Search Results - "RUSLIM, Lany"

Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors by Xu, Ying-zi, Yuan, Shendong, Bowers, Simeon, Hom, Roy K., Chan, Wayman, Sham, Hing L., Zhu, Yong L., Beroza, Paul, Pan, Hu, Brecht, Eric, Yao, Nanhua, Lougheed, Julie, Yan, Jiangli, Tam, Danny, Ren, Zhao, Ruslim, Lany, Bova, Michael P., Artis, Dean R.

“…Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1…”
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Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors by Bowers, Simeon, Truong, Anh P., Ye, Michael, Aubele, Danielle L., Sealy, Jennifer M., Neitz, R. Jeffrey, Hom, Roy K., Chan, Wayman, Dappen, Michael S., Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Zhu, Yong L., Beroza, Paul, Tonn, George, Zhang, Heather, Hoffman, Jennifer, Motter, Ruth, Fauss, Donald, Tanaka, Pearl, Bova, Michael P., Ren, Zhao, Tam, Danny, Ruslim, Lany, Baker, Jeanne, Pandya, Deepal, Diep, Linnea, Fitzgerald, Kent, Artis, Dean R., Anderson, John P., Bergeron, Marcelle

“…Polo-like kinase-2 (Plk-2) is a potential therapeutic target for Parkinson’s disease and this Letter describes the SAR of a series of dihydropteridinone based…”
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Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model by Truong, Anh P., Tóth, Gergley, Probst, Gary D., Sealy, Jennifer M., Bowers, Simeon, Wone, David W.G., Dressen, Darren, Hom, Roy K., Konradi, Andrei W., Sham, Hing L., Wu, Jing, Peterson, Brian T., Ruslim, Lany, Bova, Michael P., Kholodenko, Dora, Motter, Ruth N., Bard, Frédérique, Santiago, Pamela, Ni, Huifang, Chian, David, Soriano, Ferdie, Cole, Tracy, Brigham, Elizabeth F., Wong, Karina, Zmolek, Wes, Goldbach, Erich, Samant, Bhushan, Chen, Linda, Zhang, Hongbing, Nakamura, David F., Quinn, Kevin P., Yednock, Ted A., Sauer, John-Michael

“…In this letter, we describe our efforts to design HEA BACE-1 inhibitors that are highly permeable coupled with negligible levels of permeability-glycoprotein…”
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Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor by Bowers, Simeon, Truong, Anh P., Neitz, R. Jeffrey, Neitzel, Martin, Probst, Gary D., Hom, Roy K., Peterson, Brian, Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Tóth, Gergley, Pan, Hu, Yao, Nanhua, Artis, Dean R., Brigham, Elizabeth F., Quinn, Kevin P., Sauer, John-Michael, Powell, Kyle, Ruslim, Lany, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene

“…The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the…”
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Design and synthesis of cell potent BACE-1 inhibitors: Structure–activity relationship of P1′ substituents by Sealy, Jennifer M., Truong, Anh P., Tso, Luke, Probst, Gary D., Aquino, Jose, Hom, Roy K., Jagodzinska, Barbara M., Dressen, Darren, Wone, David W.G., Brogley, Louis, John, Varghese, Tung, Jay S., Pleiss, Michael A., Tucker, John A., Konradi, Andrei W., Dappen, Michael S., Toth, Gergely, Pan, Hu, Ruslim, Lany, Miller, Jim, Bova, Michael P., Sinha, Sukanto, Quinn, Kevin P., Sauer, John-Michael

“…Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Aβ cellular inhibition with selectivity against cathepsin-D…”
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Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958 by Hawkinson, Jon E, Szoke, Balazs G, Garofalo, Albert W, Hom, Dennis S, Zhang, Hongbing, Dreyer, Mark, Fukuda, Juri Y, Chen, Linda, Samant, Bhushan, Simmonds, Stellanie, Zeitz, Karla P, Wadsworth, Angie, Liao, Anna, Chavez, Raymond A, Zmolek, Wes, Ruslim, Lany, Bova, Michael P, Holcomb, Ryan, Butelman, Eduardo R, Ko, Mei-Chuan, Malmberg, Annika B

