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Items: 36

1.

Correction to Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.

Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

J Med Chem. 2019 Feb 28;62(4):2213. doi: 10.1021/acs.jmedchem.9b00202. Epub 2019 Feb 8. No abstract available.

PMID:
30734560
2.

Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.

Yeung KS, Beno BR, Mosure K, Zhu J, Grant-Young KA, Parcella K, Anjanappa P, Bora RO, Selvakumar K, Wang YK, Fang H, Krause R, Rigat K, Liu M, Lemm J, Sheriff S, Witmer M, Tredup J, Jardel A, Kish K, Parker D, Haskell R, Santone K, Meanwell NA, Soars MG, Roberts SB, Kadow JF.

ACS Med Chem Lett. 2018 Nov 5;9(12):1217-1222. doi: 10.1021/acsmedchemlett.8b00379. eCollection 2018 Dec 13.

PMID:
30613329
3.

Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.

Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

J Med Chem. 2019 Jan 24;62(2):831-856. doi: 10.1021/acs.jmedchem.8b01550. Epub 2019 Jan 8. Erratum in: J Med Chem. 2019 Feb 28;62(4):2213.

PMID:
30576602
4.

Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.

Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C.

Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9.

PMID:
28818462
5.

Improving Metabolic Stability with Deuterium: The Discovery of BMT-052, a Pan-genotypic HCV NS5B Polymerase Inhibitor.

Parcella K, Eastman K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Liu M, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF.

ACS Med Chem Lett. 2017 Jun 29;8(7):771-774. doi: 10.1021/acsmedchemlett.7b00211. eCollection 2017 Jul 13.

6.

Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.

Yeung KS, Beno BR, Parcella K, Bender JA, Grant-Young KA, Nickel A, Gunaga P, Anjanappa P, Bora RO, Selvakumar K, Rigat K, Wang YK, Liu M, Lemm J, Mosure K, Sheriff S, Wan C, Witmer M, Kish K, Hanumegowda U, Zhuo X, Shu YZ, Parker D, Haskell R, Ng A, Gao Q, Colston E, Raybon J, Grasela DM, Santone K, Gao M, Meanwell NA, Sinz M, Soars MG, Knipe JO, Roberts SB, Kadow JF.

J Med Chem. 2017 May 25;60(10):4369-4385. doi: 10.1021/acs.jmedchem.7b00328. Epub 2017 May 4.

PMID:
28430437
7.

Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.

Wu YJ, Guernon J, Shi J, Ditta J, Robbins KJ, Rajamani R, Easton A, Newton A, Bourin C, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C.

J Med Chem. 2017 Mar 23;60(6):2513-2525. doi: 10.1021/acs.jmedchem.6b01918. Epub 2017 Mar 10.

PMID:
28234467
8.

The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase.

Eastman KJ, Parcella K, Yeung KS, Grant-Young KA, Zhu J, Wang T, Zhang Z, Yin Z, Beno BR, Sheriff S, Kish K, Tredup J, Jardel AG, Halan V, Ghosh K, Parker D, Mosure K, Fang H, Wang YK, Lemm J, Zhuo X, Hanumegowda U, Rigat K, Donoso M, Tuttle M, Zvyaga T, Haarhoff Z, Meanwell NA, Soars MG, Roberts SB, Kadow JF.

Medchemcomm. 2017 Feb 8;8(4):796-806. doi: 10.1039/c6md00636a. eCollection 2017 Apr 1.

9.

Development of a high-throughput mass spectrometry based analytical method to support an in vitro OATP1B1 inhibition screening assay.

Wagner AD, Elkin L, Mosure K, Gallagher L, Stavola LK, Soars MG, Shou W.

Rapid Commun Mass Spectrom. 2016 Aug 15;30(15):1787-96. doi: 10.1002/rcm.7655.

PMID:
27426455
10.

Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

Engers DW, Blobaum AL, Gogliotti RD, Cheung YY, Salovich JM, Garcia-Barrantes PM, Daniels JS, Morrison R, Jones CK, Soars MG, Zhuo X, Hurley J, Macor JE, Bronson JJ, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

ACS Chem Neurosci. 2016 Sep 21;7(9):1192-200. doi: 10.1021/acschemneuro.6b00035. Epub 2016 May 3.

