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Items: 41

1.

Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline.

Thorn CA, Moon J, Bourbonais CA, Harms J, Edgerton JR, Stark E, Steyn SJ, Butler CR, Lazzaro JT, O'Connor RE, Popiolek M.

ACS Chem Neurosci. 2019 Aug 21;10(8):3910. doi: 10.1021/acschemneuro.9b00335. Epub 2019 Jul 9. No abstract available.

PMID:
31286767
2.

Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline.

Thorn CA, Moon J, Bourbonais CA, Harms J, Edgerton JR, Stark E, Steyn SJ, Butter CR, Lazzaro JT, O'Connor RE, Popiolek M.

ACS Chem Neurosci. 2019 Mar 20;10(3):1753-1764. doi: 10.1021/acschemneuro.8b00625. Epub 2018 Dec 11. Erratum in: ACS Chem Neurosci. 2019 Aug 21;10(8):3910.

PMID:
30480428
3.

Lack of Effect of Sodium Benzoate at Reported Clinical Therapeutic Concentration on d-Alanine Metabolism in Dogs.

Popiolek M, Tierney B, Steyn SJ, DeVivo M.

ACS Chem Neurosci. 2018 Nov 21;9(11):2832-2837. doi: 10.1021/acschemneuro.8b00229. Epub 2018 Jun 19.

PMID:
29893546
4.

Design and Synthesis of γ- and δ-Lactam M1 Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M1-Selective PAM with Weak Agonist Activity.

Davoren JE, Garnsey M, Pettersen B, Brodney MA, Edgerton JR, Fortin JP, Grimwood S, Harris AR, Jenkinson S, Kenakin T, Lazzaro JT, Lee CW, Lotarski SM, Nottebaum L, O'Neil SV, Popiolek M, Ramsey S, Steyn SJ, Thorn CA, Zhang L, Webb D.

J Med Chem. 2017 Aug 10;60(15):6649-6663. doi: 10.1021/acs.jmedchem.7b00597. Epub 2017 Jul 26.

PMID:
28598634
5.

Extended Clearance Classification System (ECCS) informed approach for evaluating investigational drugs as substrates of drug transporters.

Varma MV, El-Kattan AF, Feng B, Steyn SJ, Maurer TS, Scott DO, Rodrigues AD, Tremaine LM.

Clin Pharmacol Ther. 2017 Jul;102(1):33-36. doi: 10.1002/cpt.595. Epub 2017 Feb 3. No abstract available.

PMID:
27984654
6.

Inositol Phosphate Accumulation in Vivo Provides a Measure of Muscarinic M1 Receptor Activation.

Popiolek M, Nguyen DP, Reinhart V, Edgerton JR, Harms J, Lotarski SM, Steyn SJ, Davoren JE, Grimwood S.

Biochemistry. 2016 Dec 27;55(51):7073-7085. doi: 10.1021/acs.biochem.6b00688. Epub 2016 Dec 13.

PMID:
27958713
7.

Projecting ADME Behavior and Drug-Drug Interactions in Early Discovery and Development: Application of the Extended Clearance Classification System.

El-Kattan AF, Varma MV, Steyn SJ, Scott DO, Maurer TS, Bergman A.

Pharm Res. 2016 Dec;33(12):3021-3030. Epub 2016 Sep 12.

PMID:
27620173
8.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Pettersson M, Johnson DS, Rankic DA, Kauffman GW, Am Ende CW, Butler TW, Boscoe B, Evrard E, Helal CJ, Humphrey JM, Stepan AF, Stiff CM, Yang E, Xie L, Bales KR, Hajos-Korcsok E, Jenkinson S, Pettersen B, Pustilnik LR, Ramirez DS, Steyn SJ, Wood KM, Verhoest PR.

Medchemcomm. 2016 Nov 2;8(4):730-743. doi: 10.1039/c6md00406g. eCollection 2017 Apr 1.

