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Items: 27

1.

Novel Small-Molecule Inhibitors of Protein Kinase C Epsilon Reduce Ethanol Consumption in Mice.

Blasio A, Wang J, Wang D, Varodayan FP, Pomrenze MB, Miller J, Lee AM, McMahon T, Gyawali S, Wang HY, Roberto M, McHardy S, Pleiss MA, Messing RO.

Biol Psychiatry. 2018 Aug 1;84(3):193-201. doi: 10.1016/j.biopsych.2017.10.017. Epub 2017 Dec 2.

2.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.

Ng RA, Sun M, Bowers S, Hom RK, Probst GD, John V, Fang LY, Maillard M, Gailunas A, Brogley L, Neitz RJ, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Adler M, Yao N, Zmolek W, Nakamura D, Quinn KP, Sauer JM, Bova MP, Ruslim L, Artis DR, Yednock TA.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4674-9. doi: 10.1016/j.bmcl.2013.06.006. Epub 2013 Jun 11.

PMID:
23856050
3.

Orally available and efficacious α4β1/α4β7 integrin inhibitors.

Xu YZ, Smith JL, Semko CM, Rossiter KI, Fukuda JY, Dappen MS, Quincy DA, Konradi AW, Mao W, Welch B, Dreyer ML, Samant B, Zhang H, Lugar J, Liao Z, Henschel C, Petersen E, Vandevert C, Shoemaker M, Wehner N, Mutter L, Shopp G, Krimm M, Chen L, Wipke B, Dofiles L, Gallager I, Sauer JM, Messersmith EK, Pleiss MA, Bard F, Yednock TA.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4370-3. doi: 10.1016/j.bmcl.2013.05.076. Epub 2013 May 31.

PMID:
23777782
4.

PEG conjugates of potent α4 integrin inhibitors, maintaining sustained levels and bioactivity in vivo, following subcutaneous administration.

Smith JL, Rossiter KI, Semko CM, Xu YZ, Quincy DA, Jagodzinski J, Dappen MS, Konradi AW, Vandevert C, Garrido C, Mao W, San Pablo FB, Wipke B, Dofiles L, Wadsworth A, Peterson E, Lorenzana C, Simmonds S, Messersmith EK, Bard F, Pleiss MA, Yednock TA.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4117-9. doi: 10.1016/j.bmcl.2013.05.048. Epub 2013 May 24.

PMID:
23743283
5.

Arylsulfonamide pyrimidines as VLA-4 antagonists.

Xu YZ, Konradi AW, Bard F, Dappen M, Dofiles L, Dreyer M, Gallager I, Garrido C, Krimm M, Liao Z, Messersmith E, Mutter L, Pleiss MA, Samant B, Semko CM, Smith J, Stappenbeck F, Stupi B, Vandervert C, Welch B, Wipke B, Yednock T.

Bioorg Med Chem Lett. 2013 May 15;23(10):3070-4. doi: 10.1016/j.bmcl.2013.03.010. Epub 2013 Mar 15.

PMID:
23562062
6.

Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons.

Chen HK, Liu Z, Meyer-Franke A, Brodbeck J, Miranda RD, McGuire JG, Pleiss MA, Ji ZS, Balestra ME, Walker DW, Xu Q, Jeong DE, Budamagunta MS, Voss JC, Freedman SB, Weisgraber KH, Huang Y, Mahley RW.

J Biol Chem. 2012 Feb 17;287(8):5253-66. doi: 10.1074/jbc.M111.276162. Epub 2011 Dec 12.

7.

Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.

Neitzel ML, Aubele DL, Marugg JL, Jagodzinski JJ, Konradi AW, Pleiss MA, Szoke B, Zmolek W, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Bova MP, Hemphill S, Basi G.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3715-20. doi: 10.1016/j.bmcl.2011.04.079. Epub 2011 May 1.

PMID:
21571529
8.

Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.

Semko CM, Chen L, Dressen DB, Dreyer ML, Dunn W, Farouz FS, Freedman SB, Holsztynska EJ, Jefferies M, Konradi AW, Liao A, Lugar J, Mutter L, Pleiss MA, Quinn KP, Thompson T, Thorsett ED, Vandevert C, Xu YZ, Yednock TA.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1741-3. doi: 10.1016/j.bmcl.2011.01.075. Epub 2011 Jan 22.

PMID:
21316228
9.

Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D.

Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60.

10.

