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Items: 41

1.

Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.

Bryan MC, Drobnick J, Gobbi A, Kolesnikov A, Chen Y, Rajapaksa N, Ndubaku C, Feng J, Chang W, Francis R, Yu C, Choo EF, DeMent K, Ran Y, An L, Emson C, Huang Z, Sujatha-Bhaskar S, Brightbill H, DiPasquale A, Maher J, Wai J, McKenzie BS, Lupardus PJ, Zarrin AA, Kiefer JR.

J Med Chem. 2019 Jul 11;62(13):6223-6240. doi: 10.1021/acs.jmedchem.9b00439. Epub 2019 May 24.

PMID:
31082230
2.

Assessment of OATP transporter-mediated drug-drug interaction using physiologically-based pharmacokinetic (PBPK) modeling - a case example.

Chen Y, Zhu R, Ma F, Mao J, Chen EC, Choo EF, Sahasranaman S, Liu L.

Biopharm Drug Dispos. 2018 Nov;39(9):420-430. doi: 10.1002/bdd.2159. Epub 2018 Nov 20.

PMID:
30335192
3.

Leveraging Humanized Animal Models to Understand Human Drug Disposition: Opportunities, Challenges, and Future Directions.

Choo EF, Salphati L.

Clin Pharmacol Ther. 2018 Feb;103(2):188-192. doi: 10.1002/cpt.908. Epub 2017 Nov 28.

PMID:
29193027
4.

Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.

Lai KW, Romero FA, Tsui V, Beresini MH, de Leon Boenig G, Bronner SM, Chen K, Chen Z, Choo EF, Crawford TD, Cyr P, Kaufman S, Li Y, Liao J, Liu W, Ly J, Murray J, Shen W, Wai J, Wang F, Zhu C, Zhu X, Magnuson S.

Bioorg Med Chem Lett. 2018 Jan 1;28(1):15-23. doi: 10.1016/j.bmcl.2017.11.025. Epub 2017 Nov 14.

PMID:
29169673
5.

A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.

Bronner SM, Murray J, Romero FA, Lai KW, Tsui V, Cyr P, Beresini MH, de Leon Boenig G, Chen Z, Choo EF, Clark KR, Crawford TD, Jayaram H, Kaufman S, Li R, Li Y, Liao J, Liang X, Liu W, Ly J, Maher J, Wai J, Wang F, Zheng A, Zhu X, Magnuson S.

J Med Chem. 2017 Dec 28;60(24):10151-10171. doi: 10.1021/acs.jmedchem.7b01372. Epub 2017 Dec 11.

PMID:
29155580
6.

GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).

Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, Crawford TD, Cyr P, de Almeida Nagata D, Gascoigne KE, Grogan JL, Hatzivassiliou G, Huang W, Hunsaker TL, Kaufman S, Koenig SG, Li R, Li Y, Liang X, Liao J, Liu W, Ly J, Maher J, Masui C, Merchant M, Ran Y, Taylor AM, Wai J, Wang F, Wei X, Yu D, Zhu BY, Zhu X, Magnuson S.

J Med Chem. 2017 Nov 22;60(22):9162-9183. doi: 10.1021/acs.jmedchem.7b00796. Epub 2017 Sep 21.

PMID:
28892380
7.

Utility of CYP3A4 and PXR-CAR-CYP3A4/3A7 Transgenic Mouse Models To Assess the Magnitude of CYP3A4 Mediated Drug-Drug Interactions.

Ly JQ, Messick K, Qin A, Takahashi RH, Choo EF.

Mol Pharm. 2017 May 1;14(5):1754-1759. doi: 10.1021/acs.molpharmaceut.7b00006. Epub 2017 Apr 7.

PMID:
28345929
8.

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.

Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S.

J Med Chem. 2016 Dec 8;59(23):10549-10563. Epub 2016 Sep 28.

PMID:
27682507
9.

Absorption, metabolism and excretion of cobimetinib, an oral MEK inhibitor, in rats and dogs.

Takahashi RH, Ma S, Yue Q, Kim-Kang H, Yi Y, Ly J, Boggs JW, Fettes A, McClory A, Deng Y, Hop CE, Khojasteh SC, Choo EF.

Xenobiotica. 2017 Jan;47(1):50-65. doi: 10.3109/00498254.2016.1157645. Epub 2016 Apr 8.

PMID:
27055783
10.

Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans.

Takahashi RH, Choo EF, Ma S, Wong S, Halladay J, Deng Y, Rooney I, Gates M, Hop CE, Khojasteh SC, Dresser MJ, Musib L.

Drug Metab Dispos. 2016 Jan;44(1):28-39. doi: 10.1124/dmd.115.066282. Epub 2015 Oct 8.

PMID:
26451002
11.

