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Items: 46

1.

The effect of fluconazole on oral methadone in dogs.

KuKanich B, KuKanich K, Rankin D, Locuson CW.

Vet Anaesth Analg. 2019 Jul;46(4):501-509. doi: 10.1016/j.vaa.2019.02.003. Epub 2019 Feb 19.

PMID:
30982709
2.

A Two-Step Immunocapture LC/MS/MS Assay for Plasma Stability and Payload Migration Assessment of Cysteine-Maleimide-Based Antibody Drug Conjugates.

Dong L, Li C, Locuson C, Chen S, Qian MG.

Anal Chem. 2018 May 15;90(10):5989-5994. doi: 10.1021/acs.analchem.8b00694. Epub 2018 Apr 24.

PMID:
29688004
3.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead CJ, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neill JC, Zhan X, Niswender CM, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126. Epub 2018 Apr 26.

4.

Comparison of predicted intrinsic hepatic clearance of 30 pharmaceuticals in canine and feline liver microsomes.

Visser M, Zaya MJ, Locuson CW, Boothe DM, Merritt DA.

Xenobiotica. 2019 Feb;49(2):177-186. doi: 10.1080/00498254.2018.1437933. Epub 2018 Mar 6.

PMID:
29405805
5.

Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound.

Bertron JL, Ennis EA, Tarr CJ, Wright J, Dickerson JW, Locuson CW, Blobaum AL, Rook JM, Blakely RD, Lindsley CW.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4637-4640. doi: 10.1016/j.bmcl.2016.08.062. Epub 2016 Aug 21.

PMID:
27575469
6.

Subcutaneous meloxicam suspension pharmacokinetics in mice and dose considerations for postoperative analgesia.

Chen PH, Boyd KL, Fickle EK, Locuson CW.

J Vet Pharmacol Ther. 2016 Aug;39(4):356-62. doi: 10.1111/jvp.12297. Epub 2016 Feb 20.

PMID:
26896236
7.

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.

Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA.

J Med Chem. 2015 Nov 25;58(22):9027-40. doi: 10.1021/acs.jmedchem.5b01371. Epub 2015 Nov 11.

8.

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.

Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW.

J Med Chem. 2015 Oct 22;58(20):7959-71. doi: 10.1021/acs.jmedchem.5b00727. Epub 2015 Oct 8.

9.

A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo.

Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS.

Drug Metab Dispos. 2015 Nov;43(11):1718-26. doi: 10.1124/dmd.115.064006. Epub 2015 Aug 11.

10.

Evaluation of tizanidine as a marker of canine CYP1A2 activity.

Locuson CW, Williams P, Adcock JM, Daniels JS.

J Vet Pharmacol Ther. 2016 Apr;39(2):122-30. doi: 10.1111/jvp.12256. Epub 2015 Jul 30.

PMID:
26228837
11.

Role for the M1 Muscarinic Acetylcholine Receptor in Top-Down Cognitive Processing Using a Touchscreen Visual Discrimination Task in Mice.

Gould RW, Dencker D, Grannan M, Bubser M, Zhan X, Wess J, Xiang Z, Locuson C, Lindsley CW, Conn PJ, Jones CK.

ACS Chem Neurosci. 2015 Oct 21;6(10):1683-95. doi: 10.1021/acschemneuro.5b00123. Epub 2015 Aug 5.

12.

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility.

Senter T, Gogliotti RD, Han C, Locuson CW, Morrison R, Daniels JS, Cierpicki T, Grembecka J, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2015 Jul 1;25(13):2720-5. doi: 10.1016/j.bmcl.2015.04.026. Epub 2015 Apr 25.

PMID:
25987377
13.

VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.

Lepesheva GI, Hargrove TY, Rachakonda G, Wawrzak Z, Pomel S, Cojean S, Nde PN, Nes WD, Locuson CW, Calcutt MW, Waterman MR, Daniels JS, Loiseau PM, Villalta F.

J Infect Dis. 2015 Nov 1;212(9):1439-48. doi: 10.1093/infdis/jiv228. Epub 2015 Apr 15.

14.

Progress towards small molecule inhibitors of the Menin-Mixed Lineage Leukemia (MLL) interaction with in vivo utility.

Senter T, Gogliotti R, Han C, Locuson CW II, Morrison R, Daniels JS, Cierpicki T, Grembecka J, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Apr 15 [updated 2015 Feb 11].

15.

Discovery and characterization of ML398, a potent and selective chiral morpholine based antagonist of the dopamine 4 (D4) receptor.

