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Items: 1 to 50 of 75

1.

A Comparison of Total and Plasma Membrane Abundance of Transporters in Suspended, Plated, Sandwich-Cultured Human Hepatocytes vs. Human Liver Tissue Using Quantitative Targeted Proteomics and Cell-Surface Biotinylation.

Kumar V, Salphati L, Hop CECA, Xiao G, Lai Y, Mathias A, Chu X, Humphreys WG, Liao M, Heyward S, Unadkat JD.

Drug Metab Dispos. 2019 Jan 8. pii: dmd.118.084988. doi: 10.1124/dmd.118.084988. [Epub ahead of print]

PMID:
30622164
2.

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
3.

Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors.

Nayak-Kapoor A, Hao Z, Sadek R, Dobbins R, Marshall L, Vahanian NN, Jay Ramsey W, Kennedy E, Mautino MR, Link CJ, Lin RS, Royer-Joo S, Liang X, Salphati L, Morrissey KM, Mahrus S, McCall B, Pirzkall A, Munn DH, Janik JE, Khleif SN.

J Immunother Cancer. 2018 Jun 20;6(1):61. doi: 10.1186/s40425-018-0351-9.

4.

Abundance of Phase 1 and 2 Drug-Metabolizing Enzymes in Alcoholic and Hepatitis C Cirrhotic Livers: A Quantitative Targeted Proteomics Study.

Prasad B, Bhatt DK, Johnson K, Chapa R, Chu X, Salphati L, Xiao G, Lee C, Hop CECA, Mathias A, Lai Y, Liao M, Humphreys WG, Kumer SC, Unadkat JD.

Drug Metab Dispos. 2018 Jul;46(7):943-952. doi: 10.1124/dmd.118.080523. Epub 2018 Apr 25.

PMID:
29695616
5.

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
6.

Individual serum bile acid profiling in rats aids in human risk assessment of drug-induced liver injury due to BSEP inhibition.

Cepa S, Potter D, Wong L, Schutt L, Tarrant J, Pang J, Zhang X, Andaya R, Salphati L, Ran Y, An L, Morgan R, Maher J.

Toxicol Appl Pharmacol. 2018 Jan 1;338:204-213. doi: 10.1016/j.taap.2017.11.007. Epub 2017 Nov 13.

PMID:
29146462
7.

Transporter Expression in Noncancerous and Cancerous Liver Tissue from Donors with Hepatocellular Carcinoma and Chronic Hepatitis C Infection Quantified by LC-MS/MS Proteomics.

Billington S, Ray AS, Salphati L, Xiao G, Chu X, Humphreys WG, Liao M, Lee CA, Mathias A, Hop CECA, Rowbottom C, Evers R, Lai Y, Kelly EJ, Prasad B, Unadkat JD.

Drug Metab Dispos. 2018 Feb;46(2):189-196. doi: 10.1124/dmd.117.077289. Epub 2017 Nov 14.

PMID:
29138286
8.

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
9.

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.

Safina BS, Elliott RL, Forrest AK, Heald RA, Murray JM, Nonomiya J, Pang J, Salphati L, Seward EM, Staben ST, Ultsch M, Wei B, Yang W, Sutherlin DP.

ACS Med Chem Lett. 2017 Aug 25;8(9):936-940. doi: 10.1021/acsmedchemlett.7b00170. eCollection 2017 Sep 14.

10.

Combining "Bottom-up" and "Top-down" Approaches to Assess the Impact of Food and Gastric pH on Pictilisib (GDC-0941) Pharmacokinetics.

Lu T, Fraczkiewicz G, Salphati L, Budha N, Dalziel G, Smelick GS, Morrissey KM, Davis JD, Jin JY, Ware JA.

CPT Pharmacometrics Syst Pharmacol. 2017 Nov;6(11):747-755. doi: 10.1002/psp4.12228. Epub 2017 Oct 17.

11.

An Investigation of Oral Exposure Variability and Formulation Strategy: A Case Study of PI3Kδ Inhibitor and Physiologically Based Pharmacokinetic Modeling in Beagle Dogs.

Chiang PC, Pang J, Liu J, Salphati L.

J Pharm Sci. 2018 Jan;107(1):466-475. doi: 10.1016/j.xphs.2017.06.014. Epub 2017 Jun 23.

