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Items: 45

1.

Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species.

Foti RS, Biswas K, Aral J, Be X, Berry L, Cheng Y, Conner K, Falsey JR, Glaus C, Herberich B, Hickman D, Ikotun T, Li H, Long J, Huang L, Miranda LP, Murray J, Moyer B, Netirojjanakul C, Nixey TE, Sham K, Soto M, Tegley CM, Tran L, Wu B, Yin L, Rock DA.

Drug Metab Dispos. 2019 Aug 6. pii: dmd.119.087742. doi: 10.1124/dmd.119.087742. [Epub ahead of print]

2.

Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.

Murray JK, Wu B, Tegley CM, Nixey TE, Falsey JR, Herberich B, Yin L, Sham K, Long J, Aral J, Cheng Y, Netirojjanakul C, Doherty L, Glaus C, Ikotun T, Li H, Tran L, Soto M, Salimi-Moosavi H, Ligutti J, Amagasu S, Andrews KL, Be X, Lin MJ, Foti RS, Ilch CP, Youngblood B, Kornecook TJ, Karow M, Walker KW, Moyer BD, Biswas K, Miranda LP.

ACS Chem Biol. 2019 Apr 19;14(4):806-818. doi: 10.1021/acschembio.9b00183. Epub 2019 Mar 27.

PMID:
30875193
3.

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition.

Boezio AA, Andrews K, Boezio C, Chu-Moyer M, Copeland KW, DiMauro EF, Foti RS, Fremeau RT Jr, Gao H, Geuns-Meyer S, Graceffa RF, Gunaydin H, Huang H, La DS, Ligutti J, Moyer BD, Peterson EA, Yu V, Weiss MM.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2103-2108. doi: 10.1016/j.bmcl.2018.04.035. Epub 2018 Apr 17.

PMID:
29709252
4.

Polymorphic Human Sulfotransferase 2A1 Mediates the Formation of 25-Hydroxyvitamin D3-3-O-Sulfate, a Major Circulating Vitamin D Metabolite in Humans.

Wong T, Wang Z, Chapron BD, Suzuki M, Claw KG, Gao C, Foti RS, Prasad B, Chapron A, Calamia J, Chaudhry A, Schuetz EG, Horst RL, Mao Q, de Boer IH, Thornton TA, Thummel KE.

Drug Metab Dispos. 2018 Apr;46(4):367-379. doi: 10.1124/dmd.117.078428. Epub 2018 Jan 17.

5.

Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors.

Schenkel LB, DiMauro EF, Nguyen HN, Chakka N, Du B, Foti RS, Guzman-Perez A, Jarosh M, La DS, Ligutti J, Milgram BC, Moyer BD, Peterson EA, Roberts J, Yu VL, Weiss MM.

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3817-3824. doi: 10.1016/j.bmcl.2017.06.054. Epub 2017 Jun 26.

PMID:
28684121
6.

Correction to "Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement".

Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Nguyen HN, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM.

ACS Med Chem Lett. 2017 Feb 28;8(3):378. doi: 10.1021/acsmedchemlett.7b00075. eCollection 2017 Mar 9.

7.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.

Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss MM.

J Med Chem. 2017 Jul 27;60(14):5990-6017. doi: 10.1021/acs.jmedchem.6b01850. Epub 2017 Apr 20.

PMID:
28324649
8.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.

Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr.

J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20.

PMID:
28287723
9.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.

Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM.

ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. eCollection 2016 Dec 8. Erratum in: ACS Med Chem Lett. 2017 Feb 28;8(3):378.

10.

Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors.

Sparling BA, Yi S, Able J, Bregman H, DiMauro EF, Foti RS, Gao H, Guzman-Perez A, Huang H, Jarosh M, Kornecook T, Ligutti J, Milgram BC, Moyer BD, Youngblood B, Yu VL, Weiss MM.

Medchemcomm. 2016 Dec 2;8(4):744-754. doi: 10.1039/c6md00578k. eCollection 2017 Apr 1.

11.

Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.

DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Bojic EF, Foti RS, Fremeau R, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, Kornecook T, Lee J, Ligutti J, Liu D, Moyer BD, Ortuno D, Rose PE, Schenkel LB, Taborn K, Wang J, Wang Y, Yu V, Weiss MM.

J Med Chem. 2016 Sep 8;59(17):7818-39. doi: 10.1021/acs.jmedchem.6b00425. Epub 2016 Aug 29.

PMID:
27441383
13.

Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).

Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD.

J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25.

PMID:
27411843
14.

Cytochrome P450 and Non-Cytochrome P450 Oxidative Metabolism: Contributions to the Pharmacokinetics, Safety, and Efficacy of Xenobiotics.

Foti RS, Dalvie DK.

Drug Metab Dispos. 2016 Aug;44(8):1229-45. doi: 10.1124/dmd.116.071753. Epub 2016 Jun 13. Erratum in: Drug Metab Dispos. 2016 Sep;44(9):1516.

