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Items: 1 to 50 of 65

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.

A quantitative method for detection of circulating fms related tyrosine kinase 3 (FLT-3) in acute myeloid leukemia (AML) patients.

Cook KD, Finger EC, Santos CD, Rock DA.

J Immunol Methods. 2019 Jul;470:55-58. doi: 10.1016/j.jim.2019.04.010. Epub 2019 Apr 26.

PMID:
31034878
3.

Immunoaffinity capture coupled with capillary electrophoresis - mass spectrometry to study therapeutic protein stability in vivo.

Han M, Pearson JT, Wang Y, Winters D, Soto M, Rock DA, Rock BM.

Anal Biochem. 2017 Dec 15;539:118-126. doi: 10.1016/j.ab.2017.10.005. Epub 2017 Oct 10.

PMID:
29029979
4.

In Vitro Metabolism of Oprozomib, an Oral Proteasome Inhibitor: Role of Epoxide Hydrolases and Cytochrome P450s.

Wang Z, Fang Y, Teague J, Wong H, Morisseau C, Hammock BD, Rock DA, Wang Z.

Drug Metab Dispos. 2017 Jul;45(7):712-720. doi: 10.1124/dmd.117.075226. Epub 2017 Apr 20.

5.

Immuno-affinity Capture Followed by TMPP N-Terminus Tagging to Study Catabolism of Therapeutic Proteins.

Kullolli M, Rock DA, Ma J.

J Proteome Res. 2017 Feb 3;16(2):911-919. doi: 10.1021/acs.jproteome.6b00863. Epub 2016 Nov 30.

PMID:
28152598
6.

Reagent-free LC-MS/MS-based pharmacokinetic quantification of polyhistidine-tagged therapeutic proteins.

Shi J, Wong JM, Ma J, Dickerson T, Hall C, Rock DA, Carlson TJ.

Bioanalysis. 2017 Feb;9(3):251-264. doi: 10.4155/bio-2016-0126. Epub 2017 Jan 18.

PMID:
28097886
7.

SRM-based measurements of proprotein convertase subtilisin/kexin type 9 and lipoprotein(a) kinetics in nonhuman primate serum.

Xie F, Emery MG, Gibbs JP, Rock DA, Rock BM.

Bioanalysis. 2016 Dec;8(24):2551-2563.

PMID:
27884075
8.

Altering Antibody-Drug Conjugate Binding to the Neonatal Fc Receptor Impacts Efficacy and Tolerability.

Hamblett KJ, Le T, Rock BM, Rock DA, Siu S, Huard JN, Conner KP, Milburn RR, O'Neill JW, Tometsko ME, Fanslow WC.

Mol Pharm. 2016 Jul 5;13(7):2387-96. doi: 10.1021/acs.molpharmaceut.6b00153. Epub 2016 Jun 13.

PMID:
27248573
9.

Intact mass analysis of monoclonal antibodies by capillary electrophoresis-Mass spectrometry.

Han M, Rock BM, Pearson JT, Rock DA.

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Feb 1;1011:24-32. doi: 10.1016/j.jchromb.2015.12.045. Epub 2015 Dec 28.

PMID:
26751590
10.

Current Approaches for Absorption, Distribution, Metabolism, and Excretion Characterization of Antibody-Drug Conjugates: An Industry White Paper.

Kraynov E, Kamath AV, Walles M, Tarcsa E, Deslandes A, Iyer RA, Datta-Mannan A, Sriraman P, Bairlein M, Yang JJ, Barfield M, Xiao G, Escandon E, Wang W, Rock DA, Chemuturi NV, Moore DJ.

Drug Metab Dispos. 2016 May;44(5):617-23. doi: 10.1124/dmd.115.068049. Epub 2015 Dec 15. Review.

PMID:
26669328
11.

SLC46A3 Is Required to Transport Catabolites of Noncleavable Antibody Maytansine Conjugates from the Lysosome to the Cytoplasm.

Hamblett KJ, Jacob AP, Gurgel JL, Tometsko ME, Rock BM, Patel SK, Milburn RR, Siu S, Ragan SP, Rock DA, Borths CJ, O'Neill JW, Chang WS, Weidner MF, Bio MM, Quon KC, Fanslow WC.

Cancer Res. 2015 Dec 15;75(24):5329-40. doi: 10.1158/0008-5472.CAN-15-1610. Epub 2015 Dec 2.

