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Items: 35

1.

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.

Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2294-2301. doi: 10.1016/j.bmcl.2019.06.021. Epub 2019 Jun 26.

PMID:
31307887
2.

Targeting the PI3K/Akt/mTOR-pathway with the pan-Akt inhibitor GDC-0068 in PIK3CA-mutant breast cancer brain metastases.

Ippen FM, Grosch JK, Subramanian M, Kuter BM, Liederer BM, Plise EG, Mora JL, Nayyar N, Schmidt SP, Giobbie-Hurder A, Martinez-Lage M, Carter SL, Cahill DP, Wakimoto H, Brastianos PK.

Neuro Oncol. 2019 Jun 7. pii: noz105. doi: 10.1093/neuonc/noz105. [Epub ahead of print]

PMID:
31173106
3.

An Integrated Analysis of Solid Form Change Impact on Solubility and Permeability: Case Study of Oral Exposure in Rats of an RAR Related Orphan Receptor C Inhibitor.

Chiang PC, Nagapudi K, Liu J, Crawford JJ, Zbieg JR, Plise E, Deng Y.

J Pharm Sci. 2019 Jul;108(7):2256-2263. doi: 10.1016/j.xphs.2019.01.031. Epub 2019 Feb 7.

PMID:
30738851
4.

Evaluating the Utility of Canine Mdr1 Knockout Madin-Darby Canine Kidney I Cells in Permeability Screening and Efflux Substrate Determination.

Chen EC, Broccatelli F, Plise E, Chen B, Liu L, Cheong J, Zhang S, Jorski J, Gaffney K, Umemoto KK, Salphati L.

Mol Pharm. 2018 Nov 5;15(11):5103-5113. doi: 10.1021/acs.molpharmaceut.8b00688. Epub 2018 Oct 10.

PMID:
30222362
5.

The Effects of Drug Metabolizing Enzyme Inhibitors on Hepatic Efflux and Uptake Transporters.

Cheong J, Halladay JS, Plise E, Sodhi JK, Salphati L.

Drug Metab Lett. 2017;11(2):111-118. doi: 10.2174/1872312811666171010101248.

PMID:
29032766
6.

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.

7.

Predicting Passive Permeability of Drug-like Molecules from Chemical Structure: Where Are We?

Broccatelli F, Salphati L, Plise E, Cheong J, Gobbi A, Lee ML, Aliagas I.

Mol Pharm. 2016 Dec 5;13(12):4199-4208. Epub 2016 Nov 11.

PMID:
27806577
8.

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma.

Salphati L, Alicke B, Heffron TP, Shahidi-Latham S, Nishimura M, Cao T, Carano RA, Cheong J, Greve J, Koeppen H, Lau S, Lee LB, Nannini-Pepe M, Pang J, Plise EG, Quiason C, Rangell L, Zhang X, Gould SE, Phillips HS, Olivero AG.

Drug Metab Dispos. 2016 Dec;44(12):1881-1889. Epub 2016 Sep 16.

PMID:
27638506
9.

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Heffron TP, Ndubaku CO, Salphati L, Alicke B, Cheong J, Drobnick J, Edgar K, Gould SE, Lee LB, Lesnick JD, Lewis C, Nonomiya J, Pang J, Plise EG, Sideris S, Wallin J, Wang L, Zhang X, Olivero AG.

ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. doi: 10.1021/acsmedchemlett.6b00005. eCollection 2016 Apr 14.

10.

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
11.

Novel antibody-antibiotic conjugate eliminates intracellular S. aureus.

Lehar SM, Pillow T, Xu M, Staben L, Kajihara KK, Vandlen R, DePalatis L, Raab H, Hazenbos WL, Morisaki JH, Kim J, Park S, Darwish M, Lee BC, Hernandez H, Loyet KM, Lupardus P, Fong R, Yan D, Chalouni C, Luis E, Khalfin Y, Plise E, Cheong J, Lyssikatos JP, Strandh M, Koefoed K, Andersen PS, Flygare JA, Wah Tan M, Brown EJ, Mariathasan S.