PMID:
27298339
15.

Identification of Tazarotenic Acid as the First Xenobiotic Substrate of Human Retinoic Acid Hydroxylase CYP26A1 and CYP26B1.

Foti RS, Isoherranen N, Zelter A, Dickmann LJ, Buttrick BR, Diaz P, Douguet D.

J Pharmacol Exp Ther. 2016 May;357(2):281-92. doi: 10.1124/jpet.116.232637. Epub 2016 Mar 2.

16.

Potent and Selective Inhibition of Plasma Membrane Monoamine Transporter by HIV Protease Inhibitors.

Duan H, Hu T, Foti RS, Pan Y, Swaan PW, Wang J.

Drug Metab Dispos. 2015 Nov;43(11):1773-80. doi: 10.1124/dmd.115.064824. Epub 2015 Aug 18.

17.

"Target-Site" Drug Metabolism and Transport.

Foti RS, Tyndale RF, Garcia KL, Sweet DH, Nagar S, Sharan S, Rock DA.

Drug Metab Dispos. 2015 Aug;43(8):1156-68. doi: 10.1124/dmd.115.064576. Epub 2015 May 18.

PMID:
25986849
18.

Induction of CYP26A1 by metabolites of retinoic acid: evidence that CYP26A1 is an important enzyme in the elimination of active retinoids.

Topletz AR, Tripathy S, Foti RS, Shimshoni JA, Nelson WL, Isoherranen N.

Mol Pharmacol. 2015;87(3):430-41. doi: 10.1124/mol.114.096784. Epub 2014 Dec 9.

19.

Characterization of the active site properties of CYP4F12.

Eksterowicz J, Rock DA, Rock BM, Wienkers LC, Foti RS.

Drug Metab Dispos. 2014 Oct;42(10):1698-707. doi: 10.1124/dmd.114.059626. Epub 2014 Jul 29.

PMID:
25074871
20.

Fluoxetine- and norfluoxetine-mediated complex drug-drug interactions: in vitro to in vivo correlation of effects on CYP2D6, CYP2C19, and CYP3A4.

Sager JE, Lutz JD, Foti RS, Davis C, Kunze KL, Isoherranen N.

Clin Pharmacol Ther. 2014 Jun;95(6):653-62. doi: 10.1038/clpt.2014.50. Epub 2014 Feb 25.

21.

Evaluation of UGT protein interactions in human hepatocytes: effect of siRNA down regulation of UGT1A9 and UGT2B7 on propofol glucuronidation in human hepatocytes.

Konopnicki CM, Dickmann LJ, Tracy JM, Tukey RH, Wienkers LC, Foti RS.

Arch Biochem Biophys. 2013 Jul 15;535(2):143-9. doi: 10.1016/j.abb.2013.03.012. Epub 2013 Apr 4.

22.

Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.

Foti RS, Pearson JT, Wong SL, Zalikowski JA, Boudreaux MD, Prokop SP, Davis JA, Banfield C, Emery MG, Rock DA, Wahlstrom JL, Wienkers LC, Amore BM.

Drug Metab Dispos. 2012 Dec;40(12):2239-49. doi: 10.1124/dmd.112.047928. Epub 2012 Aug 28.

PMID:
22930276
23.

Cytochrome p450 architecture and cysteine nucleophile placement impact raloxifene-mediated mechanism-based inactivation.

VandenBrink BM, Davis JA, Pearson JT, Foti RS, Wienkers LC, Rock DA.

Mol Pharmacol. 2012 Nov;82(5):835-42. doi: 10.1124/mol.112.080739. Epub 2012 Aug 2.

PMID:
22859722
24.

Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19.

Foti RS, Rock DA, Han X, Flowers RA, Wienkers LC, Wahlstrom JL.

J Med Chem. 2012 Feb 9;55(3):1205-14. doi: 10.1021/jm201346g. Epub 2012 Jan 31.

PMID:
22239545
25.

Prediction of CYP2D6 drug interactions from in vitro data: evidence for substrate-dependent inhibition.

VandenBrink BM, Foti RS, Rock DA, Wienkers LC, Wahlstrom JL.

Drug Metab Dispos. 2012 Jan;40(1):47-53. doi: 10.1124/dmd.111.041210. Epub 2011 Oct 5.

PMID:
21976621
26.

Evaluation of CYP2C8 inhibition in vitro: utility of montelukast as a selective CYP2C8 probe substrate.

VandenBrink BM, Foti RS, Rock DA, Wienkers LC, Wahlstrom JL.

Drug Metab Dispos. 2011 Sep;39(9):1546-54. doi: 10.1124/dmd.111.039065. Epub 2011 Jun 22.

PMID:
21697463
27.

Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.

Foti RS, Rock DA, Pearson JT, Wahlstrom JL, Wienkers LC.

Drug Metab Dispos. 2011 Jul;39(7):1188-95. doi: 10.1124/dmd.111.038505. Epub 2011 Mar 29.

