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Items: 24

1.

Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species.

Foti RS, Biswas K, Aral J, Be X, Berry L, Cheng Y, Conner K, Falsey JR, Glaus C, Herberich B, Hickman D, Ikotun T, Li H, Long J, Huang L, Miranda LP, Murray J, Moyer B, Netirojjanakul C, Nixey TE, Sham K, Soto M, Tegley CM, Tran L, Wu B, Yin L, Rock DA.

Drug Metab Dispos. 2019 Aug 6. pii: dmd.119.087742. doi: 10.1124/dmd.119.087742. [Epub ahead of print]

2.

Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.

Murray JK, Wu B, Tegley CM, Nixey TE, Falsey JR, Herberich B, Yin L, Sham K, Long J, Aral J, Cheng Y, Netirojjanakul C, Doherty L, Glaus C, Ikotun T, Li H, Tran L, Soto M, Salimi-Moosavi H, Ligutti J, Amagasu S, Andrews KL, Be X, Lin MJ, Foti RS, Ilch CP, Youngblood B, Kornecook TJ, Karow M, Walker KW, Moyer BD, Biswas K, Miranda LP.

ACS Chem Biol. 2019 Apr 19;14(4):806-818. doi: 10.1021/acschembio.9b00183. Epub 2019 Mar 27.

PMID:
30875193
3.

Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx-1 Peptide-Antibody Conjugates.

Biswas K, Nixey TE, Murray JK, Falsey JR, Yin L, Liu H, Gingras J, Hall BE, Herberich B, Holder JR, Li H, Ligutti J, Lin MJ, Liu D, Soriano BD, Soto M, Tran L, Tegley CM, Zou A, Gunasekaran K, Moyer BD, Doherty L, Miranda LP.

ACS Chem Biol. 2017 Sep 15;12(9):2427-2435. doi: 10.1021/acschembio.7b00542. Epub 2017 Aug 28.

PMID:
28800217
4.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr.

J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1.

5.

Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease.

Chen JJ, Qian W, Biswas K, Yuan C, Amegadzie A, Liu Q, Nixey T, Zhu J, Ncube M, Rzasa RM, Chavez F Jr, Chen N, DeMorin F, Rumfelt S, Tegley CM, Allen JR, Hitchcock S, Hungate R, Bartberger MD, Zalameda L, Liu Y, McCarter JD, Zhang J, Zhu L, Babu-Khan S, Luo Y, Bradley J, Wen PH, Reid DL, Koegler F, Dean C Jr, Hickman D, Correll TL, Williamson T, Wood S.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6447-54. doi: 10.1016/j.bmcl.2013.09.041. Epub 2013 Sep 29.

PMID:
24139583
6.

Different modes of inhibitor binding to prolyl hydroxylase by combined use of X-ray crystallography and NMR spectroscopy of paramagnetic complexes.

Poppe L, Tegley CM, Li V, Lewis J, Zondlo J, Yang E, Kurzeja RJ, Syed R.

J Am Chem Soc. 2009 Nov 25;131(46):16654-5. doi: 10.1021/ja907933p.

PMID:
19886658
7.

Kinetic characterization and identification of a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 using a time-resolved fluorescence resonance energy transfer-based assay technology.

Dao JH, Kurzeja RJ, Morachis JM, Veith H, Lewis J, Yu V, Tegley CM, Tagari P.

Anal Biochem. 2009 Jan 15;384(2):213-23. doi: 10.1016/j.ab.2008.09.052. Epub 2008 Oct 14.

PMID:
18952043
8.

Discovery of novel hydroxy-thiazoles as HIF-alpha prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation.

Tegley CM, Viswanadhan VN, Biswas K, Frohn MJ, Peterkin TA, Chang C, Bürli RW, Dao JH, Veith H, Rogers N, Yoder SC, Biddlecome G, Tagari P, Allen JR, Hungate RW.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3925-8. doi: 10.1016/j.bmcl.2008.06.031. Epub 2008 Jun 13.

PMID:
18579373
9.

Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.

