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Items: 23

1.

A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose.

Durham TB, Marimuthu J, Toth JL, Liu C, Adams L, Mudra DR, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR.

J Med Chem. 2017 Jul 13;60(13):5933-5939. doi: 10.1021/acs.jmedchem.7b00650. Epub 2017 Jun 29.

PMID:
28613895
2.

Translational pharmacokinetic-pharmacodynamic analysis in the pharmaceutical industry: an IQ Consortium PK-PD Discussion Group perspective.

Wong H, Bohnert T, Damian-Iordache V, Gibson C, Hsu CP, Krishnatry AS, Liederer BM, Lin J, Lu Q, Mettetal JT, Mudra DR, Nijsen MJMA, Schroeder P, Schuck E, Suryawanshi S, Trapa P, Tsai A, Wang H, Wu F.

Drug Discov Today. 2017 Oct;22(10):1447-1459. doi: 10.1016/j.drudis.2017.04.015. Epub 2017 May 2. Review.

PMID:
28476536
3.

Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1.

Partridge KM, Antonysamy S, Bhattachar SN, Chandrasekhar S, Fisher MJ, Fretland A, Gooding K, Harvey A, Hughes NE, Kuklish SL, Luz JG, Manninen PR, McGee JE, Mudra DR, Navarro A, Norman BH, Quimby SJ, Schiffler MA, Sloan AV, Warshawsky AM, Weller JM, York JS, Yu XP.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1478-1483. doi: 10.1016/j.bmcl.2016.11.011. Epub 2016 Nov 7.

PMID:
28190634
4.

Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.

Jones SB, Pfeifer LA, Bleisch TJ, Beauchamp TJ, Durbin JD, Klimkowski VJ, Hughes NE, Rito CJ, Dao Y, Gruber JM, Bui H, Chambers MG, Chandrasekhar S, Lin C, McCann DJ, Mudra DR, Oskins JL, Swearingen CA, Thirunavukkarasu K, Norman BH.

ACS Med Chem Lett. 2016 Aug 2;7(9):857-61. doi: 10.1021/acsmedchemlett.6b00207. eCollection 2016 Sep 8.

5.

Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.

Wiley MR, Durham TB, Adams LA, Chambers MG, Lin C, Liu C, Marimuthu J, Mitchell PG, Mudra DR, Swearingen CA, Toth JL, Weller JM, Thirunavukkarasu K.

J Med Chem. 2016 Jun 23;59(12):5810-22. doi: 10.1021/acs.jmedchem.6b00398. Epub 2016 Jun 9.

PMID:
27194201
6.

Identification and biological activity of 6-alkyl-substituted 3-methyl-pyridine-2-carbonyl amino dimethyl-benzoic acid EP4 antagonists.

Blanco MJ, Vetman T, Chandrasekhar S, Fisher MJ, Harvey A, Kuklish SL, Chambers M, Lin C, Mudra D, Oskins J, Wang XS, Yu XP, Warshawsky AM.

Bioorg Med Chem Lett. 2016 May 1;26(9):2303-7. doi: 10.1016/j.bmcl.2016.03.041. Epub 2016 Mar 12.

PMID:
27020304
7.

Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.

Blanco MJ, Vetman T, Chandrasekhar S, Fisher MJ, Harvey A, Chambers M, Lin C, Mudra D, Oskins J, Wang XS, Yu XP, Warshawsky AM.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):931-935. doi: 10.1016/j.bmcl.2015.12.057. Epub 2015 Dec 25.

PMID:
26764191
8.

Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.

Blanco MJ, Vetman T, Chandrasekhar S, Fisher MJ, Harvey A, Mudra D, Wang XS, Yu XP, Schiffler MA, Warshawsky AM.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):105-9. doi: 10.1016/j.bmcl.2015.11.023. Epub 2015 Nov 10.

PMID:
26608552
9.

Preclinical pharmacokinetic/pharmacodynamic modeling and simulation in the pharmaceutical industry: an IQ consortium survey examining the current landscape.