11.

Phosphocholine conjugation: an unexpected in vivo conjugation pathway associated with hepatitis c ns5b inhibitors featuring a bicyclo[1.1.1]pentane.

Zhuo X, Cantone JL, Wang Y, Leet JE, Drexler DM, Yeung KS, Huang XS, Eastman KJ, Parcella KE, Mosure KW, Soars MG, Kadow JF, Johnson BM.

Drug Metab Dispos. 2016 Aug;44(8):1332-1340. doi: 10.1124/dmd.115.069062. Epub 2016 Mar 9.

PMID:
26961241
12.

Hepatic drug transporters: the journey so far.

Riley RJ, Foley SA, Barton P, Soars MG, Williamson B.

Expert Opin Drug Metab Toxicol. 2016;12(2):201-16. doi: 10.1517/17425255.2016.1132308. Epub 2016 Jan 8. Review.

PMID:
26670591
13.

Preclinical Pharmacokinetics and In Vitro Metabolism of Asunaprevir (BMS-650032), a Potent Hepatitis C Virus NS3 Protease Inhibitor.

Mosure KW, Knipe JO, Browning M, Arora V, Shu YZ, Phillip T, Mcphee F, Scola P, Balakrishnan A, Soars MG, Santone K, Sinz M.

J Pharm Sci. 2015 Sep;104(9):2813-23. doi: 10.1002/jps.24356. Epub 2015 Jan 28.

PMID:
25631585
14.

A systematic evaluation of solubility enhancing excipients to enable the generation of permeability data for poorly soluble compounds in Caco-2 model.

Shah D, Paruchury S, Matta M, Chowan G, Subramanian M, Saxena A, Soars MG, Herbst J, Haskell R, Marathe P, Mandlekar S.

Drug Metab Lett. 2014;8(2):109-18.

PMID:
25429513
15.

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.

PMID:
24855184
16.

Application of an in vitro OAT assay in drug design and optimization of renal clearance.

Soars MG, Barton P, Elkin LL, Mosure KW, Sproston JL, Riley RJ.

Xenobiotica. 2014 Jul;44(7):657-65. doi: 10.3109/00498254.2013.879625. Epub 2014 Jan 13.

PMID:
24417751
17.

Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: mechanistic considerations beyond the direct inhibition of the bile salt export pump.

Rodrigues AD, Lai Y, Cvijic ME, Elkin LL, Zvyaga T, Soars MG.

Drug Metab Dispos. 2014 Apr;42(4):566-74. doi: 10.1124/dmd.113.054205. Epub 2013 Oct 10. Review. Erratum in: Drug Metab Dispos. 2014 Nov;42(11):1978.

PMID:
24115749
18.

Development of novel, 384-well high-throughput assay panels for human drug transporters: drug interaction and safety assessment in support of discovery research.

Tang H, Shen DR, Han YH, Kong Y, Balimane P, Marino A, Gao M, Wu S, Xie D, Soars MG, O'Connell JC, Rodrigues AD, Zhang L, Cvijic ME.

J Biomol Screen. 2013 Oct;18(9):1072-83. doi: 10.1177/1087057113494807.

PMID:
24062352
19.

Dissecting the relative contribution of OATP1B1-mediated uptake of xenobiotics into human hepatocytes using siRNA.

Williamson B, Soars AC, Owen A, White P, Riley RJ, Soars MG.

Xenobiotica. 2013 Oct;43(10):920-31. doi: 10.3109/00498254.2013.776194. Epub 2013 Mar 6.

PMID:
23461378
20.

The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.

Soars MG, Barton P, Ismair M, Jupp R, Riley RJ.

Drug Metab Dispos. 2012 Aug;40(8):1641-8. doi: 10.1124/dmd.111.042382. Epub 2012 May 15.

PMID:
22587986
21.