Nature. 2015 Nov 19;527(7578):323-8. doi: 10.1038/nature16057. Epub 2015 Nov 4.

PMID:
26536114
12.

Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery.

Fan PW, Song Y, Berezhkovskiy LM, Cheong J, Plise EG, Khojasteh SC.

Future Med Chem. 2014;6(18):1995-2012. doi: 10.4155/fmc.14.141.

PMID:
25531965
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.

Differential effects of Rifampin and Ketoconazole on the blood and liver concentration of atorvastatin in wild-type and Cyp3a and Oatp1a/b knockout mice.

Chang JH, Ly J, Plise E, Zhang X, Messick K, Wright M, Cheong J.

Drug Metab Dispos. 2014 Jun;42(6):1067-73. doi: 10.1124/dmd.114.057968. Epub 2014 Mar 26.

PMID:
24671957
15.

SAHA enhances synaptic function and plasticity in vitro but has limited brain availability in vivo and does not impact cognition.

Hanson JE, La H, Plise E, Chen YH, Ding X, Hanania T, Sabath EV, Alexandrov V, Brunner D, Leahy E, Steiner P, Liu L, Scearce-Levie K, Zhou Q.

PLoS One. 2013 Jul 26;8(7):e69964. doi: 10.1371/journal.pone.0069964. Print 2013.

16.

Evaluating the in vitro inhibition of UGT1A1, OATP1B1, OATP1B3, MRP2, and BSEP in predicting drug-induced hyperbilirubinemia.

Chang JH, Plise E, Cheong J, Ho Q, Lin M.

Mol Pharm. 2013 Aug 5;10(8):3067-75. doi: 10.1021/mp4001348. Epub 2013 Jun 21.

PMID:
23750830
17.

Variability in P-glycoprotein inhibitory potency (IC₅₀) using various in vitro experimental systems: implications for universal digoxin drug-drug interaction risk assessment decision criteria.

Bentz J, O'Connor MP, Bednarczyk D, Coleman J, Lee C, Palm J, Pak YA, Perloff ES, Reyner E, Balimane P, Brännström M, Chu X, Funk C, Guo A, Hanna I, Herédi-Szabó K, Hillgren K, Li L, Hollnack-Pusch E, Jamei M, Lin X, Mason AK, Neuhoff S, Patel A, Podila L, Plise E, Rajaraman G, Salphati L, Sands E, Taub ME, Taur JS, Weitz D, Wortelboer HM, Xia CQ, Xiao G, Yabut J, Yamagata T, Zhang L, Ellens H.

Drug Metab Dispos. 2013 Jul;41(7):1347-66. doi: 10.1124/dmd.112.050500. Epub 2013 Apr 25.

18.

Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier.

Salphati L, Heffron TP, Alicke B, Nishimura M, Barck K, Carano RA, Cheong J, Edgar KA, Greve J, Kharbanda S, Koeppen H, Lau S, Lee LB, Pang J, Plise EG, Pokorny JL, Reslan HB, Sarkaria JN, Wallin JJ, Zhang X, Gould SE, Olivero AG, Phillips HS.

Clin Cancer Res. 2012 Nov 15;18(22):6239-48. doi: 10.1158/1078-0432.CCR-12-0720. Epub 2012 Sep 19.

19.

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

Heffron TP, Salphati L, Alicke B, Cheong J, Dotson J, Edgar K, Goldsmith R, Gould SE, Lee LB, Lesnick JD, Lewis C, Ndubaku C, Nonomiya J, Olivero AG, Pang J, Plise EG, Sideris S, Trapp S, Wallin J, Wang L, Zhang X.

J Med Chem. 2012 Sep 27;55(18):8007-20. Epub 2012 Sep 11.

PMID:
22946614
20.

Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human.

Salphati L, Pang J, Plise EG, Lee LB, Olivero AG, Prior WW, Sampath D, Wong S, Zhang X.

Drug Metab Dispos. 2012 Sep;40(9):1785-96. doi: 10.1124/dmd.112.046052. Epub 2012 Jun 13.

PMID:
22696419
21.