12.

Bioanalytical approaches to assess the proteolytic stability of therapeutic fusion proteins.

Pearson JT, Rock DA.

Bioanalysis. 2015 Dec;7(23):3035-51. doi: 10.4155/bio.15.217. Epub 2015 Nov 30. Review.

PMID:
26617274
13.

Intracellular Catabolism of an Antibody Drug Conjugate with a Noncleavable Linker.

Rock BM, Tometsko ME, Patel SK, Hamblett KJ, Fanslow WC, Rock DA.

Drug Metab Dispos. 2015 Sep;43(9):1341-4. doi: 10.1124/dmd.115.064253. Epub 2015 Jun 22.

PMID:
26101225
14.

"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
15.

Characterization of ritonavir-mediated inactivation of cytochrome P450 3A4.

Rock BM, Hengel SM, Rock DA, Wienkers LC, Kunze KL.

Mol Pharmacol. 2014 Dec;86(6):665-74. doi: 10.1124/mol.114.094862. Epub 2014 Oct 1.

PMID:
25274602
16.

Evaluation of near infrared fluorescent labeling of monoclonal antibodies as a tool for tissue distribution.

Conner KP, Rock BM, Kwon GK, Balthasar JP, Abuqayyas L, Wienkers LC, Rock DA.

Drug Metab Dispos. 2014 Nov;42(11):1906-13. doi: 10.1124/dmd.114.060319. Epub 2014 Sep 10. Erratum in: Drug Metab Dispos. 2015 Jan;43(1):53.

PMID:
25209366
17.

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
18.

Absolute quantification of aldehyde oxidase protein in human liver using liquid chromatography-tandem mass spectrometry.

Barr JT, Jones JP, Joswig-Jones CA, Rock DA.

Mol Pharm. 2013 Oct 7;10(10):3842-9. doi: 10.1021/mp4003046. Epub 2013 Sep 19.

19.

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
20.

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
21.

In vitro characterization of the drug-drug interaction potential of catabolites of antibody-maytansinoid conjugates.

Davis JA, Rock DA, Wienkers LC, Pearson JT.

Drug Metab Dispos. 2012 Oct;40(10):1927-34. doi: 10.1124/dmd.112.046169. Epub 2012 Jun 29.

PMID:
22752008
22.

Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.

Henne KR, Tran TB, VandenBrink BM, Rock DA, Aidasani DK, Subramanian R, Mason AK, Stresser DM, Teffera Y, Wong SG, Johnson MG, Chen X, Tonn GR, Wong BK.

Drug Metab Dispos. 2012 Jul;40(7):1429-40. doi: 10.1124/dmd.112.045708. Epub 2012 Apr 19.

PMID:
22517972
23.

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
24.

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
25.

Small molecule quantification by liquid chromatography-mass spectrometry for metabolites of drugs and drug candidates.

Dahal UP, Jones JP, Davis JA, Rock DA.

Drug Metab Dispos. 2011 Dec;39(12):2355-60. doi: 10.1124/dmd.111.040865. Epub 2011 Sep 21.

26.

Formation of raloxifene homo-dimer in CYP3A4, evidence for multi-substrate binding in a single catalytically competent P450 active site.

Davis JA, Greene RJ, Han S, Rock DA, Wienkers LC.

Arch Biochem Biophys. 2011 Sep 15;513(2):110-8. doi: 10.1016/j.abb.2011.06.016. Epub 2011 Jul 13.

PMID:
21767526
27.

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
28.

Effects of interleukin-6 (IL-6) and an anti-IL-6 monoclonal antibody on drug-metabolizing enzymes in human hepatocyte culture.

Dickmann LJ, Patel SK, Rock DA, Wienkers LC, Slatter JG.

Drug Metab Dispos. 2011 Aug;39(8):1415-22. doi: 10.1124/dmd.111.038679. Epub 2011 May 9.

PMID:
21555507
29.

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
30.

The effects of type II binding on metabolic stability and binding affinity in cytochrome P450 CYP3A4.

Peng CC, Pearson JT, Rock DA, Joswig-Jones CA, Jones JP.

Arch Biochem Biophys. 2010 May;497(1-2):68-81. doi: 10.1016/j.abb.2010.03.011. Epub 2010 Mar 25.

31.

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
32.