Elucidating the Mechanisms of Formation for Two Unusual Cytochrome P450-Mediated Fused Ring Metabolites of GDC-0623, a MAPK/ERK Kinase Inhibitor.

Takahashi RH, Ma S, Robinson SJ, Yue Q, Choo EF, Khojasteh SC.

Drug Metab Dispos. 2015 Dec;43(12):1929-33. doi: 10.1124/dmd.115.067181. Epub 2015 Oct 5.

PMID:
26438627
12.

Use of transgenic mouse models to understand the oral disposition and drug-drug interaction potential of cobimetinib, a MEK inhibitor.

Choo EF, Woolsey S, DeMent K, Ly J, Messick K, Qin A, Takahashi R.

Drug Metab Dispos. 2015 Jun;43(6):864-9. doi: 10.1124/dmd.115.063743. Epub 2015 Mar 26.

PMID:
25813936
13.

Role of P-glycoprotein on the brain penetration and brain pharmacodynamic activity of the MEK inhibitor cobimetinib.

Choo EF, Ly J, Chan J, Shahidi-Latham SK, Messick K, Plise E, Quiason CM, Yang L.

Mol Pharm. 2014 Nov 3;11(11):4199-207. doi: 10.1021/mp500435s. Epub 2014 Oct 3.

PMID:
25243894
14.

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P, Burton B, Choo EF, Pang J, Boggs J, Yang A, Yang X, Baumgardner M.

Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723. doi: 10.1016/j.bmcl.2014.08.008. Epub 2014 Aug 15.

PMID:
25193232
15.

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G.

ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12.

16.

Assessment of the hepatic CYP reductase null mouse model and its potential application in drug discovery.

Boggs JW, Hop CE, McNamara E, Deng Y, Messick K, West K, Choo EF.

Mol Pharm. 2014 Mar 3;11(3):1062-8. doi: 10.1021/mp400556x. Epub 2014 Jan 29.

PMID:
24450768
17.

The role of lymphatic transport on the systemic bioavailability of the Bcl-2 protein family inhibitors navitoclax (ABT-263) and ABT-199.

Choo EF, Boggs J, Zhu C, Lubach JW, Catron ND, Jenkins G, Souers AJ, Voorman R.

Drug Metab Dispos. 2014 Feb;42(2):207-12. doi: 10.1124/dmd.113.055053. Epub 2013 Nov 8.

PMID:
24212376
18.

Systemic in vitro and in vivo evaluation for determining the feasibility of making an amorphous solid dispersion of a B-Raf (rapidly accelerated fibrosarcoma) inhibitor.

Cui Y, Chiang PC, Choo EF, Boggs J, Rudolph J, Grina J, Wenglowsky S, Ran Y.

Int J Pharm. 2013 Sep 15;454(1):241-8. doi: 10.1016/j.ijpharm.2013.06.064. Epub 2013 Jul 5.

PMID:
23834830
19.

Determination of clinically therapeutic endoxifen concentrations based on efficacy from human MCF7 breast cancer xenografts.

Gong IY, Teft WA, Ly J, Chen YH, Alicke B, Kim RB, Choo EF.

Breast Cancer Res Treat. 2013 May;139(1):61-9. doi: 10.1007/s10549-013-2530-1. Epub 2013 Apr 19.

PMID:
23605084
20.

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
21.

PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts.

Choo EF, Ng CM, Berry L, Belvin M, Lewin-Koh N, Merchant M, Salphati L.

Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. doi: 10.1007/s00280-012-1988-6. Epub 2012 Oct 7.

PMID:
23053270
22.

Antitumor activity of targeted and cytotoxic agents in murine subcutaneous tumor models correlates with clinical response.

Wong H, Choo EF, Alicke B, Ding X, La H, McNamara E, Theil FP, Tibbitts J, Friedman LS, Hop CE, Gould SE.

Clin Cancer Res. 2012 Jul 15;18(14):3846-55. doi: 10.1158/1078-0432.CCR-12-0738. Epub 2012 May 30.

23.

Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.

Wong H, Vernillet L, Peterson A, Ware JA, Lee L, Martini JF, Yu P, Li C, Del Rosario G, Choo EF, Hoeflich KP, Shi Y, Aftab BT, Aoyama R, Lam ST, Belvin M, Prescott J.

Clin Cancer Res. 2012 Jun 1;18(11):3090-9. doi: 10.1158/1078-0432.CCR-12-0445. Epub 2012 Apr 10.

24.

Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.

Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J.

J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29.

PMID:
22335519
25.

Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.

Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH.

Drug Metab Dispos. 2012 May;40(5):919-27. doi: 10.1124/dmd.111.043778. Epub 2012 Feb 7.

PMID:
22315332
26.

Preclinical assessment of novel BRAF inhibitors: integrating pharmacokinetic-pharmacodynamic modelling in the drug discovery process.

