SL, Hobra DF Jr, Coleman JB, Vincent SH, Evans DC.

Drug Metab Dispos. 2006 Aug;34(8):1367-75. Epub 2006 May 12.

36.

Metabolic activation of a pentafluorophenylethylamine derivative: formation of glutathione conjugates in vitro in the rat.

Shang J, Xu S, Teffera Y, Doss GA, Stearns RA, Edmonson S, Beconi MG.

Xenobiotica. 2005 Jul;35(7):697-713.

PMID:
16316929
37.

Metabolic activation of a 1,3-disubstituted piperazine derivative: evidence for a novel ring contraction to an imidazoline.

Doss GA, Miller RR, Zhang Z, Teffera Y, Nargund RP, Palucki B, Park MK, Tang YS, Evans DC, Baillie TA, Stearns RA.

Chem Res Toxicol. 2005 Feb;18(2):271-6.

PMID:
15720132
38.

Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes.

Xu S, Zhu B, Teffera Y, Pan DE, Caldwell CG, Doss G, Stearns RA, Evans DC, Beconi MG.

Drug Metab Dispos. 2005 Jan;33(1):121-30. Epub 2004 Oct 14.

39.

Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.

Brockunier LL, He J, Colwell LF Jr, Habulihaz B, He H, Leiting B, Lyons KA, Marsilio F, Patel RA, Teffera Y, Wu JK, Thornberry NA, Weber AE, Parmee ER.

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4763-6.

PMID:
15324904
40.

Amidines as amide bond replacements in VLA-4 antagonists.

Kamenecka TM, Park YJ, Lin LS, de Laszlo S, McCauley ED, Van Riper G, Egger L, Kidambi U, Mumford RA, Tong S, Tang W, Colletti A, Teffera Y, Stearns R, MacCoss M, Schmidt JA, Hagmann WK.

Bioorg Med Chem Lett. 2004 May 3;14(9):2323-6.

PMID:
15081033
41.

Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.

Kopka IE, Lin LS, Mumford RA, Lanza T Jr, Magriotis PA, Young D, DeLaszlo SE, MacCoss M, Mills SG, Van Riper G, McCauley E, Lyons K, Vincent S, Egger LA, Kidambi U, Stearns R, Colletti A, Teffera Y, Tong S, Owens K, Levorse D, Schmidt JA, Hagmann WK.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2415-8.

PMID:
12161146
42.

The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.

Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T Jr, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4. Erratum in: Bioorg Med Chem Lett. 2002 Jun 17;12(12):1695.

PMID:
11844683
43.

Bioactivation of diclofenac via benzoquinone imine intermediates-identification of urinary mercapturic acid derivatives in rats and humans.

Poon GK, Chen Q, Teffera Y, Ngui JS, Griffin PR, Braun MP, Doss GA, Freeden C, Stearns RA, Evans DC, Baillie TA, Tang W.

Drug Metab Dispos. 2001 Dec;29(12):1608-13.

45.

Studying the reaction between clozapine and glutathione with element-selective detection.

Teng J, Teffera Y, McLean M, Abramson FP.

Res Commun Mol Pathol Pharmacol. 1998 Feb;99(2):131-42.

PMID:
9583088
46.

Replacing 14C with stable isotopes in drug metabolism studies.

Abramson FP, Teffera Y, Kusmierz J, Steenwyk RC, Pearson PG.

Drug Metab Dispos. 1996 Jul;24(7):697-701.

PMID:
8818564
47.

Isotopic differences in human growth hormone preparations.

Abramson FP, Osborn BL, Teffera Y.

Anal Chem. 1996 Jun 1;68(11):1971-2.

PMID:
8686917
48.
49.
50.

Direct determination of human urinary cortisol metabolites by HPLC/CRIMS.

Yergey AL, Teffera Y, Esteban NV, Abramson FP.

Steroids. 1995 Mar;60(3):295-8.

PMID:
7792835

Supplemental Content

Loading ...
Support Center