In vitro modulation of cytochrome P450 reductase supported indoleamine 2,3-dioxygenase activity by allosteric effectors cytochrome b(5) and methylene blue.

Pearson JT, Siu S, Meininger DP, Wienkers LC, Rock DA.

Biochemistry. 2010 Mar 30;49(12):2647-56. doi: 10.1021/bi100022c.

PMID:
20178337
33.

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
34.

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
35.

Assessment of the metabolism and intrinsic reactivity of a novel catechol metabolite.

Hutzler JM, Melton RJ, Rumsey JM, Thompson DC, Rock DA, Wienkers LC.

Chem Res Toxicol. 2008 May;21(5):1125-33. doi: 10.1021/tx700429v. Epub 2008 Apr 12.

PMID:
18407675
36.

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
37.

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
38.

Time-dependent inactivation of P450 3A4 by raloxifene: identification of Cys239 as the site of apoprotein alkylation.

Baer BR, Wienkers LC, Rock DA.

Chem Res Toxicol. 2007 Jun;20(6):954-64. Epub 2007 May 12.

PMID:
17497897
39.

Formation of the active species of cytochrome p450 by using iodosylbenzene: a case for spin-selective reactivity.

Cho KB, Moreau Y, Kumar D, Rock DA, Jones JP, Shaik S.

Chemistry. 2007;13(14):4103-15.

PMID:
17367100
40.

Advances in predicting CYP-mediated drug interactions in the drug discovery setting.

Wahlstrom JL, Rock DA, Slatter JG, Wienkers LC.

Expert Opin Drug Discov. 2006 Dec;1(7):677-91. doi: 10.1517/17460441.1.7.677.

PMID:
23495993
41.

CYP2C9 inhibition: impact of probe selection and pharmacogenetics on in vitro inhibition profiles.

Kumar V, Wahlstrom JL, Rock DA, Warren CJ, Gorman LA, Tracy TS.

Drug Metab Dispos. 2006 Dec;34(12):1966-75. Epub 2006 Sep 8.

PMID:
16963489
42.

Enzyme source effects on CYP2C9 kinetics and inhibition.

Kumar V, Rock DA, Warren CJ, Tracy TS, Wahlstrom JL.

Drug Metab Dispos. 2006 Nov;34(11):1903-8. Epub 2006 Aug 23.

43.

Influence of fluorescent probe size and cytochrome b5 on drug-drug interactions in CYP2C9.

Hummel MA, Tracy TS, Hutzler JM, Wahlstrom JL, Zhou Y, Rock DA.

J Biomol Screen. 2006 Apr;11(3):303-9. Epub 2006 Feb 20.

PMID:
16490777
44.

Assessment issues in the testing of children at school entry.

Rock DA, Stenner AJ.

Future Child. 2005 Spring;15(1):15-34.

PMID:
16130539
45.

CYP2C9 genotype-dependent effects on in vitro drug-drug interactions: switching of benzbromarone effect from inhibition to activation in the CYP2C9.3 variant.

Hummel MA, Locuson CW, Gannett PM, Rock DA, Mosher CM, Rettie AE, Tracy TS.

Mol Pharmacol. 2005 Sep;68(3):644-51. Epub 2005 Jun 13.

PMID:
15955872
46.

Active-site characteristics of CYP2C19 and CYP2C9 probed with hydantoin and barbiturate inhibitors.

Suzuki H, Kneller MB, Rock DA, Jones JP, Trager WF, Rettie AE.

Arch Biochem Biophys. 2004 Sep 1;429(1):1-15.

PMID:
15288804
47.

Kinetic isotope effects implicate the iron-oxene as the sole oxidant in P450-catalyzed N-dealkylation.

Dowers TS, Rock DA, Rock DA, Jones JP.

J Am Chem Soc. 2004 Jul 28;126(29):8868-9.

PMID:
15264797
48.

Quantitative binding models for CYP2C9 based on benzbromarone analogues.

Locuson CW 2nd, Rock DA, Jones JP.

Biochemistry. 2004 Jun 8;43(22):6948-58.

PMID:
15170332
49.

An analysis of the regioselectivity of aromatic hydroxylation and N-oxygenation by cytochrome P450 enzymes.

Dowers TS, Rock DA, Rock DA, Perkins BN, Jones JP.

Drug Metab Dispos. 2004 Mar;32(3):328-32.

PMID:
14977867
50.

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