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Page 1
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.
Probst GD, Bowers S, Sealy JM, Stupi B, Dressen D, Jagodzinska BM, Aquino J, Gailunas A, Truong AP, Tso L, Xu YZ, Hom RK, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Sham HL, Jagodzinski J, Toth G, Brecht E, Yao N, Pan H, Lin M, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Gauby S, Zmolek W, Quinn KP, Sauer JM. Probst GD, et al. Among authors: toth g. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6034-9. doi: 10.1016/j.bmcl.2010.08.070. Epub 2010 Aug 19. Bioorg Med Chem Lett. 2010. PMID: 20822903
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
Sealy JM, Truong AP, Tso L, Probst GD, Aquino J, Hom RK, Jagodzinska BM, Dressen D, Wone DW, Brogley L, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Dappen MS, Toth G, Pan H, Ruslim L, Miller J, Bova MP, Sinha S, Quinn KP, Sauer JM. Sealy JM, et al. Among authors: toth g. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6386-91. doi: 10.1016/j.bmcl.2009.09.061. Epub 2009 Sep 19. Bioorg Med Chem Lett. 2009. PMID: 19811916
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Hom RK, Bowers S, Sealy JM, Truong AP, Probst GD, Neitzel ML, Neitz RJ, Fang L, Brogley L, Wu J, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Quinn K, Sauer JM, Powell K, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Hom RK, et al. Among authors: toth g. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7303-7. doi: 10.1016/j.bmcl.2010.10.066. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 21071223
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: toth g. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7. Bioorg Med Chem Lett. 2011. PMID: 21813278
Targeting the intrinsically disordered structural ensemble of α-synuclein by small molecules as a potential therapeutic strategy for Parkinson's disease.
Tóth G, Gardai SJ, Zago W, Bertoncini CW, Cremades N, Roy SL, Tambe MA, Rochet JC, Galvagnion C, Skibinski G, Finkbeiner S, Bova M, Regnstrom K, Chiou SS, Johnston J, Callaway K, Anderson JP, Jobling MF, Buell AK, Yednock TA, Knowles TP, Vendruscolo M, Christodoulou J, Dobson CM, Schenk D, McConlogue L. Tóth G, et al. PLoS One. 2014 Feb 14;9(2):e87133. doi: 10.1371/journal.pone.0087133. eCollection 2014. PLoS One. 2014. PMID: 24551051 Free PMC article.
Novel Small Molecules Targeting the Intrinsically Disordered Structural Ensemble of α-Synuclein Protect Against Diverse α-Synuclein Mediated Dysfunctions.
Tóth G, Neumann T, Berthet A, Masliah E, Spencer B, Tao J, Jobling MF, Gardai SJ, Bertoncini CW, Cremades N, Bova M, Ballaron S, Chen XH, Mao W, Nguyen P, Tabios MC, Tambe MA, Rochet JC, Junker HD, Schwizer D, Sekul R, Ott I, Anderson JP, Szoke B, Hoffman W, Christodoulou J, Yednock T, Agard DA, Schenk D, McConlogue L. Tóth G, et al. Sci Rep. 2019 Nov 18;9(1):16947. doi: 10.1038/s41598-019-52598-4. Sci Rep. 2019. PMID: 31740740 Free PMC article.
DJ-1 can form β-sheet structured aggregates that co-localize with pathological amyloid deposits.
Solti K, Kuan WL, Fórizs B, Kustos G, Mihály J, Varga Z, Herberth B, Moravcsik É, Kiss R, Kárpáti M, Mikes A, Zhao Y, Imre T, Rochet JC, Aigbirhio F, Williams-Gray CH, Barker RA, Tóth G. Solti K, et al. Among authors: toth g. Neurobiol Dis. 2020 Feb;134:104629. doi: 10.1016/j.nbd.2019.104629. Epub 2019 Nov 11. Neurobiol Dis. 2020. PMID: 31669752 Free article.
Probing small molecule binding to amyloid fibrils.
Buell AK, Esbjörner EK, Riss PJ, White DA, Aigbirhio FI, Toth G, Welland ME, Dobson CM, Knowles TP. Buell AK, et al. Among authors: toth g. Phys Chem Chem Phys. 2011 Dec 7;13(45):20044-52. doi: 10.1039/c1cp22283j. Epub 2011 Oct 17. Phys Chem Chem Phys. 2011. PMID: 22006124 Review.
1,414 results