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Items: 42

1.

Use of Subcutaneous and Intraperitoneal Administration Methods to Facilitate Cassette Dosing in Microdialysis Studies in Rats.

Durk MR, Deshmukh G, Valle N, Ding X, Liederer BM, Liu X.

Drug Metab Dispos. 2018 Jul;46(7):964-969. doi: 10.1124/dmd.118.080697. Epub 2018 Apr 26.

PMID:
29700231
2.

Preclinical QSP Modeling in the Pharmaceutical Industry: An IQ Consortium Survey Examining the Current Landscape.

Nijsen MJMA, Wu F, Bansal L, Bradshaw-Pierce E, Chan JR, Liederer BM, Mettetal JT, Schroeder P, Schuck E, Tsai A, Xu C, Chimalakonda A, Le K, Penney M, Topp B, Yamada A, Spilker ME.

CPT Pharmacometrics Syst Pharmacol. 2018 Mar;7(3):135-146. doi: 10.1002/psp4.12282. Epub 2018 Feb 1. Review.

3.

From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.

Liang J, Labadie S, Zhang B, Ortwine DF, Patel S, Vinogradova M, Kiefer JR, Mauer T, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, An L, Ran Y, Classon M, Trojer P, Dragovich PS, Murray L.

Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981. doi: 10.1016/j.bmcl.2017.05.016. Epub 2017 May 5.

PMID:
28512031
4.

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
5.

GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile.

Villemure E, Volgraf M, Jiang Y, Wu G, Ly CQ, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Wang TM, Hanson JE, Hackos DH, Scearce-Levie K, Schwarz JB, Sellers BD.

ACS Med Chem Lett. 2016 Oct 31;8(1):84-89. doi: 10.1021/acsmedchemlett.6b00388. eCollection 2017 Jan 12.

6.

Balancing Blood Sample Volume with 3Rs: Implementation and Best Practices for Small Molecule Toxicokinetic Assessments in Rats.

Harstad E, Andaya R, Couch J, Ding X, Liang X, Liederer BM, Messick K, Nguyen T, Schweiger M, Tarrant J, Zhong S, Dean B.

ILAR J. 2016 Dec;57(2):157-165. doi: 10.1093/ilar/ilw023. Review.

PMID:
28053069
7.

Cardiotoxicity Associated with Nicotinamide Phosphoribosyltransferase Inhibitors in Rodents and in Rat and Human-Derived Cells Lines.

Misner DL, Kauss MA, Singh J, Uppal H, Bruening-Wright A, Liederer BM, Lin T, McCray B, La N, Nguyen T, Sampath D, Dragovich PS, O'Brien T, Zabka TS.

Cardiovasc Toxicol. 2017 Jul;17(3):307-318. doi: 10.1007/s12012-016-9387-6.

PMID:
27783203
8.

Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.

Zak M, Yuen PW, Liu X, Patel S, Sampath D, Oeh J, Liederer BM, Wang W, O'Brien T, Xiao Y, Skelton N, Hua R, Sodhi J, Wang Y, Zhang L, Zhao G, Zheng X, Ho YC, Bair KW, Dragovich PS.

J Med Chem. 2016 Sep 22;59(18):8345-68. doi: 10.1021/acs.jmedchem.6b00697. Epub 2016 Aug 30.

PMID:
27541271
9.

Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.

Labadie SS, Dragovich PS, Cummings RT, Deshmukh G, Gustafson A, Han N, Harmange JC, Kiefer JR, Li Y, Liang J, Liederer BM, Liu Y, Manieri W, Mao W, Murray L, Ortwine DF, Trojer P, VanderPorten E, Vinogradova M, Wen L.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4492-4496. doi: 10.1016/j.bmcl.2016.07.070. Epub 2016 Jul 29.

PMID:
27499454
10.

Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.

Liang J, Zhang B, Labadie S, Ortwine DF, Vinogradova M, Kiefer JR, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, Classon M, Trojer P, Dragovich PS, Murray L.

Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41. doi: 10.1016/j.bmcl.2016.06.078. Epub 2016 Jun 29.

PMID:
27406798
11.

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.

Volgraf M, Sellers BD, Jiang Y, Wu G, Ly CQ, Villemure E, Pastor RM, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Sun L, Fu Y, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Reynen P, Herrington J, Gustafson A, Liu Y, Dirksen A, Dietz MG, Liu Y, Wang TM, Hanson JE, Hackos D, Scearce-Levie K, Schwarz JB.

J Med Chem. 2016 Mar 24;59(6):2760-79. doi: 10.1021/acs.jmedchem.5b02010. Epub 2016 Mar 8.

PMID:
26919761
12.

Use of cassette dosing to enhance the throughput of rat brain microdialysis studies.

Deshmukh G, Sun K, Liederer BM, Ding X, Liu X.

Drug Metab Dispos. 2015 Jul;43(7):1123-8. doi: 10.1124/dmd.115.064204. Epub 2015 May 5.

13.

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.

14.

Prediction of drug distribution in subcutaneous xenografts of human tumor cell lines and healthy tissues in mouse: application of the tissue composition-based model to antineoplastic drugs.

Poulin P, Chen YH, Ding X, Gould SE, Hop CE, Messick K, Oeh J, Liederer BM.

J Pharm Sci. 2015 Apr;104(4):1508-21. doi: 10.1002/jps.24336. Epub 2015 Jan 14.

PMID:
25615572
15.

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Zak M, Liederer BM, Sampath D, Yuen PW, Bair KW, Baumeister T, Buckmelter AJ, Clodfelter KH, Cheng E, Crocker L, Fu B, Han B, Li G, Ho YC, Lin J, Liu X, Ly J, O'Brien T, Reynolds DJ, Skelton N, Smith CC, Tay S, Wang W, Wang Z, Xiao Y, Zhang L, Zhao G, Zheng X, Dragovich PS.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):529-41. doi: 10.1016/j.bmcl.2014.12.026. Epub 2014 Dec 17.

PMID:
25556090
16.

Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

Zabka TS, Singh J, Dhawan P, Liederer BM, Oeh J, Kauss MA, Xiao Y, Zak M, Lin T, McCray B, La N, Nguyen T, Beyer J, Farman C, Uppal H, Dragovich PS, O'Brien T, Sampath D, Misner DL.

Toxicol Sci. 2015 Mar;144(1):163-72. doi: 10.1093/toxsci/kfu268. Epub 2014 Dec 11.

PMID:
25505128
17.

Measuring NAD(+) levels in mouse blood and tissue samples via a surrogate matrix approach using LC-MS/MS.

Liang X, Yang L, Qin AR, Ly J, Liederer BM, Messick K, Ma S, Zak M, Dragovich PS, Dean BJ, Hop CE, Deng Y.

Bioanalysis. 2014 Jun;6(11):1445-57. doi: 10.4155/bio.14.8. Erratum in: Bioanalysis. 2014;6(13):1870.

PMID:
25046046
18.

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Giannetti AM, Zheng X, Skelton NJ, Wang W, Bravo BJ, Bair KW, Baumeister T, Cheng E, Crocker L, Feng Y, Gunzner-Toste J, Ho YC, Hua R, Liederer BM, Liu Y, Ma X, O'Brien T, Oeh J, Sampath D, Shen Y, Wang C, Wang L, Wu H, Xiao Y, Yuen PW, Zak M, Zhao G, Zhao Q, Dragovich PS.

J Med Chem. 2014 Feb 13;57(3):770-92. doi: 10.1021/jm4015108. Epub 2014 Jan 22.

PMID:
24405419
19.

Supplementation of nicotinic acid with NAMPT inhibitors results in loss of in vivo efficacy in NAPRT1-deficient tumor models.