PMID:
28652157
12.

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors.

Juric D, Krop I, Ramanathan RK, Wilson TR, Ware JA, Sanabria Bohorquez SM, Savage HM, Sampath D, Salphati L, Lin RS, Jin H, Parmar H, Hsu JY, Von Hoff DD, Baselga J.

Cancer Discov. 2017 Jul;7(7):704-715. doi: 10.1158/2159-8290.CD-16-1080. Epub 2017 Mar 22. Erratum in: Cancer Discov. 2018 Nov;8(11):1491.

13.

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
14.

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.

15.

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, Labadie SS, Lai KW, Liu W, Liu Y, Li C, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhang H, Zhou A.

ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. eCollection 2016 Oct 13.

16.

Transporter Expression in Liver Tissue from Subjects with Alcoholic or Hepatitis C Cirrhosis Quantified by Targeted Quantitative Proteomics.

Wang L, Collins C, Kelly EJ, Chu X, Ray AS, Salphati L, Xiao G, Lee C, Lai Y, Liao M, Mathias A, Evers R, Humphreys W, Hop CE, Kumer SC, Unadkat JD.

Drug Metab Dispos. 2016 Nov;44(11):1752-1758. Epub 2016 Aug 19.

17.

Impact of Blood-Brain Barrier Integrity on Tumor Growth and Therapy Response in Brain Metastases.

Osswald M, Blaes J, Liao Y, Solecki G, Gömmel M, Berghoff AS, Salphati L, Wallin JJ, Phillips HS, Wick W, Winkler F.

Clin Cancer Res. 2016 Dec 15;22(24):6078-6087. Epub 2016 Aug 12.

19.

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.

Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, Lai T, Li Y, Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S, Hatzivassiliou G, Sampath D, Evangelista M, O'Brien T.

Nat Chem Biol. 2016 Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1.

PMID:
27479743
20.

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L, Ramaswamy S, Salphati L, Schmidt S, Schneider EV, Wu J, Beresini M.

ACS Med Chem Lett. 2016 Apr 5;7(6):595-600. doi: 10.1021/acsmedchemlett.6b00044. eCollection 2016 Jun 9.

21.

Ontogeny of Hepatic Drug Transporters as Quantified by LC-MS/MS Proteomics.

Prasad B, Gaedigk A, Vrana M, Gaedigk R, Leeder JS, Salphati L, Chu X, Xiao G, Hop C, Evers R, Gan L, Unadkat JD.

Clin Pharmacol Ther. 2016 Oct;100(4):362-70. doi: 10.1002/cpt.409. Epub 2016 Aug 13.

22.

Investigation of Dose-Dependent Factors Limiting Oral Bioavailability: Case Study With the PI3K-δ Inhibitor.

Chiang PC, Sutherlin D, Pang J, Salphati L.

J Pharm Sci. 2016 Jun;105(6):1802-1809. doi: 10.1016/j.xphs.2016.04.003.

PMID:
27238480
23.

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.

24.

Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Koehler MF, Bergeron P, Blackwood EM, Bowman K, Clark KR, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L, Salphati L, Schmidt S, Schneider EV, Wu J, Beresini MH.

ACS Med Chem Lett. 2016 Jan 6;7(3):223-8. doi: 10.1021/acsmedchemlett.5b00278. eCollection 2016 Mar 10.

25.

Generation and Characterization of a Breast Cancer Resistance Protein Humanized Mouse Model.

Dallas S, Salphati L, Gomez-Zepeda D, Wanek T, Chen L, Chu X, Kunta J, Mezler M, Menet MC, Chasseigneaux S, Declèves X, Langer O, Pierre E, DiLoreto K, Hoft C, Laplanche L, Pang J, Pereira T, Andonian C, Simic D, Rode A, Yabut J, Zhang X, Scheer N.

Mol Pharmacol. 2016 May;89(5):492-504. doi: 10.1124/mol.115.102079. Epub 2016 Feb 18.

26.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG.

J Med Chem. 2016 Feb 11;59(3):985-1002. doi: 10.1021/acs.jmedchem.5b01483. Epub 2016 Jan 20.

PMID:
26741947
27.