Berry CB, Locuson CW, Daniels JS, Lindsley CW, Hopkins CR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2014 Apr 15 [updated 2015 Jan 16].

16.

Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter.

Bollinger SR, Engers DW, Ennis EA, Wright J, Locuson CW, Lindsley CW, Blakely RD, Hopkins CR.

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1757-1760. doi: 10.1016/j.bmcl.2015.02.058. Epub 2015 Feb 28.

17.

Characterization of bovine phenol sulfotransferases: evidence of a major role for SULT1B1 in the liver.

Choughule KV, Locuson CW, Coughtrie MW.

Xenobiotica. 2015;45(6):495-502. doi: 10.3109/00498254.2014.997325. Epub 2014 Dec 24.

PMID:
25539458
18.

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW.

J Med Chem. 2014 Dec 11;57(23):10192-7. doi: 10.1021/jm501375c. Epub 2014 Dec 2.

19.

Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.

Berry CB, Bubser M, Jones CK, Hayes JP, Wepy JA, Locuson CW, Daniels JS, Lindsley CW, Hopkins CR.

ACS Med Chem Lett. 2014 Jul 9;5(9):1060-4. doi: 10.1021/ml500267c. eCollection 2014 Sep 11.

20.

Discovery of a highly selective PLD2 inhibitor (ML395): a new probe with improved physiochemical properties and broad-spectrum antiviral activity against influenza strains.

O'Reilly MC, Oguin TH 3rd, Scott SA, Thomas PG, Locuson CW, Morrison RD, Daniels JS, Brown HA, Lindsley CW.

ChemMedChem. 2014 Dec;9(12):2633-7. doi: 10.1002/cmdc.201402333. Epub 2014 Sep 10.

21.

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

Wen W, Young SE, Duvernay MT, Schulte ML, Nance KD, Melancon BJ, Engers J, Locuson CW 2nd, Wood MR, Daniels JS, Wu W, Lindsley CW, Hamm HE, Stauffer SR.

Bioorg Med Chem Lett. 2014 Oct 1;24(19):4708-4713. doi: 10.1016/j.bmcl.2014.08.021. Epub 2014 Aug 15.

22.

Challenges in exploring the cytochrome P450 system as a source of variation in canine drug pharmacokinetics.

Martinez MN, Antonovic L, Court M, Dacasto M, Fink-Gremmels J, Kukanich B, Locuson C, Mealey K, Myers MJ, Trepanier L.

Drug Metab Rev. 2013 May;45(2):218-30. doi: 10.3109/03602532.2013.765445. Epub 2013 Feb 25. Review.

PMID:
23432217
23.

A non-acidic sulfaphenazole analog demonstrating high intrinsic clearance and selectivity by canine CYP2C21.

Locuson CW, Alfaro JF, Zaya MJ, Billen D, White JA, Jones JP.

Drug Metab Lett. 2011 Dec;5(4):253-8.

PMID:
22423626
24.

Pharmacokinetic interaction of the antiparasitic agents ivermectin and spinosad in dogs.

Dunn ST, Hedges L, Sampson KE, Lai Y, Mahabir S, Balogh L, Locuson CW.

Drug Metab Dispos. 2011 May;39(5):789-95. doi: 10.1124/dmd.110.034827. Epub 2011 Feb 14.

PMID:
21321059
25.

Distribution, metabolism, and excretion of toceranib phosphate (Palladia, SU11654), a novel tyrosine kinase inhibitor, in dogs.

Yancey MF, Merritt DA, White JA, Marsh SA, Locuson CW.

J Vet Pharmacol Ther. 2010 Apr;33(2):154-61. doi: 10.1111/j.1365-2885.2009.01120.x.

PMID:
20444040
26.

Canine CYP2B11 metabolizes and is inhibited by anesthetic agents often co-administered in dogs.

Baratta MT, Zaya MJ, White JA, Locuson CW.

J Vet Pharmacol Ther. 2010 Feb;33(1):50-5. doi: 10.1111/j.1365-2885.2009.01101.x.

PMID:
20444025
27.

Current cytochrome P450 phenotyping methods applied to metabolic drug-drug interaction prediction in dogs.

Mills BM, Zaya MJ, Walters RR, Feenstra KL, White JA, Gagne J, Locuson CW.

Drug Metab Dispos. 2010 Mar;38(3):396-404. doi: 10.1124/dmd.109.030429. Epub 2009 Dec 9.

PMID:
20007294
28.

CYP2D6-CYP2C9 protein-protein interactions and isoform-selective effects on substrate binding and catalysis.

Subramanian M, Low M, Locuson CW, Tracy TS.