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ.

J Med Chem. 2012 May 10;55(9):4101-13. doi: 10.1021/jm300060k. Epub 2012 Mar 28.

22.

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
23.

Antibody-mediated inhibition of fibroblast growth factor 19 results in increased bile acids synthesis and ileal malabsorption of bile acids in cynomolgus monkeys.

Pai R, French D, Ma N, Hotzel K, Plise E, Salphati L, Setchell KD, Ware J, Lauriault V, Schutt L, Hartley D, Dambach D.

Toxicol Sci. 2012 Apr;126(2):446-56. doi: 10.1093/toxsci/kfs011. Epub 2012 Jan 19.

PMID:
22268002
24.

A whole cell assay to measure caspase-6 activity by detecting cleavage of lamin A/C.

Mintzer R, Ramaswamy S, Shah K, Hannoush RN, Pozniak CD, Cohen F, Zhao X, Plise E, Lewcock JW, Heise CE.

PLoS One. 2012;7(1):e30376. doi: 10.1371/journal.pone.0030376. Epub 2012 Jan 12.

25.

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
26.

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human.

Salphati L, Pang J, Plise EG, Chou B, Halladay JS, Olivero AG, Rudewicz PJ, Tian Q, Wong S, Zhang X.

Xenobiotica. 2011 Dec;41(12):1088-99. doi: 10.3109/00498254.2011.603384. Epub 2011 Aug 13.

PMID:
21838594
27.

Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449).

Giannetti AM, Wong H, Dijkgraaf GJ, Dueber EC, Ortwine DF, Bravo BJ, Gould SE, Plise EG, Lum BL, Malhi V, Graham RA.

J Med Chem. 2011 Apr 28;54(8):2592-601. doi: 10.1021/jm1008924. Epub 2011 Mar 25.

PMID:
21438527
28.
29.

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.

Castanedo GM, Wang S, Robarge KD, Blackwood E, Burdick D, Chang C, Dijkgraaf GJ, Gould S, Gunzner J, Guichert O, Halladay J, Khojasteh C, Lee L, Marsters JC Jr, Murray L, Peterson D, Plise E, Salphati L, de Sauvage FJ, Wong S, Sutherlin DP.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6748-53. doi: 10.1016/j.bmcl.2010.08.134. Epub 2010 Sep 15.

PMID:
20875741
30.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

Staben ST, Heffron TP, Sutherlin DP, Bhat SR, Castanedo GM, Chuckowree IS, Dotson J, Folkes AJ, Friedman LS, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Olivero AG, Plise E, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Tsui V, Wan NC, Wang S, Weismann C, Wu P, Zhu BY.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6048-51. doi: 10.1016/j.bmcl.2010.08.067. Epub 2010 Aug 19.

PMID:
20822905
31.

Semi-automated protein binding methodology using equilibrium dialysis and a novel mixed-matrix cassette approach.

Plise EG, Tran D, Salphati L.

J Pharm Sci. 2010 Dec;99(12):5070-8. doi: 10.1002/jps.22188.

PMID:
20821380
32.

Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

Salphati L, Lee LB, Pang J, Plise EG, Zhang X.

Drug Metab Dispos. 2010 Sep;38(9):1422-6. doi: 10.1124/dmd.110.034256. Epub 2010 Jun 3.

PMID:
20522663
33.

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor.

Wong H, Chen JZ, Chou B, Halladay JS, Kenny JR, La H, Marsters JC Jr, Plise E, Rudewicz PJ, Robarge K, Shin Y, Wong S, Zhang C, Khojasteh SC.

Xenobiotica. 2009 Nov;39(11):850-61. doi: 10.3109/00498250903180289.

PMID:
19845436
34.

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
35.

Expression and activity of the efflux transporters ABCB1, ABCC2 and ABCG2 in the human colorectal carcinoma cell line LS513.

Salphati L, Plise EG, Li G.

Eur J Pharm Sci. 2009 Jun 28;37(3-4):463-8. doi: 10.1016/j.ejps.2009.04.001. Epub 2009 Apr 9.

PMID:
19491037

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