PMID:
21447734
28.

Catalytic versus inhibitory promiscuity in cytochrome P450s: implications for evolution of new function.

Foti RS, Honaker M, Nath A, Pearson JT, Buttrick B, Isoherranen N, Atkins WM.

Biochemistry. 2011 Apr 5;50(13):2387-93. doi: 10.1021/bi1020716. Epub 2011 Mar 11.

29.

Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation.

Foti RS, Rock DA, Wienkers LC, Wahlstrom JL.

Drug Metab Dispos. 2010 Jun;38(6):981-7. doi: 10.1124/dmd.110.032094. Epub 2010 Mar 4.

PMID:
20203109
30.

Application of cytochrome P450 drug interaction screening in drug discovery.

Foti RS, Wienkers LC, Wahlstrom JL.

Comb Chem High Throughput Screen. 2010 Feb;13(2):145-58. Review.

PMID:
20053168
31.

In vitro inhibition of multiple cytochrome P450 isoforms by xanthone derivatives from mangosteen extract.

Foti RS, Pearson JT, Rock DA, Wahlstrom JL, Wienkers LC.

Drug Metab Dispos. 2009 Sep;37(9):1848-55. doi: 10.1124/dmd.109.028043. Epub 2009 Jun 18.

PMID:
19541824
32.

Prediction of CYP-mediated drug interactions in vivo using in vitro data.

Foti RS, Wahlstrom JL.

IDrugs. 2008 Dec;11(12):900-5. Review.

PMID:
19051152
33.

The combination of chemical and antibody inhibitors for superior P450 3A inhibition in reaction phenotyping studies.

Rock DA, Foti RS, Pearson JT.

Drug Metab Dispos. 2008 Dec;36(12):2410-3. doi: 10.1124/dmd.108.023572. Epub 2008 Sep 2.

PMID:
18765682
34.

Metabolism and related human risk factors for hepatic damage by usnic acid containing nutritional supplements.

Foti RS, Dickmann LJ, Davis JA, Greene RJ, Hill JJ, Howard ML, Pearson JT, Rock DA, Tay JC, Wahlstrom JL, Slatter JG.

Xenobiotica. 2008 Mar;38(3):264-80. doi: 10.1080/00498250701802514 .

PMID:
18274956
35.

CYP2C19 inhibition: the impact of substrate probe selection on in vitro inhibition profiles.

Foti RS, Wahlstrom JL.

Drug Metab Dispos. 2008 Mar;36(3):523-8. Epub 2007 Nov 29.

PMID:
18048485
36.

Differential time-dependent inactivation of P450 3A4 and P450 3A5 by raloxifene: a key role for C239 in quenching reactive intermediates.

Pearson JT, Wahlstrom JL, Dickmann LJ, Kumar S, Halpert JR, Wienkers LC, Foti RS, Rock DA.

Chem Res Toxicol. 2007 Dec;20(12):1778-86. Epub 2007 Nov 15.

PMID:
18001057
37.

Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.

Brown MF, Bahnck KB, Blumberg LC, Brissette WH, Burrell SA, Driscoll JP, Fedeles F, Fisher MB, Foti RS, Gladue RP, Guzman-Martinez A, Hayward MM, Lira PD, Lillie BM, Lu Y, Lundquist GD, McElroy EB, McGlynn MA, Paradis TJ, Poss CS, Roache JH, Shavnya A, Shepard RM, Trevena KA, Tylaska LA.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3109-12. Epub 2007 Mar 15.

PMID:
17383873
38.

The in vitro drug interaction potential of dietary supplements containing multiple herbal components.

Foti RS, Wahlstrom JL, Wienkers LC.

Drug Metab Dispos. 2007 Feb;35(2):185-8. Epub 2006 Nov 8.

PMID:
17093003
40.

A streamlined method to predict hepatic clearance using human liver microsomes in the presence of human plasma.

Skaggs SM, Foti RS, Fisher MB.

J Pharmacol Toxicol Methods. 2006 May-Jun;53(3):284-90. Epub 2005 Nov 21.

PMID:
16300971
41.

Assessment of UDP-glucuronosyltransferase catalyzed formation of ethyl glucuronide in human liver microsomes and recombinant UGTs.

Foti RS, Fisher MB.

Forensic Sci Int. 2005 Oct 29;153(2-3):109-16. Epub 2005 Jan 15.

PMID:
16139098
43.

Importance of patient selection when determining the significance of the CYP3A5 polymorphism in clinical trials.

Foti RS, Fisher MB.

Pharmacogenomics J. 2004;4(6):362-4. Review. No abstract available.

PMID:
15483658
44.
45.

Flavin-containing monooxygenase activity in hepatocytes and microsomes: in vitro characterization and in vivo scaling of benzydamine clearance.

Fisher MB, Yoon K, Vaughn ML, Strelevitz TJ, Foti RS.

Drug Metab Dispos. 2002 Oct;30(10):1087-93.

PMID:
12228184

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