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Ionization behavior of amino lipids for siRNA delivery: determination of ionization constants, SAR, and the impact of lipid pKa on cationic lipid-biomembrane interactions

Zhang, Jingtao ; Fan, Haihong ; Levorse, Dorothy A ; Crocker, Louis S

Langmuir : the ACS journal of surfaces and colloids, 01 March 2011, Vol.27(5), pp.1907-14 [Peer Reviewed Journal]

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Interaction of cholesterol-conjugated ionizable amino lipids with biomembranes: lipid polymorphism, structure-activity relationship, and implications for siRNA delivery

Zhang, Jingtao ; Fan, Haihong ; Levorse, Dorothy A ; Crocker, Louis S

Langmuir : the ACS journal of surfaces and colloids, 02 August 2011, Vol.27(15), pp.9473-83 [Peer Reviewed Journal]

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Synthesis of oxaspiropiperidines as a strategy for lowering log D

Cernak, Timothy ; Dykstra, Kevin ; Levorse, Dorothy ; Verras, Andreas ; Balkovec, James ; Nargund, Ravi ; Devita, Robert

Tetrahedron Letters, 30 November 2011, Vol.52(48), pp.6457-6459 [Peer Reviewed Journal]

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Use of molecular modeling aided design to dial out hERG liability in adenosine A2A receptor antagonists

Deng, Qiaolin ; Lim, Yeon-Hee ; Anand, Rajan ; Yu, Younong ; Kim, Jae-Hun ; Zhou, Wei ; Zheng, Junying ; Tempest, Paul ; Levorse, Dorothy ; Zhang, Xiaoping ; Greene, Scott ; Mullins, Deborra ; Culberson, Chris ; Sherborne, Brad ; Parker, Eric M. ; Stamford, Andrew ; Ali, Amjad

Bioorganic & Medicinal Chemistry Letters, 1 August 2015, Vol.25(15), pp.2958-2962 [Peer Reviewed Journal]

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Difluoroethylamines as an amide isostere in inhibitors of cathepsin K

Isabel, Elise ; Mellon, Christophe ; Boyd, Michael J. ; Chauret, Nathalie ; Deschênes, Denis ; Desmarais, Sylvie ; Falgueyret, Jean-Pierre ; Gauthier, Jacques Yves ; Khougaz, Karine ; Lau, Cheuk K. ; Léger, Serge ; Levorse, Dorothy A. ; Li, Chun Sing ; Massé, Frédéric ; David Percival, M. ; Roy, Bruno ; Scheigetz, John ; Thérien, Michel ; Truong, Vouy Linh ; Wesolowski, Gregg ; Young, Robert N. ; Zamboni, Robert ; Cameron Black, W.

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(3), pp.920-923 [Peer Reviewed Journal]

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Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder

Edmondson, Scott D ; Zhu, Cheng ; Kar, Nam Fung ; Di Salvo, Jerry ; Nagabukuro, Hiroshi ; Sacre-Salem, Beatrice ; Dingley, Karen ; Berger, Richard ; Goble, Stephen D ; Morriello, Gregori ; Harper, Bart ; Moyes, Christopher R ; Shen, Dong-Ming ; Wang, Liping ; Ball, Richard ; Fitzmaurice, Aileen ; Frenkl, Tara ; Gichuru, Loise N ; Ha, Sookhee ; Hurley, Amanda L ; Jochnowitz, Nina ; Levorse, Dorothy ; Mistry, Shruty ; Miller, Randy R ; Ormes, James ; Salituro, Gino M ; Sanfiz, Anthony ; Stevenson, Andra S ; Villa, Katherine ; Zamlynny, Beata ; Green, Stuart ; Struthers, Mary ; Weber, Ann E

Journal of medicinal chemistry, 28 January 2016, Vol.59(2), pp.609-23 [Peer Reviewed Journal]

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The elusive 8-fluoroadenosine: a simple non-enzymatic synthesis and characterization

Butora, Gabor ; Schmitt, Christoph ; Levorse, Dorothy A. ; Streckfuss, Eric ; Doss, George A. ; Maccoss, Malcolm

Tetrahedron, 2007, Vol.63(18), pp.3782-3789 [Peer Reviewed Journal]

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Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR

Finke, Paul E. ; Meurer, Laura C. ; Levorse, Dorothy A. ; Mills, Sander G. ; Maccoss, Malcolm ; Sadowski, Sharon ; Cascieri, Margaret A. ; Tsao, Kwei-Lan ; Chicchi, Gary G. ; Metzger, Joseph M. ; Macintyre, D. Euan