Drug Metab Dispos. 2009 Aug;37(8):1682-9. doi: 10.1124/dmd.109.026500. Epub 2009 May 15.

29.

Evaluation of Escherichia coli membrane preparations of canine CYP1A1, 2B11, 2C21, 2C41, 2D15, 3A12, and 3A26 with coexpressed canine cytochrome P450 reductase.

Locuson CW, Ethell BT, Voice M, Lee D, Feenstra KL.

Drug Metab Dispos. 2009 Mar;37(3):457-61. doi: 10.1124/dmd.108.025312. Epub 2008 Dec 12.

PMID:
19074522
30.

In vitro drug-drug interaction screens for canine veterinary medicines: evaluation of cytochrome P450 reversible inhibition.

Aidasani D, Zaya MJ, Malpas PB, Locuson CW.

Drug Metab Dispos. 2008 Aug;36(8):1512-8. doi: 10.1124/dmd.108.021196. Epub 2008 Apr 30.

PMID:
18448570
31.

Polymorphic variants of CYP2C9: mechanisms involved in reduced catalytic activity.

Wei L, Locuson CW, Tracy TS.

Mol Pharmacol. 2007 Nov;72(5):1280-8. Epub 2007 Aug 8.

PMID:
17686967
32.
33.

CYP2C9 protein interactions with cytochrome b(5): effects on the coupling of catalysis.

Locuson CW, Wienkers LC, Jones JP, Tracy TS.

Drug Metab Dispos. 2007 Jul;35(7):1174-81. Epub 2007 Apr 19.

34.

Use of simple docking methods to screen a virtual library for heteroactivators of cytochrome P450 2C9.

Locuson CW, Gannett PM, Ayscue R, Tracy TS.

J Med Chem. 2007 Mar 22;50(6):1158-65. Epub 2007 Feb 21.

35.

Visible spectra of type II cytochrome P450-drug complexes: evidence that "incomplete" heme coordination is common.

Locuson CW, Hutzler JM, Tracy TS.

Drug Metab Dispos. 2007 Apr;35(4):614-22. Epub 2007 Jan 24.

PMID:
17251307
36.

Inhibition of cytochrome P450 3A4 by a pyrimidineimidazole: Evidence for complex heme interactions.

Hutzler JM, Melton RJ, Rumsey JM, Schnute ME, Locuson CW, Wienkers LC.

Chem Res Toxicol. 2006 Dec;19(12):1650-9.

PMID:
17173379
37.

Identification of binding sites of non-I-helix water molecules in mammalian cytochromes p450.

Locuson CW, Tracy TS.

Drug Metab Dispos. 2006 Dec;34(12):1954-7. Epub 2006 Sep 6.

PMID:
16956955
38.

Amiodarone analog-dependent effects on CYP2C9-mediated metabolism and kinetic profiles.

Kumar V, Locuson CW, Sham YY, Tracy TS.

Drug Metab Dispos. 2006 Oct;34(10):1688-96. Epub 2006 Jun 30.

PMID:
16815961
39.

Preparation, characterization, and substrate metabolism of gold-immobilized cytochrome P450 2C9.

Gannett PM, Kabulski J, Perez FA, Liu Z, Lederman D, Locuson CW, Ayscue RR, Thomsen NM, Tracy TS.

J Am Chem Soc. 2006 Jul 5;128(26):8374-5.

40.

Heteroactivator effects on the coupling and spin state equilibrium of CYP2C9.

Locuson CW, Gannett PM, Tracy TS.

Arch Biochem Biophys. 2006 May 15;449(1-2):115-29. Epub 2006 Mar 2.

PMID:
16545770
41.

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
42.
43.

Charge and substituent effects on affinity and metabolism of benzbromarone-based CYP2C19 inhibitors.

Locuson CW 2nd, Suzuki H, Rettie AE, Jones JP.

J Med Chem. 2004 Dec 30;47(27):6768-76.

PMID:
15615526
44.

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
45.

Differential roles of Arg97, Asp293, and Arg108 in enzyme stability and substrate specificity of CYP2C9.

Dickmann LJ, Locuson CW, Jones JP, Rettie AE.

Mol Pharmacol. 2004 Apr;65(4):842-50.

PMID:
15044613
46.

A new class of CYP2C9 inhibitors: probing 2C9 specificity with high-affinity benzbromarone derivatives.

Locuson CW 2nd, Wahlstrom JL, Rock DA, Rock DA, Jones JP.

Drug Metab Dispos. 2003 Jul;31(7):967-71.

PMID:
12814975

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