“…The bradykinin B(1) receptor plays a critical role in chronic pain and inflammation, although efforts to demonstrate efficacy of receptor antagonists have been…”
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A widely applicable, high-throughput TR-FRET assay for the measurement of kinase autophosphorylation: VEGFR-2 as a prototype by Moshinsky, Deborah J, Ruslim, Lany, Blake, Robert A, Tang, Flora

“…Homogeneous time-resolved fluorescence resonance energy transfer (TR-FRET) assays represent a highly sensitive and robust high-throughput screening (HTS)…”
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A selective small molecule inhibitor of c-Met kinase inhibits c-met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo by CHRISTENSEN, James G, SCHRECK, Randall, LIPSON, Kenneth E, RAMPHAL, John, DO, Steven, CUI, Jingrong J, CHERRINGTON, Julie M, MENDEL, Dirk B, BURROWS, Jon, KURUGANTI, Poonam, CHAN, Emily, PHUONG LE, CHEN, Jeffrey, XUEYAN WANG, RUSLIM, Lany, BLAKE, Robert

“…The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor (HGF), have been implicated in the development and progression of several human…”
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Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors by Garofalo, Albert W., Adler, Marc, Aubele, Danielle L., Brigham, Elizabeth F., Chian, David, Franzini, Maurizio, Goldbach, Erich, Kwong, Grace T., Motter, Ruth, Probst, Gary D., Quinn, Kevin P., Ruslim, Lany, Sham, Hing L., Tam, Danny, Tanaka, Pearl, Truong, Anh P., Ye, Xiaocong M., Ren, Zhao

“…Mutations in leucine-rich repeat kinase 2 (LRRK2) are associated with familial Parkinson’s disease (PD). The kinase activity of this complex protein is…”
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Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2 H -pyrazolo[4,3- c ]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch by Probst, Gary, Aubele, Danielle L., Bowers, Simeon, Dressen, Darren, Garofalo, Albert W., Hom, Roy K., Konradi, Andrei W., Marugg, Jennifer L., Mattson, Matthew N., Neitzel, Martin L., Semko, Chris M., Sham, Hing L., Smith, Jenifer, Sun, Minghua, Truong, Anh P., Ye, Xiaocong M., Xu, Ying-zi, Dappen, Michael S., Jagodzinski, Jacek J., Keim, Pamela S., Peterson, Brian, Latimer, Lee H., Quincy, David, Wu, Jing, Goldbach, Erich, Ness, Daniel K., Quinn, Kevin P., Sauer, John-Michael, Wong, Karina, Zhang, Hongbin, Zmolek, Wes, Brigham, Elizabeth F., Kholodenko, Dora, Hu, Kang, Kwong, Grace T., Lee, Michael, Liao, Anna, Motter, Ruth N., Sacayon, Patricia, Santiago, Pamela, Willits, Christopher, Bard, Frédérique, Bova, Michael P., Hemphill, Susanna S., Nguyen, Lam, Ruslim, Lany, Tanaka, Kevin, Tanaka, Pearl, Wallace, William, Yednock, Ted A., Basi, Guriqbal S.

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Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce [alpha]-Synuclein Phosphorylation in Rat Brain by Aubele, Danielle L, Hom, Roy K, Adler, Marc, Galemmo, Robert A, Bowers, Simeon, Truong, Anh P, Pan, Hu, Beroza, Paul, Neitz, R Jeffrey, Yao, Nanhua, Lin, May, Tonn, George, Zhang, Heather, Bova, Michael P, Ren, Zhao, Tam, Danny, Ruslim, Lany, Baker, Jeanne, Diep, Linnea, Fitzgerald, Kent, Hoffman, Jennifer, Motter, Ruth, Fauss, Donald, Tanaka, Pearl, Dappen, Michael, Jagodzinski, Jacek, Chan, Wayman, Konradi, Andrei W, Latimer, Lee, Zhu, Yong L, Sham, Hing L, Anderson, John P, Bergeron, Marcelle, Artis, Dean R