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(17), pp.4497-4503 [Peer Reviewed Journal]

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Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities

Tang, Haifeng ; Yan, Yan ; Feng, Zhe ; De Jesus, Reynalda K ; Yang, Lihu ; Levorse, Dorothy A ; Owens, Karen A ; Akiyama, Taro E ; Bergeron, Raynald ; Castriota, Gino A ; Doebber, Thomas W ; Ellsworth, Kenneth P ; Lassman, Michael E ; Li, Cai ; Wu, Margaret S ; Zhang, Bei B ; Chapman, Kevin T ; Mills, Sander G ; Berger, Joel P ; Pasternak, Alexander

Bioorganic & medicinal chemistry letters, 15 October 2010, Vol.20(20), pp.6088-92 [Peer Reviewed Journal]

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Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities

Tang, Haifeng ; Yan, Yan ; Feng, Zhe ; de Jesus, Reynalda K. ; Yang, Lihu ; Levorse, Dorothy A. ; Owens, Karen A. ; Akiyama, Taro E. ; Bergeron, Raynald ; Castriota, Gino A. ; Doebber, Thomas W. ; Ellsworth, Kenneth P. ; Lassman, Michael E. ; Li, Cai ; Wu, Margaret S. ; Zhang, Bei B. ; Chapman, Kevin T. ; Mills, Sander G. ; Berger, Joel P. ; Pasternak, Alexander

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(20), pp.6088-6092 [Peer Reviewed Journal]

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Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase

Barrow, James C ; Stauffer, Shaun R ; Rittle, Kenneth E ; Ngo, Phung L ; Yang, Zhiqiang ; Selnick, Harold G ; Graham, Samuel L ; Munshi, Sanjeev ; Mcgaughey, Georgia B ; Holloway, M Katharine ; Simon, Adam J ; Price, Eric A ; Sankaranarayanan, Sethu ; Colussi, Dennis ; Tugusheva, Katherine ; Lai, Ming-Tain ; Espeseth, Amy S ; Xu, Min ; Huang, Qian ; Wolfe, Abigail ; Pietrak, Beth ; Zuck, Paul ; Levorse, Dorothy A ; Hazuda, Daria ; Vacca, Joseph P

Journal of medicinal chemistry, 23 October 2008, Vol.51(20), pp.6259-62 [Peer Reviewed Journal]

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Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-4-(2-18Ffluoroethoxy)phenyl-1-methylpropyl}- 2-methyl-2-(5-methylpyridin-2-yl)oxypropanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use

Liu, Ping ; Lin, Linus S ; Hamill, Terence G ; Jewell, James P ; Lanza, Thomas J ; Gibson, Raymond E ; Krause, Stephen M ; Ryan, Christine ; Eng, Waisi ; Sanabria, Sandra ; Tong, Xinchun ; Wang, Junying ; Levorse, Dorothy A ; Owens, Karen A ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Kumar, Sanjeev ; Yin, Wenji ; Payack, Joseph F ; Springfield, Shawn A ; Hargreaves, Richard ; Burns, H Donald ; Goulet, Mark T ; Hagmann, William K

Journal of medicinal chemistry, 26 July 2007, Vol.50(15), pp.3427-30 [Peer Reviewed Journal]

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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-1,2,4triazolo1,5-a-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Edmondson, Scott D ; Mastracchio, Anthony ; Mathvink, Robert J ; He, Jiafang ; Harper, Bart ; Park, You-Jung ; Beconi, Maria ; Di Salvo, Jerry ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Leone, Joseph F ; Levorse, Dorothy A ; Lyons, Kathryn ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Aleksandr ; Scapin, Giovanna ; Shang, Jackie ; Roy, Ranabir Sinha ; Smith, Aaron ; Wu, Joseph K ; Xu, Shiyao ; Zhu, Bing ; Thornberry, Nancy A ; Weber, Ann E

Journal of medicinal chemistry, 15 June 2006, Vol.49(12), pp.3614-27 [Peer Reviewed Journal]

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Substituted N-(3,5-Dichlorobenzenesulfonyl)- l-prolyl-phenylalanine analogues as potent VLA-4 antagonists