9.

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.

Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S.

J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1.

PMID:
27275946
10.

Insights From an Integrated Physiologically Based Pharmacokinetic Model for Brain Penetration.

Trapa PE, Belova E, Liras JL, Scott DO, Steyn SJ.

J Pharm Sci. 2016 Feb;105(2):965-971. doi: 10.1016/j.xphs.2015.12.005.

PMID:
26869440
11.

Design and optimization of selective azaindole amide M1 positive allosteric modulators.

Davoren JE, O'Neil SV, Anderson DP, Brodney MA, Chenard L, Dlugolenski K, Edgerton JR, Green M, Garnsey M, Grimwood S, Harris AR, Kauffman GW, LaChapelle E, Lazzaro JT, Lee CW, Lotarski SM, Nason DM, Obach RS, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Yan J, Zhang L.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. doi: 10.1016/j.bmcl.2015.11.053. Epub 2015 Nov 17.

PMID:
26631313
12.

Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS).

Varma MV, Steyn SJ, Allerton C, El-Kattan AF.

Pharm Res. 2015 Dec;32(12):3785-802. doi: 10.1007/s11095-015-1749-4. Epub 2015 Jul 9.

PMID:
26155985
13.

Leucine-rich Repeat Kinase 2 (LRRK2) Pharmacological Inhibition Abates α-Synuclein Gene-induced Neurodegeneration.

Daher JP, Abdelmotilib HA, Hu X, Volpicelli-Daley LA, Moehle MS, Fraser KB, Needle E, Chen Y, Steyn SJ, Galatsis P, Hirst WD, West AB.

J Biol Chem. 2015 Aug 7;290(32):19433-44. doi: 10.1074/jbc.M115.660001. Epub 2015 Jun 15.

14.

Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.

Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14.

15.

Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25.

PMID:
25582600
16.

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

Henderson JL, Kormos BL, Hayward MM, Coffman KJ, Jasti J, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD, Galatsis P.

J Med Chem. 2015 Jan 8;58(1):419-32. doi: 10.1021/jm5014055. Epub 2014 Nov 17.

PMID:
25353650
17.

Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold.

Galatsis P, Henderson JL, Kormos BL, Han S, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4132-40. doi: 10.1016/j.bmcl.2014.07.052. Epub 2014 Jul 30.

PMID:
25113930
18.

Permeability comparison between hepatocyte and low efflux MDCKII cell monolayer.

Li R, Bi YA, Lai Y, Sugano K, Steyn SJ, Trapa PE, Di L.

AAPS J. 2014 Jul;16(4):802-9. doi: 10.1208/s12248-014-9616-5. Epub 2014 May 23.

19.

A perspective on the prediction of drug pharmacokinetics and disposition in drug research and development.

Di L, Feng B, Goosen TC, Lai Y, Steyn SJ, Varma MV, Obach RS.

Drug Metab Dispos. 2013 Dec;41(12):1975-93. doi: 10.1124/dmd.113.054031. Epub 2013 Sep 24.

PMID:
24065860
20.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

McClure KF, Jackson M, Cameron KO, Kung DW, Perry DA, Orr ST, Zhang Y, Kohrt J, Tu M, Gao H, Fernando D, Jones R, Erasga N, Wang G, Polivkova J, Jiao W, Swartz R, Ueno H, Bhattacharya SK, Stock IA, Varma S, Bagdasarian V, Perez S, Kelly-Sullivan D, Wang R, Kong J, Cornelius P, Michael L, Lee E, Janssen A, Steyn SJ, Lapham K, Goosen T.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30.

PMID:
23953189
21.

Biochemical and pharmacological characterization of human c-Met neutralizing monoclonal antibody CE-355621.