O'Brien T, Oeh J, Xiao Y, Liang X, Vanderbilt A, Qin A, Yang L, Lee LB, Ly J, Cosino E, LaCap JA, Ogasawara A, Williams S, Nannini M, Liederer BM, Jackson P, Dragovich PS, Sampath D.

Neoplasia. 2013 Dec;15(12):1314-29.

20.

Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway renders them sensitive to NAMPT inhibition with GNE-618.

Xiao Y, Elkins K, Durieux JK, Lee L, Oeh J, Yang LX, Liang X, DelNagro C, Tremayne J, Kwong M, Liederer BM, Jackson PK, Belmont LD, Sampath D, O'Brien T.

Neoplasia. 2013 Oct;15(10):1151-60.

21.

Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Zheng X, Bair KW, Bauer P, Baumeister T, Bowman KK, Buckmelter AJ, Caligiuri M, Clodfelter KH, Feng Y, Han B, Ho YC, Kley N, Li H, Liang X, Liederer BM, Lin J, Ly J, O'Brien T, Oeh J, Oh A, Reynolds DJ, Sampath D, Sharma G, Skelton N, Smith CC, Tremayne J, Wang L, Wang W, Wang Z, Wu H, Wu J, Xiao Y, Yang G, Yuen PW, Zak M, Dragovich PS.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5488-97. doi: 10.1016/j.bmcl.2013.08.074. Epub 2013 Aug 22.

PMID:
24021463
22.

Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Dragovich PS, Bair KW, Baumeister T, Ho YC, Liederer BM, Liu X, Liu Y, O'Brien T, Oeh J, Sampath D, Skelton N, Wang L, Wang W, Wu H, Xiao Y, Yuen PW, Zak M, Zhang L, Zheng X.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4875-85. doi: 10.1016/j.bmcl.2013.06.090. Epub 2013 Jul 6.

PMID:
23899614
23.

An algorithm for evaluating potential tissue drug distribution in toxicology studies from readily available pharmacokinetic parameters.

Poulin P, Dambach DM, Hartley DH, Ford K, Theil FP, Harstad E, Halladay J, Choo E, Boggs J, Liederer BM, Dean B, Diaz D.

J Pharm Sci. 2013 Oct;102(10):3816-29. doi: 10.1002/jps.23670. Epub 2013 Jul 22.

PMID:
23878104
24.

Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.

Zheng X, Bauer P, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Han B, Ho YC, Kley N, Lin J, Reynolds DJ, Sharma G, Smith CC, Wang Z, Dragovich PS, Gunzner-Toste J, Liederer BM, Ly J, O'Brien T, Oh A, Wang L, Wang W, Xiao Y, Zak M, Zhao G, Yuen PW, Bair KW.

J Med Chem. 2013 Aug 22;56(16):6413-33. doi: 10.1021/jm4008664. Epub 2013 Jul 31.

PMID:
23859118
25.

Comparison of in vitro-in vivo extrapolation of biliary clearance using an empirical scaling factor versus transport-based scaling factors in sandwich-cultured rat hepatocytes.

Zou P, Liu X, Wong S, Feng MR, Liederer BM.

J Pharm Sci. 2013 Aug;102(8):2837-50. doi: 10.1002/jps.23620. Epub 2013 May 27.

26.

Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.

Gunzner-Toste J, Zhao G, Bauer P, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Fu B, Han B, Ho YC, Kley N, Liang X, Liederer BM, Lin J, Mukadam S, O'Brien T, Oh A, Reynolds DJ, Sharma G, Skelton N, Smith CC, Sodhi J, Wang W, Wang Z, Xiao Y, Yuen PW, Zak M, Zhang L, Zheng X, Bair KW, Dragovich PS.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3531-8. doi: 10.1016/j.bmcl.2013.04.040. Epub 2013 Apr 25.

PMID:
23668988
27.

Correlation of tissue-plasma partition coefficients between normal tissues and subcutaneous xenografts of human tumor cell lines in mouse as a prediction tool of drug penetration in tumors.

