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Items: 28

1.

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.

Boy KM, Guernon JM, Zuev DS, Xu L, Zhang Y, Shi J, Marcin LR, Higgins MA, Wu YJ, Krishnananthan S, Li J, Trehan A, Smith D, Toyn JH, Meredith JE, Burton CR, Kimura SR, Zvyaga T, Zhuo X, Lentz KA, Grace JE, Denton R, Morrison JS, Mathur A, Albright CF, Ahlijanian MK, Olson RE, Thompson LA, Macor JE.

ACS Med Chem Lett. 2019 Feb 17;10(3):312-317. doi: 10.1021/acsmedchemlett.8b00541. eCollection 2019 Mar 14.

2.

Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability.

Hartz RA, Vrudhula VM, Ahuja VT, Grace JE, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1360-1363. doi: 10.1016/j.bmcl.2017.02.015. Epub 2017 Feb 10.

PMID:
28223020
3.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

4.

Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.

Ahuja VT, Hartz RA, Molski TF, Mattson GK, Lentz KA, Grace JE Jr, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 May 1;26(9):2184-7. doi: 10.1016/j.bmcl.2016.03.067. Epub 2016 Mar 17.

PMID:
27020524
5.

Design and optimization of tricyclic gamma-secretase modulators.

Shi J, Zuev D, Xu L, Lentz KA, Grace JE, Toyn JH, Olson RE, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1498-502. doi: 10.1016/j.bmcl.2015.06.020. Epub 2015 Jun 12.

PMID:
26848108
6.

Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE).

Boy KM, Guernon JM, Wu YJ, Zhang Y, Shi J, Zhai W, Zhu S, Gerritz SW, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Good AC, Grace JE, Lentz KA, Olson RE, Macor JE, Thompson LA 3rd.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5040-7. doi: 10.1016/j.bmcl.2015.10.031. Epub 2015 Oct 20.

PMID:
26497283
7.

Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice.

Thakker DR, Sankaranarayanan S, Weatherspoon MR, Harrison J, Pierdomenico M, Heisel JM, Thompson LA, Haskell R, Grace JE, Taylor SJ, Albright CF, Shafer LL.

J Neurosci. 2015 Apr 29;35(17):6931-6. doi: 10.1523/JNEUROSCI.2262-14.2015.

8.

Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.

Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF.

Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8.

9.

[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.

Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA, Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7.

PMID:
23010264
10.

Utility of high-resolution accurate MS to eliminate interferences in the bioanalysis of ribavirin and its phosphate metabolites.

Wei C, Grace JE Jr, Zvyaga TA, Drexler DM.

Bioanalysis. 2012 Aug;4(15):1895-905. doi: 10.4155/bio.12.151.

PMID:
22943620
11.

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2.

PMID:
21974952
12.

Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor.

He K, Luettgen JM, Zhang D, He B, Grace JE Jr, Xin B, Pinto DJ, Wong PC, Knabb RM, Lam PY, Wexler RR, Grossman SJ.

Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):129-39. doi: 10.1007/s13318-011-0037-x. Epub 2011 Apr 2.

PMID:
21461793
13.

Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.

Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079.

PMID:
21078556
14.

A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.

Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ.

J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v.

PMID:
19954247
15.

Evaluation of cynomolgus monkey pregnane X receptor, primary hepatocyte, and in vivo pharmacokinetic changes in predicting human CYP3A4 induction.

Kim S, Dinchuk JE, Anthony MN, Orcutt T, Zoeckler ME, Sauer MB, Mosure KW, Vuppugalla R, Grace JE Jr, Simmermacher J, Dulac HA, Pizzano J, Sinz M.

Drug Metab Dispos. 2010 Jan;38(1):16-24. doi: 10.1124/dmd.109.029637.

PMID:
19833845
16.

Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y.

PMID:
19552437
17.

In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19552436
18.

P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.

Meredith JE Jr, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF.

J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22.

PMID:
18499745
19.

N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations.

He K, Qian M, Wong H, Bai SA, He B, Brogdon B, Grace JE, Xin B, Wu J, Ren SX, Zeng H, Deng Y, Graden DM, Olah TV, Unger SE, Luettgen JM, Knabb RM, Pinto DJ, Lam PY, Duan J, Wexler RR, Decicco CP, Christ DD, Grossman SJ.

J Pharm Sci. 2008 Jul;97(7):2568-80.

PMID:
17914718
20.

6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats.

Wong H, Dockens RC, Pajor L, Yeola S, Grace JE Jr, Stark AD, Taub RA, Yocca FD, Zaczek RC, Li YW.

Drug Metab Dispos. 2007 Aug;35(8):1387-92. Epub 2007 May 9.

PMID:
17494642
21.

Glucuronidation in the chimpanzee (Pan troglodytes): studies with acetaminophen, oestradiol and morphine.

Wong H, Grace JE Jr, Wright MR, Browning MR, Grossman SJ, Bai SA, Christ DD.

Xenobiotica. 2006 Dec;36(12):1178-90.

PMID:
17162465
22.

Development and validation of a preclinical food effect model.

Lentz KA, Quitko M, Morgan DG, Grace JE Jr, Gleason C, Marathe PH.

J Pharm Sci. 2007 Feb;96(2):459-72.

PMID:
17075867
23.

Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.

Gillman KW, Higgins MA, Poindexter GS, Browning M, Clarke WJ, Flowers S, Grace JE Jr, Hogan JB, McGovern RT, Iben LG, Mattson GK, Ortiz A, Rassnick S, Russell JW, Antal-Zimanyi I.

Bioorg Med Chem. 2006 Aug 15;14(16):5517-26. Epub 2006 May 11.

PMID:
16697206
24.

The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application.

Wong H, Grossman SJ, Bai SA, Diamond S, Wright MR, Grace JE Jr, Qian M, He K, Yeleswaram K, Christ DD.

Drug Metab Dispos. 2004 Dec;32(12):1359-69. Epub 2004 Aug 27.

PMID:
15333515
25.

Production of recombinant human apoferritin heteromers.

Grace JE Jr, Van Eden ME, Aust SD.

Arch Biochem Biophys. 2000 Dec 1;384(1):116-22.

PMID:
11147822
26.

Behavioral and alimentary response of the rat to acute and chronic changes in environmental temperature.

Mogenson GJ, Mok A, Grace JE, Stevenson JA.

J Physiol (Paris). 1971 May;63(3):346-9. No abstract available.

PMID:
5121944
27.

Thermogenic drinking in the rat.

Grace JE, Stevenson JA.

Am J Physiol. 1971 Apr;220(4):1009-15. No abstract available.

PMID:
5551128
28.

Wire versus silk: choice of surgical wound closure in patients with cancer.

Mendoza CB Jr, Watne AL, Grace JE, Moore GE.

Am J Surg. 1966 Dec;112(6):839-45. No abstract available.

PMID:
5923801

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