Michaud NR, Jani JP, Hillerman S, Tsaparikos KE, Barbacci-Tobin EG, Knauth E, Putz H Jr, Campbell M, Karam GA, Chrunyk B, Gebhard DF, Green LL, Xu JJ, Dunn MC, Coskran TM, Lapointe JM, Cohen BD, Coleman KG, Bedian V, Vincent P, Kajiji S, Steyn SJ, Borzillo GV, Los G.

MAbs. 2012 Nov-Dec;4(6):710-23. doi: 10.4161/mabs.22160. Epub 2012 Sep 24.

22.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Kung DW, Coffey SB, Jones RM, Cabral S, Jiao W, Fichtner M, Carpino PA, Rose CR, Hank RF, Lopaze MG, Swartz R, Chen HT, Hendsch Z, Posner B, Wielis CF, Manning B, Dubins J, Stock IA, Varma S, Campbell M, DeBartola D, Kosa-Maines R, Steyn SJ, McClure KF.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. doi: 10.1016/j.bmcl.2012.05.024. Epub 2012 May 17.

PMID:
22677316
23.

pH-Dependent solubility and permeability criteria for provisional biopharmaceutics classification (BCS and BDDCS) in early drug discovery.

Varma MV, Gardner I, Steyn SJ, Nkansah P, Rotter CJ, Whitney-Pickett C, Zhang H, Di L, Cram M, Fenner KS, El-Kattan AF.

Mol Pharm. 2012 May 7;9(5):1199-212. doi: 10.1021/mp2004912. Epub 2012 Apr 26.

PMID:
22489626
24.

Modulation of NMDA receptor function by inhibition of D-amino acid oxidase in rodent brain.

Strick CA, Li C, Scott L, Harvey B, Hajós M, Steyn SJ, Piotrowski MA, James LC, Downs JT, Rago B, Becker SL, El-Kattan A, Xu Y, Ganong AH, Tingley FD 3rd, Ramirez AD, Seymour PA, Guanowsky V, Majchrzak MJ, Fox CB, Schmidt CJ, Duplantier AJ.

Neuropharmacology. 2011 Oct-Nov;61(5-6):1001-15. doi: 10.1016/j.neuropharm.2011.06.029. Epub 2011 Jul 7.

PMID:
21763704
25.

Strategic use of plasma and microsome binding to exploit in vitro clearance in early drug discovery.

Chang G, Steyn SJ, Umland JP, Scott DO.

ACS Med Chem Lett. 2010 Feb 3;1(2):50-3. doi: 10.1021/ml900012h. eCollection 2010 May 13.

26.

PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy.

Jani JP, Arcari J, Bernardo V, Bhattacharya SK, Briere D, Cohen BD, Coleman K, Christensen JG, Emerson EO, Jakowski A, Hook K, Los G, Moyer JD, Pruimboom-Brees I, Pustilnik L, Rossi AM, Steyn SJ, Su C, Tsaparikos K, Wishka D, Yoon K, Jakubczak JL.

Mol Cancer Ther. 2010 Apr;9(4):883-94. doi: 10.1158/1535-7163.MCT-09-0915. Epub 2010 Mar 30.

27.

Assessment of in silico models for fraction of unbound drug in human liver microsomes.

Gao H, Steyn SJ, Chang G, Lin J.

Expert Opin Drug Metab Toxicol. 2010 May;6(5):533-42. doi: 10.1517/17425251003671022. Review.

PMID:
20233033
28.

Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.

Varma MV, Obach RS, Rotter C, Miller HR, Chang G, Steyn SJ, El-Kattan A, Troutman MD.

J Med Chem. 2010 Feb 11;53(3):1098-108. doi: 10.1021/jm901371v.

PMID:
20070106
29.

Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.

Duplantier AJ, Becker SL, Bohanon MJ, Borzilleri KA, Chrunyk BA, Downs JT, Hu LY, El-Kattan A, James LC, Liu S, Lu J, Maklad N, Mansour MN, Mente S, Piotrowski MA, Sakya SM, Sheehan S, Steyn SJ, Strick CA, Williams VA, Zhang L.