Poulin P, Hop CE, Salphati L, Liederer BM.

J Pharm Sci. 2013 Apr;102(4):1355-69. doi: 10.1002/jps.23452. Epub 2013 Jan 18.

PMID:
23334959
28.

Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.

Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K.

Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3.

29.

High-throughput liquid chromatography/mass spectrometry method for the quantitation of small molecules using accurate mass technologies in supporting discovery drug screening.

Ding X, Ghobarah H, Zhang X, Jaochico A, Liu X, Deshmukh G, Liederer BM, Hop CE, Dean B.

Rapid Commun Mass Spectrom. 2013 Feb 15;27(3):401-8. doi: 10.1002/rcm.6461.

PMID:
23280971
30.

An alternative approach for quantitative bioanalysis using diluted blood to profile oral exposure of small molecule anticancer drugs in mice.

Liederer BM, Berezhkovskiy LM, Ubhayakar SS, Deng Y.

J Pharm Sci. 2013 Feb;102(2):750-60. doi: 10.1002/jps.23395. Epub 2012 Dec 5.

PMID:
23225118
31.

Pharmacokinetic drivers of toxicity for basic molecules: strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor.

Diaz D, Ford KA, Hartley DP, Harstad EB, Cain GR, Achilles-Poon K, Nguyen T, Peng J, Zheng Z, Merchant M, Sutherlin DP, Gaudino JJ, Kaus R, Lewin-Koh SC, Choo EF, Liederer BM, Dambach DM.

Toxicol Appl Pharmacol. 2013 Jan 1;266(1):86-94. doi: 10.1016/j.taap.2012.10.026. Epub 2012 Nov 7.

PMID:
23142475
32.

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.

PMID:
22934575
33.

Use of the cassette-dosing approach to assess brain penetration in drug discovery.

Liu X, Ding X, Deshmukh G, Liederer BM, Hop CE.

Drug Metab Dispos. 2012 May;40(5):963-9. doi: 10.1124/dmd.111.044420. Epub 2012 Feb 10.

34.

Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors.

Liederer BM, Liu X, Berezhkovskiy LM, Cain G, Ding X, Gaudino J, Kaus R, Plise EG, Sutherlin DP, Harstad EB.

Xenobiotica. 2012 May;42(5):456-65. doi: 10.3109/00498254.2011.632697. Epub 2011 Nov 28.

PMID:
22122353
35.

Evaluation of homogenization techniques for the preparation of mouse tissue samples to support drug discovery.

Liang X, Ubhayakar S, Liederer BM, Dean B, Ran-Ran Qin A, Shahidi-Latham S, Deng Y.

Bioanalysis. 2011 Sep;3(17):1923-33. doi: 10.4155/bio.11.181.

PMID:
21899502
36.
37.

Enzymes involved in the bioconversion of ester-based prodrugs.

Liederer BM, Borchardt RT.

J Pharm Sci. 2006 Jun;95(6):1177-95. Review.

PMID:
16639719
38.

Effects of amino acid chirality and the chemical linker on the cell permeation characteristics of cyclic prodrugs of opioid peptides.

Liederer BM, Fuchs T, Vander Velde D, Siahaan TJ, Borchardt RT.

J Med Chem. 2006 Feb 23;49(4):1261-70.

PMID:
16480263
39.
41.

Preformulation study of epigallocatechin gallate, a promising antioxidant for topical skin cancer prevention.

Proniuk S, Liederer BM, Blanchard J.

J Pharm Sci. 2002 Jan;91(1):111-6.

PMID:
11782902
42.

Topical formulation studies with DEET (N,N-diethyl-3-methylbenzamide) and cyclodextrins.

Proniuk S, Liederer BM, Dixon SE, Rein JA, Kallen MA, Blanchard J.

J Pharm Sci. 2002 Jan;91(1):101-10.

PMID:
11782901

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