Late intervention with a myeloperoxidase inhibitor stops progression of experimental chronic obstructive pulmonary disease.

Churg A, Marshall CV, Sin DD, Bolton S, Zhou S, Thain K, Cadogan EB, Maltby J, Soars MG, Mallinder PR, Wright JL.

Am J Respir Crit Care Med. 2012 Jan 1;185(1):34-43. doi: 10.1164/rccm.201103-0468OC.

PMID:
21997333
22.
23.

Use of hepatocytes to assess the contribution of hepatic uptake to clearance in vivo.

Soars MG, Grime K, Sproston JL, Webborn PJ, Riley RJ.

Drug Metab Dispos. 2007 Jun;35(6):859-65. Epub 2007 Mar 7.

PMID:
17344337
24.

The pivotal role of hepatocytes in drug discovery.

Soars MG, McGinnity DF, Grime K, Riley RJ.

Chem Biol Interact. 2007 May 20;168(1):2-15. Epub 2006 Nov 18. Review.

PMID:
17208208
25.

Comparative analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5.

Soars MG, Grime K, Riley RJ.

Xenobiotica. 2006 Apr;36(4):287-99.

PMID:
16684709
26.

Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance.

McGinnity DF, Soars MG, Urbanowicz RA, Riley RJ.

Drug Metab Dispos. 2004 Nov;32(11):1247-53. Epub 2004 Jul 30.

PMID:
15286053
27.

An assessment of udp-glucuronosyltransferase induction using primary human hepatocytes.

Soars MG, Petullo DM, Eckstein JA, Kasper SC, Wrighton SA.

Drug Metab Dispos. 2004 Jan;32(1):140-8.

PMID:
14709631
28.

The effect of incubation conditions on the enzyme kinetics of udp-glucuronosyltransferases.

Soars MG, Ring BJ, Wrighton SA.

Drug Metab Dispos. 2003 Jun;31(6):762-7.

PMID:
12756209
29.

Cloning and characterisation of the first drug-metabolising canine UDP-glucuronosyltransferase of the 2B subfamily.

Soars MG, Fettes M, O'Sullivan AC, Riley RJ, Ethell BT, Burchell B.

Biochem Pharmacol. 2003 Apr 15;65(8):1251-9.

PMID:
12694866
30.

Biosynthesis of drug glucuronides for use as authentic standards.

Soars MG, Mattiuz EL, Jackson DA, Kulanthaivel P, Ehlhardt WJ, Wrighton SA.

J Pharmacol Toxicol Methods. 2002 May-Jun;47(3):161-8.

PMID:
12628307
31.
32.

Tissue-specific regulation of canine intestinal and hepatic phenol and morphine UDP-glucuronosyltransferases by beta-naphthoflavone in comparison with humans.

Bock KW, Bock-Hennig BS, Münzel PA, Brandenburg JO, Köhle CT, Soars MG, Riley RJ, Burchell B, von Richter O, Eichelbaum MF, Swedmark S, Orzechowski A.

Biochem Pharmacol. 2002 May 1;63(9):1683-90.

PMID:
12007571
33.

In vitro analysis of human drug glucuronidation and prediction of in vivo metabolic clearance.

Soars MG, Burchell B, Riley RJ.

J Pharmacol Exp Ther. 2002 Apr;301(1):382-90.

PMID:
11907196
34.

Evaluation of the marmoset as a model species for drug glucuronidation.

Soars MG, Riley RJ, Burchell B.

Xenobiotica. 2001 Dec;31(12):849-60.

PMID:
11780760
35.

Cloning and characterization of a canine UDP-glucuronosyltransferase.

Soars MG, Smith DJ, Riley RJ, Burchell B.

Arch Biochem Biophys. 2001 Jul 15;391(2):218-24.

PMID:
11437353
36.

Evidence for significant differences in microsomal drug glucuronidation by canine and human liver and kidney.

Soars MG, Riley RJ, Findlay KA, Coffey MJ, Burchell B.

Drug Metab Dispos. 2001 Feb;29(2):121-6.

PMID:
11159800

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