Kopka, Ihor E ; Young, David N ; Lin, Linus S ; Mumford, Richard A ; Magriotis, Plato A ; Maccoss, Malcolm ; Mills, Sander G ; Riper, Gail Van ; Mccauley, Ermengilda ; Egger, Linda E ; Kidambi, Usha ; Schmidt, John A ; Lyons, Kathryn ; Stearns, Ralph ; Vincent, Stella ; Colletti, Adria ; Wang, Zhen ; Tong, Sharon ; Wang, Junying ; Zheng, Song ; Owens, Karen ; Levorse, Dorothy ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(4), pp.637-640 [Peer Reviewed Journal]

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Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists

Kopka, Ihor E ; Lin, Linus S ; Mumford, Richard A ; Lanza, Thomas ; Magriotis, Plato A ; Young, David ; Delaszlo, Stephen E ; Maccoss, Malcolm ; Mills, Sander G ; Van Riper, Gail ; Mccauley, Ermengilda ; Lyons, Kathryn ; Vincent, Stella ; Egger, Linda A ; Kidambi, Usha ; Stearns, Ralph ; Colletti, Adria ; Teffera, Yohannes ; Tong, Sharon ; Owens, Karen ; Levorse, Dorothy ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(17), pp.2415-2418 [Peer Reviewed Journal]

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The discovery of sulfonylated dipeptides as Potent VLA-4 antagonists

Hagmann, William K ; Durette, Philippe L ; Lanza, Thomas ; Kevin, Nancy Jo ; de Laszlo, Stephen E ; Kopka, Ihor E ; Young, David ; Magriotis, Plato A ; Li, Bing ; Lin, Linus S ; Yang, Ginger ; Kamenecka, Theodore ; Chang, Linda L ; Wilson, Jonathan ; Maccoss, Malcolm ; Mills, Sander G ; Van Riper, Gail ; Mccauley, Ermengilda ; Egger, Linda A ; Kidambi, Usha ; Lyons, Kathryn ; Vincent, Stella ; Stearns, Ralph ; Colletti, Adria ; Teffera, Johannes ; Tong, Sharon ; Fenyk-Melody, Judy ; Owens, Karen ; Levorse, Dorothy ; Kim, Philip ; Schmidt, John A ; Mumford, Richard A

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(20), pp.2709-2713 [Peer Reviewed Journal]

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Inhibition of Stromelysin-1 (MMP-3) by P 1 ‘-Biphenylylethyl Carboxyalkyl Dipeptides
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Inhibition of Stromelysin-1 (MMP-3) by P 1 ‘-Biphenylylethyl Carboxyalkyl Dipeptides

Esser, Craig K. ; Bugianesi, Robert L. ; Caldwell, Charles G. ; Chapman, Kevin T. ; Durette, Philippe L. ; Girotra, Narindar N. ; Kopka, Ihor E. ; Lanza, Thomas J. ; Levorse, Dorothy A. ; Maccoss, Malcolm ; Owens, Karen A. ; Ponpipom, Mitree M. ; Simeone, Joseph P. ; Harrison, Richard K. ; Niedzwiecki, Lisa ; Becker, Joseph W. ; Marcy, Alice I. ; Axel, Melinda G. ; Christen, Amy J. ; Mcdonnell, Joseph ; Moore, Vernon L. ; Olszewski, Julie M. ; Saphos, Cheryl ; Visco, Denise M. ; Shen, Frank ; Colletti, Adria ; Krieter, Philip A. ; Hagmann, William K.

Journal of Medicinal Chemistry, 03/1997, Vol.40(6), pp.1026-1040 [Peer Reviewed Journal]

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CCDC 1421635: Experimental Crystal Structure Determination

Edmondson, Scott D. ; Zhu, Cheng ; Kar, Nam Fung ; Di Salvo, Jerry ; Nagabukuro, Hiroshi ; Sacre-Salem, Beatrice ; Dingley, Karen ; Berger, Richard ; Goble, Stephen D. ; Morriello, Gregori ; Harper, Bart ; Moyes, Christopher R. ; Shen, Dong-Ming ; Wang, Liping ; Ball, Richard ; Fitzmaurice, Aileen ; Frenkl, Tara ; Gichuru, Loise N. ; Ha, Sookhee ; Hurley, Amanda L. ; Jochnowitz, Nina ; Levorse, Dorothy ; Mistry, Shruty ; Miller, Randy R. ; Ormes, James ; Salituro, Gino M. ; Sanfiz, Anthony ; Stevenson, Andra S. ; Villa, Katherine ; Zamlynny, Beata ; Green, Stuart ; Struthers, Mary ; Weber, Ann E.

2016

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