Steyn SJ - Search Results

1

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. Daher JP, et al. Among authors: steyn sj. J Biol Chem. 2015 Aug 7;290(32):19433-44. doi: 10.1074/jbc.M115.660001. Epub 2015 Jun 15. J Biol Chem. 2015. PMID: 26078453 Free PMC article.

2

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. Steyn SJ, et al. J Biochem Biophys Methods. 2005 Jan 31;62(1):25-40. doi: 10.1016/j.jbbm.2004.07.002. Epub 2004 Sep 23. J Biochem Biophys Methods. 2005. PMID: 15656941

3

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. Galatsis P, et al. Among authors: steyn sj. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4132-40. doi: 10.1016/j.bmcl.2014.07.052. Epub 2014 Jul 30. Bioorg Med Chem Lett. 2014. PMID: 25113930

4

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. Henderson JL, et al. Among authors: steyn sj. J Med Chem. 2015 Jan 8;58(1):419-32. doi: 10.1021/jm5014055. Epub 2014 Nov 17. J Med Chem. 2015. PMID: 25353650

5

Imaging Leucine-Rich Repeat Kinase 2 In Vivo with ¹⁸F-Labeled Positron Emission Tomography Ligand.

Chen Z, Chen J, Chen L, Yoo CH, Rong J, Fu H, Shao T, Coffman K, Steyn SJ, Davenport AT, Daunais JB, Haider A, Collier L, Josephson L, Wey HY, Zhang L, Liang SH. Chen Z, et al. Among authors: steyn sj. J Med Chem. 2023 Feb 9;66(3):1712-1724. doi: 10.1021/acs.jmedchem.2c00551. Epub 2022 Oct 18. J Med Chem. 2023. PMID: 36256881

6

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. Davoren JE, et al. Among authors: steyn sj. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. doi: 10.1016/j.bmcl.2015.11.053. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26631313

7

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. Varma MV, et al. Among authors: steyn sj. J Med Chem. 2010 Feb 11;53(3):1098-108. doi: 10.1021/jm901371v. J Med Chem. 2010. PMID: 20070106

8

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. McClure KF, et al. Among authors: steyn sj. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30. Bioorg Med Chem Lett. 2013. PMID: 23953189

9

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. Popiolek M, et al. Among authors: steyn sj. Biochemistry. 2016 Dec 27;55(51):7073-7085. doi: 10.1021/acs.biochem.6b00688. Epub 2016 Dec 13. Biochemistry. 2016. PMID: 27958713

10

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. Davoren JE, et al. Among authors: steyn sj. J Med Chem. 2017 Aug 10;60(15):6649-6663. doi: 10.1021/acs.jmedchem.7b00597. Epub 2017 Jul 26. J Med Chem. 2017. PMID: 28598634

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