Strategically Timing Inhibition of Phosphatidylinositol 3-Kinase to Maximize Therapeutic Index in Estrogen Receptor Alpha-Positive, PIK3CA-Mutant Breast Cancer.

Yang W, Hosford SR, Dillon LM, Shee K, Liu SC, Bean JR, Salphati L, Pang J, Zhang X, Nannini MA, Demidenko E, Bates D, Lewis LD, Marotti JD, Eastman AR, Miller TW.

Clin Cancer Res. 2016 May 1;22(9):2250-60. doi: 10.1158/1078-0432.CCR-15-2276. Epub 2016 Jan 5.

28.

Determination of GDC-0980 (apitolisib), a small molecule dual phosphatidylinositide 3-kinase/mammalian target of rapamycin inhibitor in dog plasma by LC-MS/MS to support a GLP toxicology study.

Ding X, Salphati L, Kim A, Morinello E, Wong L, Pang J, Percey S, Meng M, Reuschel S, Dean B.

Biomed Chromatogr. 2015 Aug;29(8):1274-9. doi: 10.1002/bmc.3417. Epub 2015 Feb 10.

PMID:
25677784
29.

Interspecies variability in expression of hepatobiliary transporters across human, dog, monkey, and rat as determined by quantitative proteomics.

Wang L, Prasad B, Salphati L, Chu X, Gupta A, Hop CE, Evers R, Unadkat JD.

Drug Metab Dispos. 2015 Mar;43(3):367-74. doi: 10.1124/dmd.114.061580. Epub 2014 Dec 22.

30.

Quantitative transporter proteomics by liquid chromatography with tandem mass spectrometry: addressing methodologic issues of plasma membrane isolation and expression-activity relationship.

Kumar V, Prasad B, Patilea G, Gupta A, Salphati L, Evers R, Hop CE, Unadkat JD.

Drug Metab Dispos. 2015 Feb;43(2):284-8. doi: 10.1124/dmd.114.061614. Epub 2014 Dec 8.

31.

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Labadie S, Dragovich PS, Chen J, Fauber BP, Boggs J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Ho Q, Lai KW, Ma S, Malek S, Peterson D, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A.

Bioorg Med Chem Lett. 2015 Jan 1;25(1):75-82. Epub 2014 Nov 10.

PMID:
25466195
32.

The use of betaine HCl to enhance dasatinib absorption in healthy volunteers with rabeprazole-induced hypochlorhydria.

Yago MR, Frymoyer A, Benet LZ, Smelick GS, Frassetto LA, Ding X, Dean B, Salphati L, Budha N, Jin JY, Dresser MJ, Ware JA.

AAPS J. 2014 Nov;16(6):1358-65. doi: 10.1208/s12248-014-9673-9. Epub 2014 Oct 2.

33.

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, Malek S, Peterson D, Pitts KE, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3764-71. doi: 10.1016/j.bmcl.2014.06.076. Epub 2014 Jul 1.

PMID:
25037916
34.

Evaluation of organic anion transporting polypeptide 1B1 and 1B3 humanized mice as a translational model to study the pharmacokinetics of statins.

Salphati L, Chu X, Chen L, Prasad B, Dallas S, Evers R, Mamaril-Fishman D, Geier EG, Kehler J, Kunta J, Mezler M, Laplanche L, Pang J, Rode A, Soars MG, Unadkat JD, van Waterschoot RA, Yabut J, Schinkel AH, Scheer N.

Drug Metab Dispos. 2014 Aug;42(8):1301-13. doi: 10.1124/dmd.114.057976. Epub 2014 May 22.

35.

Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging.

Salphati L, Shahidi-Latham S, Quiason C, Barck K, Nishimura M, Alicke B, Pang J, Carano RA, Olivero AG, Phillips HS.

Drug Metab Dispos. 2014 Jul;42(7):1110-6. doi: 10.1124/dmd.114.057513. Epub 2014 Apr 22.

36.

Interindividual variability in hepatic organic anion-transporting polypeptides and P-glycoprotein (ABCB1) protein expression: quantification by liquid chromatography tandem mass spectroscopy and influence of genotype, age, and sex.

Prasad B, Evers R, Gupta A, Hop CE, Salphati L, Shukla S, Ambudkar SV, Unadkat JD.