Choo EF, Alicke B, Boggs J, Dinkel V, Gould S, Grina J, West K, Menghrajani K, Ran Y, Rudolph J, Wenglowsky S.

Xenobiotica. 2011 Dec;41(12):1076-87. doi: 10.3109/00498254.2011.603384. Epub 2011 Aug 25.

PMID:
21864203
27.

Overview of SLC22A and SLCO families of drug uptake transporters in the context of cancer treatments.

Cutler MJ, Choo EF.

Curr Drug Metab. 2011 Oct;12(8):793-807. Review.

PMID:
21787263
28.

Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Wenglowsky S, Ren L, Ahrendt KA, Laird ER, Aliagas I, Alicke B, Buckmelter AJ, Choo EF, Dinkel V, Feng B, Gloor SL, Gould SE, Gross S, Gunzner-Toste J, Hansen JD, Hatzivassiliou G, Liu B, Malesky K, Mathieu S, Newhouse B, Raddatz NJ, Ran Y, Rana S, Randolph N, Risom T, Rudolph J, Savage S, Selby LT, Shrag M, Song K, Sturgis HL, Voegtli WC, Wen Z, Willis BS, Woessner RD, Wu WI, Young WB, Grina J.

ACS Med Chem Lett. 2011 Mar 8;2(5):342-7. doi: 10.1021/ml200025q. eCollection 2011 May 12.

29.

Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor.

Choo EF, Belvin M, Chan J, Hoeflich K, Orr C, Robarge K, Yang X, Zak M, Boggs J.

Xenobiotica. 2010 Nov;40(11):751-62. doi: 10.3109/00498254.2010.514365.

PMID:
20836753
30.

Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species.

Choo EF, Driscoll JP, Feng J, Liederer B, Plise E, Randolph N, Shin Y, Wong S, Ran Y.

Xenobiotica. 2009 Sep;39(9):700-9. doi: 10.1080/00498250902991827.

PMID:
19552528
32.

Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human.

Kalgutkar AS, Feng B, Nguyen HT, Frederick KS, Campbell SD, Hatch HL, Bi YA, Kazolias DC, Davidson RE, Mireles RJ, Duignan DB, Choo EF, Zhao SX.

Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8.

PMID:
17686907
33.
34.

Differential in vivo sensitivity to inhibition of P-glycoprotein located in lymphocytes, testes, and the blood-brain barrier.

Choo EF, Kurnik D, Muszkat M, Ohkubo T, Shay SD, Higginbotham JN, Glaeser H, Kim RB, Wood AJ, Wilkinson GR.

J Pharmacol Exp Ther. 2006 Jun;317(3):1012-8. Epub 2006 Mar 14.

PMID:
16537797
35.

Disposition of cisapride appears to be influenced by P-glycoprotein in the mouse.

Choo EF, Venkatakrishnan K, Hatch HL, Rahematpura S.

Clin Pharmacol Ther. 2005 Mar;77(3):225-6. No abstract available.

PMID:
15735616
36.

Single plasma concentrations of 1'-hydroxymidazolam or the ratio of 1'-hydroxymidazolam:midazolam do not predict midazolam clearance in healthy subjects.

Rogers JF, Nafziger AN, Kashuba AD, Streetman DS, Rocci ML Jr, Choo EF, Wilkinson GR, Bertino JS Jr.

J Clin Pharmacol. 2002 Oct;42(10):1079-82.

PMID:
12362920
37.

Identification of functionally variant MDR1 alleles among European Americans and African Americans.

Kim RB, Leake BF, Choo EF, Dresser GK, Kubba SV, Schwarz UI, Taylor A, Xie HG, McKinsey J, Zhou S, Lan LB, Schuetz JD, Schuetz EG, Wilkinson GR.

Clin Pharmacol Ther. 2001 Aug;70(2):189-99.

PMID:
11503014
38.

In vivo inhibition of human CYP1A2 activity by oltipraz.

Sofowora GG, Choo EF, Mayo G, Shyr Y, Wilkinson GR.

Cancer Chemother Pharmacol. 2001 Jun;47(6):505-10.

PMID:
11459203
39.

Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.

Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, Kim RB.

Drug Metab Dispos. 2000 Jun;28(6):655-60.

PMID:
10820137
40.

Effect of cirrhosis on sulphation by the isolated perfused rat liver.

Choo EF, Angus PW, Morgan DJ.

J Hepatol. 1999 Mar;30(3):498-502.

PMID:
10190735
41.

Increased sensitivity of propranolol clearance to reduced oxygen delivery in the isolated perfused cirrhotic rat liver.

Hickey PL, McLean AJ, Angus PW, Choo EF, Morgan DJ.

Gastroenterology. 1996 Oct;111(4):1039-48.

PMID:
8831600

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