Schuck E, Bohnert T, Chakravarty A, Damian-Iordache V, Gibson C, Hsu CP, Heimbach T, Krishnatry AS, Liederer BM, Lin J, Maurer T, Mettetal JT, Mudra DR, Nijsen MJ, Raybon J, Schroeder P, Schuck V, Suryawanshi S, Su Y, Trapa P, Tsai A, Vakilynejad M, Wang S, Wong H.

AAPS J. 2015 Mar;17(2):462-73. doi: 10.1208/s12248-014-9716-2. Epub 2015 Jan 29.

10.

Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.

Toledo MA, Pedregal C, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Torrado A, Mateos C, Joshi EM, Kahl SD, Rash KS, Mudra DR, Barth VN, Shaw DB, McKinzie D, Witkin JM, Statnick MA.

J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11.

PMID:
24678969
11.

Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.

Pedregal C, Joshi EM, Toledo MA, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Navarro A, Chen Z, Mudra DR, Kahl SD, Rash KS, Statnick MA, Barth VN.

J Med Chem. 2012 Jun 14;55(11):4955-67. doi: 10.1021/jm201629q. Epub 2012 May 16.

PMID:
22541041
12.

In silico, in vitro and in situ models to assess interplay between CYP3A and P-gp.

Mudra DR, Desino KE, Desai PV.

Curr Drug Metab. 2011 Oct;12(8):750-73. Review.

PMID:
21568936
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16.

The effect of fenbuconazole on cell proliferation and enzyme induction in the liver of female CD1 mice.

Juberg DR, Mudra DR, Hazelton GA, Parkinson A.

Toxicol Appl Pharmacol. 2006 Jul 15;214(2):178-87. Epub 2006 Mar 20.

PMID:
16542693
17.

The effects of gender, age, ethnicity, and liver cirrhosis on cytochrome P450 enzyme activity in human liver microsomes and inducibility in cultured human hepatocytes.

Parkinson A, Mudra DR, Johnson C, Dwyer A, Carroll KM.

Toxicol Appl Pharmacol. 2004 Sep 15;199(3):193-209. Review.

PMID:
15364537
18.

Effects of prototypical microsomal enzyme inducers on cytochrome P450 expression in cultured human hepatocytes.

Madan A, Graham RA, Carroll KM, Mudra DR, Burton LA, Krueger LA, Downey AD, Czerwinski M, Forster J, Ribadeneira MD, Gan LS, LeCluyse EL, Zech K, Robertson P Jr, Koch P, Antonian L, Wagner G, Yu L, Parkinson A.

Drug Metab Dispos. 2003 Apr;31(4):421-31.

PMID:
12642468
19.

Analysis of CYP mRNA expression by branched DNA technology.

Czerwinski M, Opdam P, Madan A, Carroll K, Mudra DR, Gan LL, Luo G, Parkinson A.

Methods Enzymol. 2002;357:170-9. No abstract available.

PMID:
12424908
20.

In vivo and in vitro induction of cytochrome P450 enzymes in beagle dogs.

Graham RA, Downey A, Mudra D, Krueger L, Carroll K, Chengelis C, Madan A, Parkinson A.

Drug Metab Dispos. 2002 Nov;30(11):1206-13.

PMID:
12386126
21.

CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes.

Luo G, Cunningham M, Kim S, Burn T, Lin J, Sinz M, Hamilton G, Rizzo C, Jolley S, Gilbert D, Downey A, Mudra D, Graham R, Carroll K, Xie J, Madan A, Parkinson A, Christ D, Selling B, LeCluyse E, Gan LS.

Drug Metab Dispos. 2002 Jul;30(7):795-804.

PMID:
12065438
22.

Preparation of hepatocytes.

Mudra DR, Parkinson A.

Curr Protoc Toxicol. 2001 Aug;Chapter 14:Unit 14.2. doi: 10.1002/0471140856.tx1402s08.

PMID:
23045038
23.

Effect of cryopreservation on cytochrome P-450 enzyme induction in cultured rat hepatocytes.

Madan A, DeHaan R, Mudra D, Carroll K, LeCluyse E, Parkinson A.

Drug Metab Dispos. 1999 Mar;27(3):327-35.

PMID:
10064562

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