Drug Metab Dispos. 2014 Jan;42(1):78-88. doi: 10.1124/dmd.113.053819. Epub 2013 Oct 11.

37.

Impact of food and the proton pump inhibitor rabeprazole on the pharmacokinetics of GDC-0941 in healthy volunteers: bench to bedside investigation of pH-dependent solubility.

Ware JA, Dalziel G, Jin JY, Pellett JD, Smelick GS, West DA, Salphati L, Ding X, Sutton R, Fridyland J, Dresser MJ, Morrisson G, Holden SN.

Mol Pharm. 2013 Nov 4;10(11):4074-81. doi: 10.1021/mp4005595. Epub 2013 Oct 24.

PMID:
24099279
38.

Pharmacokinetics and absorption of the anticancer agents dasatinib and GDC-0941 under various gastric conditions in dogs--reversing the effect of elevated gastric pH with betaine HCl.

Pang J, Dalziel G, Dean B, Ware JA, Salphati L.

Mol Pharm. 2013 Nov 4;10(11):4024-31. doi: 10.1021/mp400356m. Epub 2013 Sep 11.

PMID:
23980865
39.

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Safina BS, Sweeney ZK, Li J, Chan BK, Bisconte A, Carrera D, Castanedo G, Flagella M, Heald R, Lewis C, Murray JM, Nonomiya J, Pang J, Price S, Reif K, Salphati L, Seward EM, Wei B, Sutherlin DP.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4953-9. doi: 10.1016/j.bmcl.2013.06.052. Epub 2013 Jun 29.

40.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG.

J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3.

PMID:
23662903
41.

Application of receiver operating characteristic analysis to refine the prediction of potential digoxin drug interactions.

Ellens H, Deng S, Coleman J, Bentz J, Taub ME, Ragueneau-Majlessi I, Chung SP, Herédi-Szabó K, Neuhoff S, Palm J, Balimane P, Zhang L, Jamei M, Hanna I, O'Connor M, Bednarczyk D, Forsgard M, Chu X, Funk C, Guo A, Hillgren KM, Li L, Pak AY, Perloff ES, Rajaraman G, Salphati L, Taur JS, Weitz D, Wortelboer HM, Xia CQ, Xiao G, Yamagata T, Lee CA.

Drug Metab Dispos. 2013 Jul;41(7):1367-74. doi: 10.1124/dmd.112.050542. Epub 2013 Apr 25.

42.

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.

43.

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.

Staben ST, Ndubaku C, Blaquiere N, Belvin M, Bull RJ, Dudley D, Edgar K, Gray D, Heald R, Heffron TP, Jones GE, Jones M, Kolesnikov A, Lee L, Lesnick J, Lewis C, Murray J, McLean NJ, Nonomiya J, Olivero AG, Ord R, Pang J, Price S, Prior WW, Rouge L, Salphati L, Sampath D, Wallin J, Wang L, Wei B, Weismann C, Wu P.

Bioorg Med Chem Lett. 2013 May 1;23(9):2606-13. doi: 10.1016/j.bmcl.2013.02.102. Epub 2013 Mar 7.

PMID:
23540645
44.

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
45.

Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.

Staben ST, Blaquiere N, Tsui V, Kolesnikov A, Do S, Bradley EK, Dotson J, Goldsmith R, Heffron TP, Lesnick J, Lewis C, Murray J, Nonomiya J, Olivero AG, Pang J, Rouge L, Salphati L, Wei B, Wiesmann C, Wu P.

Bioorg Med Chem Lett. 2013 Feb 1;23(3):897-901. doi: 10.1016/j.bmcl.2012.10.121. Epub 2012 Nov 5.

PMID:
23265894
46.

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
47.

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.

48.

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
49.

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Murray JM, Sweeney ZK, Chan BK, Balazs M, Bradley E, Castanedo G, Chabot C, Chantry D, Flagella M, Goldstein DM, Kondru R, Lesnick J, Li J, Lucas MC, Nonomiya J, Pang J, Price S, Salphati L, Safina B, Savy PP, Seward EM, Ultsch M, Sutherlin DP.

J Med Chem. 2012 Sep 13;55(17):7686-95. doi: 10.1021/jm300717c. Epub 2012 Aug 21.

PMID:
22877085
50.

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.

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