Higuchi RI, Thompson AW, Chen JH, Caferro TR, Cummings ML, Deckhut CP, Adams ME, Tegley CM, Edwards JP, López FJ, Kallel EA, Karanewsky DS, Schrader WT, Marschke KB, Zhi L.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5442-6. Epub 2007 Jul 25.

10.

Discovery of ligands for Nurr1 by combined use of NMR screening with different isotopic and spin-labeling strategies.

Poppe L, Harvey TS, Mohr C, Zondlo J, Tegley CM, Nuanmanee O, Cheetham J.

J Biomol Screen. 2007 Apr;12(3):301-11.

PMID:
17438066
11.

Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.

van Oeveren A, Pio BA, Tegley CM, Higuchi RI, Wu M, Jones TK, Marschke KB, Negro-Vilar A, Zhi L.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1523-6. Epub 2007 Jan 13.

PMID:
17257838
12.

(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.

Kim TS, Hague AB, Lee TI, Lian B, Tegley CM, Wang X, Burgess TL, Qian YX, Ross S, Tagari P, Lin CH, Mayeda C, Dao J, Jordan S, Mohr C, Cheetham J, Viswanadhan V, Tasker AS.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):87-90.

PMID:
14684304
13.

5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.

Zhi L, Tegley CM, Pio B, Edwards JP, Motamedi M, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT.

J Med Chem. 2003 Sep 11;46(19):4104-12.

PMID:
12954062
14.

Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.

Zhi L, Ringgenberg JD, Edwards JP, Tegley CM, West SJ, Pio B, Motamedi M, Jones TK, Marschke KB, Mais DE, Schrader WT.

Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.

PMID:
12781198
15.

Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.

Zhi L, Tegley CM, Pio B, Edwards JP, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT.

Bioorg Med Chem Lett. 2003 Jun 16;13(12):2071-4.

PMID:
12781197
16.

Synthesis and biological activity of analogues of the antidiabetic/antiobesity agent 3-guanidinopropionic acid: discovery of a novel aminoguanidinoacetic acid antidiabetic agent.

Larsen SD, Connell MA, Cudahy MM, Evans BR, May PD, Meglasson MD, O'Sullivan TJ, Schostarez HJ, Sih JC, Stevens FC, Tanis SP, Tegley CM, Tucker JA, Vaillancourt VA, Vidmar TJ, Watt W, Yu JH.

J Med Chem. 2001 Apr 12;44(8):1217-30.

PMID:
11312922
17.

Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.

Zhi L, Tegley CM, Pio B, West SJ, Marschke KB, Mais DE, Jones TK.

Bioorg Med Chem Lett. 2000 Mar 6;10(5):415-8.

PMID:
10743938
18.

Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.

Zhi L, Tegley CM, Marschke KB, Jones TK.

Bioorg Med Chem Lett. 1999 Apr 5;9(7):1009-12.

PMID:
10230629
19.
20.

5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.

Zhi L, Tegley CM, Edwards JP, West SJ, Marschke KB, Gottardis MM, Mais DE, Jones TK.

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3365-70.

PMID:
9873735
21.

Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.

Hamann LG, Winn DT, Pooley CL, Tegley CM, West SJ, Farmer LJ, Zhi L, Edwards JP, Marschke KB, Mais DE, Goldman ME, Jones TK.

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2731-6.

PMID:
9873612
22.

5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.

Tegley CM, Zhi L, Marschke KB, Gottardis MM, Yang Q, Jones TK.

J Med Chem. 1998 Oct 22;41(22):4354-9.

PMID:
9784110
23.

Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.

Edwards JP, Zhi L, Pooley CL, Tegley CM, West SJ, Wang MW, Gottardis MM, Pathirana C, Schrader WT, Jones TK.

J Med Chem. 1998 Jul 16;41(15):2779-85.

PMID:
9667968
24.

5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.

Zhi L, Tegley CM, Kallel EA, Marschke KB, Mais DE, Gottardis MM, Jones TK.

J Med Chem. 1998 Jan 29;41(3):291-302.

PMID:
9464360

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