J Med Chem. 2009 Jun 11;52(11):3576-85. doi: 10.1021/jm900128w.

PMID:
19438227
30.

High throughput ADME screening: practical considerations, impact on the portfolio and enabler of in silico ADME models.

Hop CE, Cole MJ, Davidson RE, Duignan DB, Federico J, Janiszewski JS, Jenkins K, Krueger S, Lebowitz R, Liston TE, Mitchell W, Snyder M, Steyn SJ, Soglia JR, Taylor C, Troutman MD, Umland J, West M, Whalen KM, Zelesky V, Zhao SX.

Curr Drug Metab. 2008 Nov;9(9):847-53. Review.

PMID:
18991580
31.

Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor.

Jani JP, Finn RS, Campbell M, Coleman KG, Connell RD, Currier N, Emerson EO, Floyd E, Harriman S, Kath JC, Morris J, Moyer JD, Pustilnik LR, Rafidi K, Ralston S, Rossi AM, Steyn SJ, Wagner L, Winter SM, Bhattacharya SK.

Cancer Res. 2007 Oct 15;67(20):9887-93.

32.

Measurement of mitochondrial respiration in permeabilized murine neuroblastoma (N-2alpha) cells, a simple and rapid in situ assay to investigate mitochondrial toxins.

Steyn SJ, Pieterse DJ, Mienie LJ, Van der Schyf CJ.

J Biochem Biophys Methods. 2005 Jan 31;62(1):25-40. Epub 2004 Sep 23.

PMID:
15656941
33.

Inhibition of human MAO-A and MAO-B by a compound isolated from flue-cured tobacco leaves and its neuroprotective properties in the MPTP mouse model of neurodegeneration.

Castagnoli K, Petzer JB, Steyn SJ, van der Schyf CJ, Castagnoli N Jr.

Inflammopharmacology. 2003;11(2):183-8.

PMID:
15035820
34.

Studies on the interactions of tobacco leaf and tobacco smoke constituents and monoamine oxidase.

Castagnoli K, Steyn SJ, Magnin G, Van Der Schyf CJ, Fourie I, Khalil A, Castagnoli N Jr.

Neurotox Res. 2002 Mar;4(2):151-60.

PMID:
12829416
35.
36.

The effects of age, sex, and shoulder dominance on range of motion of the shoulder.

Barnes CJ, Van Steyn SJ, Fischer RA.

J Shoulder Elbow Surg. 2001 May-Jun;10(3):242-6.

PMID:
11408905
37.

Neuroprotection in the MPTP Parkinsonian C57BL/6 mouse model by a compound isolated from tobacco.

Castagnoli KP, Steyn SJ, Petzer JP, Van der Schyf CJ, Castagnoli N Jr.

Chem Res Toxicol. 2001 May;14(5):523-7.

PMID:
11368550
38.
39.

p-Fluorophenylglycine in the urine of baboons treated with HPTP, the tetrahydropyridine analog of haloperidol.

Mienie LJ, Bergh JJ, Bloomquist JR, Castagnoli N Jr, Steyn SJ, Van der Schyf CJ.

Life Sci. 1999;65(5):535-42.

PMID:
10462080
40.

Enzyme-catalyzed bioactivation of cyclic tertiary amines to form potential neurotoxins.

Castagnoli N Jr, Castagnoli KP, Van der Schyf CJ, Usuki E, Igarashi K, Steyn SJ, Riker RR.

Pol J Pharmacol. 1999 Jan-Feb;51(1):31-8. Review.

PMID:
10389142
41.

Metabolic defects caused by treatment with the tetrahydropyridine analog of haloperidol (HPTP), in baboons.

Mienie LJ, Bergh JJ, Van Staden E, Steyn SJ, Pond SM, Castagnoli N Jr, Van der Schyf CJ.

Life Sci. 1997;61(3):265-72.

PMID:
9217286

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