A small-molecule scaffold induces autophagy in primary neurons and protects against toxicity in a Huntington disease model.

Tsvetkov AS, Miller J, Arrasate M, Wong JS, Pleiss MA, Finkbeiner S.

Proc Natl Acad Sci U S A. 2010 Sep 28;107(39):16982-7. doi: 10.1073/pnas.1004498107. Epub 2010 Sep 10.

11.

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.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6034-9. doi: 10.1016/j.bmcl.2010.08.070. Epub 2010 Aug 19.

PMID:
20822903
12.

Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.

Truong AP, Probst GD, Aquino J, Fang L, Brogley L, Sealy JM, Hom RK, Tucker JA, John V, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Tóth G, Yao N, Brecht E, Pan H, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Zmolek W, Quinn KP, Sauer JM.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4789-94. doi: 10.1016/j.bmcl.2010.06.112. Epub 2010 Jun 25.

PMID:
20634069
13.

Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.

Mattson MN, Neitzel ML, Quincy DA, Semko CM, Garofalo AW, Keim PS, Konradi AW, Pleiss MA, Sham HL, Brigham EF, Goldbach EG, Zhang H, Sauer JM, Basi GS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14.

PMID:
20206516
14.

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.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6386-91. doi: 10.1016/j.bmcl.2009.09.061. Epub 2009 Sep 19.

PMID:
19811916
15.

Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.

Dressen D, Garofalo AW, Hawkinson J, Hom D, Jagodzinski J, Marugg JL, Neitzel ML, Pleiss MA, Szoke B, Tung JS, Wone DW, Wu J, Zhang H.

J Med Chem. 2007 Oct 18;50(21):5161-7. Epub 2007 Sep 19.

PMID:
17880055
16.

Suppression of acute experimental allergic encephalomyelitis with a small molecule inhibitor of alpha4 integrin.

Piraino PS, Yednock TA, Freedman SB, Messersmith EK, Pleiss MA, Karlik SJ.

Mult Scler. 2005 Dec;11(6):683-90.

PMID:
16320728
17.

Spontaneous remyelination following prolonged inhibition of alpha4 integrin in chronic EAE.

Piraino PS, Yednock TA, Messersmith EK, Pleiss MA, Freedman SB, Hammond RR, Karlik SJ.

J Neuroimmunol. 2005 Oct;167(1-2):53-63.

PMID:
16095724
18.

The identification and optimization of orally efficacious, small molecule VLA-4 antagonists.

Huryn DM, Konradi AW, Ashwell S, Freedman SB, Lombardo LJ, Pleiss MA, Thorsett ED, Yednock T, Kennedy JD.

Curr Top Med Chem. 2004;4(14):1473-84. Review.

PMID:
15544538
19.

Synthesis, characterization and evaluation of pro-drugs of VLA-4 antagonists.

Huryn DM, Ashwell S, Baudy R, Dressen DB, Gallaway W, Grant FS, Konradi A, Ley RW, Petusky S, Pleiss MA, Sarantakis D, Semko CM, Sherman MM, Tio C, Zhang L.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1651-4. Erratum in: Bioorg Med Chem Lett. 2004 Nov 1;14(21):5449.

PMID:
15026043
20.

Prolonged reversal of chronic experimental allergic encephalomyelitis using a small molecule inhibitor of alpha4 integrin.

Piraino PS, Yednock TA, Freedman SB, Messersmith EK, Pleiss MA, Vandevert C, Thorsett ED, Karlik SJ.

J Neuroimmunol. 2002 Oct;131(1-2):147-59.

PMID:
12458046
21.

A series of C-terminal amino alcohol dipeptide A beta inhibitors.

Garofalo AW, Wone DW, Phuc A, Audia JE, Bales CA, Dovey HF, Dressen DB, Folmer B, Goldbach EG, Guinn AC, Latimer LH, Mabry TE, Nissen JS, Pleiss MA, Sohn S, Thorsett ED, Tung JS, Wu J.

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3051-3.

PMID:
12372499
22.
23.
24.

comparative analysis of cellular respiratory inhibition by substituted phenylglyoxal-bis-(4-methyl-3-thiosemicarbazone) zinc chelates.

Coats EA, Milstein SR, Pleiss MA, Roesener JA, Schmidt J, McDonald J, Reed R.

Farmaco Sci. 1983 Mar;28(3):143-52.

PMID:
6852227
25.

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