“…Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of [alpha]-synuclein in Lewy bodies, which are one of the…”
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Discovery of (R)‑4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro‑1H‑pyrazolo[4,3‑c]quinoline (ELND006) and (R)‑4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro‑2H‑pyrazolo[4,3‑c]quinoline (ELND007): Metabolically Stable γ‑Secretase Inhibitors that Selectively Inhibit the Production of Amyloid‑β over Notch by Probst, Gary, Aubele, Danielle L, Bowers, Simeon, Dressen, Darren, Garofalo, Albert W, Hom, Roy K, Konradi, Andrei W, Marugg, Jennifer L, Mattson, Matthew N, Neitzel, Martin L, Semko, Chris M, Sham, Hing L, Smith, Jenifer, Sun, Minghua, Truong, Anh P, Ye, Xiaocong M, Xu, Ying-zi, Dappen, Michael S, Jagodzinski, Jacek J, Keim, Pamela S, Peterson, Brian, Latimer, Lee H, Quincy, David, Wu, Jing, Goldbach, Erich, Ness, Daniel K, Quinn, Kevin P, Sauer, John-Michael, Wong, Karina, Zhang, Hongbin, Zmolek, Wes, Brigham, Elizabeth F, Kholodenko, Dora, Hu, Kang, Kwong, Grace T, Lee, Michael, Liao, Anna, Motter, Ruth N, Sacayon, Patricia, Santiago, Pamela, Willits, Christopher, Bard, Frédérique, Bova, Michael P, Hemphill, Susanna S, Nguyen, Lam, Ruslim, Lany, Tanaka, Kevin, Tanaka, Pearl, Wallace, William, Yednock, Ted A, Basi, Guriqbal S

“…Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We…”
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Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce α-Synuclein Phosphorylation in Rat Brain by Aubele, Danielle L., Hom, Roy K., Adler, Marc, Galemmo Jr, Robert A., Bowers, Simeon, Truong, Anh P., Pan, Hu, Beroza, Paul, Neitz, R. Jeffrey, Yao, Nanhua, Lin, May, Tonn, George, Zhang, Heather, Bova, Michael P., Ren, Zhao, Tam, Danny, Ruslim, Lany, Baker, Jeanne, Diep, Linnea, Fitzgerald, Kent, Hoffman, Jennifer, Motter, Ruth, Fauss, Donald, Tanaka, Pearl, Dappen, Michael, Jagodzinski, Jacek, Chan, Wayman, Konradi, Andrei W., Latimer, Lee, Zhu, Yong L., Sham, Hing L., Anderson, John P., Bergeron, Marcelle, Artis, Dean R.

“…Polo‐like kinase‐2 (Plk‐2) has been implicated as the dominant kinase involved in the phosphorylation of α‐synuclein in Lewy bodies, which are one of the…”
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Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration by Bowers, Simeon, Truong, Anh P., Jeffrey Neitz, R., Hom, Roy K., Sealy, Jennifer M., Probst, Gary D., Quincy, David, Peterson, Brian, Chan, Wayman, Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Tóth, Gergely, Pan, Hu, Lin, May, Yao, Nanhua, Artis, Dean R., Zhang, Heather, Chen, Linda, Dryer, Mark, Samant, Bhushan, Zmolek, Wes, Wong, Karina, Lorentzen, Colin, Goldbach, Erich, Tonn, George, Quinn, Kevin P., Sauer, John-Michael, Wright, Sarah, Powell, Kyle, Ruslim, Lany, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene

“…The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds…”
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Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration by Probst, Gary D., Bowers, Simeon, Sealy, Jennifer M., Truong, Anh P., Hom, Roy K., Galemmo, Robert A., Konradi, Andrei W., Sham, Hing L., Quincy, David A., Pan, Hu, Yao, Nanhua, Lin, May, Tóth, Gergley, Artis, Dean R., Zmolek, Wes, Wong, Karina, Qin, Ann, Lorentzen, Colin, Nakamura, David F., Quinn, Kevin P., Sauer, John-Michael, Powell, Kyle, Ruslim, Lany, Wright, Sarah, Chereau, David, Ren, Zhao, Anderson, John P., Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene

“…In this Letter, we describe the discovery of selective JNK2 and JNK3 inhibitors, such as 10, that routinely exhibit >10-fold selectivity over JNK1 and…”
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Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates by Bowers, Simeon, Xu, Ying-zi, Yuan, Shendong, Probst, Gary D., Hom, Roy K., Chan, Wayman, Konradi, Andrei W., Sham, Hing L., Zhu, Yong L., Beroza, Paul, Pan, Hu, Brecht, Eric, Yao, Nanhua, Lougheed, Julie, Tam, Danny, Ren, Zhao, Ruslim, Lany, Bova, Michael P., Artis, Dean R.

“…The structure–activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1…”
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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors by Ng, Raymond A., Sun, Minghua, Bowers, Simeon, Hom, Roy K., Probst, Gary D., John, Varghese, Fang, Lawrence Y., Maillard, Michel, Gailunas, Andrea, Brogley, Louis, Neitz, R. Jeffrey, Tung, Jay S., Pleiss, Michael A., Konradi, Andrei W., Sham, Hing L., Dappen, Michael S., Adler, Marc, Yao, Nanhua, Zmolek, Wes, Nakamura, David, Quinn, Kevin P., Sauer, John-Michael, Bova, Michael P., Ruslim, Lany, Artis, Dean R., Yednock, Ted A.

“…The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the…”
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Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement by Neitz, R. Jeffrey, Konradi, Andrei W., Sham, Hing L., Zmolek, Wes, Wong, Karina, Qin, Ann, Lorentzen, Colin, Nakamura, David, Quinn, Kevin P., Sauer, John-Michael, Powell, Kyle, Ruslim, Lany, Chereau, David, Ren, Zhao, Anderson, John, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene

“…In this Letter, we describe the evolution of selective JNK3 inhibitors from 1, that routinely exhibit >10-fold selectivity over JNK1 and >1000-fold selectivity…”
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Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: Structure–activity relationship of P2′ substituents by Truong, Anh P., Probst, Gary D., Aquino, Jose, Fang, Larry, Brogley, Louis, Sealy, Jennifer M., Hom, Roy K., Tucker, John A., John, Varghese, Tung, Jay S., Pleiss, Michael A., Konradi, Andrei W., Sham, Hing L., Dappen, Michael S., Tóth, Gergley, Yao, Nanhua, Brecht, Eric, Pan, Hu, Artis, Dean R., Ruslim, Lany, Bova, Michael P., Sinha, Sukanto, Yednock, Ted A., Zmolek, Wes, Quinn, Kevin P., Sauer, John-Michael

“…Herein, we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration…”
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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Structure–activity relationship of the aryl region by Probst, Gary D., Bowers, Simeon, Sealy, Jennifer M., Stupi, Brian, Dressen, Darren, Jagodzinska, Barbara M., Aquino, Jose, Gailunas, Andrea, Truong, Anh P., Tso, Luke, Xu, Ying-Zi, Hom, Roy K., John, Varghese, Tung, Jay S., Pleiss, Michael A., Tucker, John A., Konradi, Andrei W., Sham, Hing L., Jagodzinski, Jacek, Toth, Gergely, Brecht, Eric, Yao, Nanhua, Pan, Hu, Lin, May, Artis, Dean R., Ruslim, Lany, Bova, Michael P., Sinha, Sukanto, Yednock, Ted A., Gauby, Shawn, Zmolek, Wes, Quinn, Kevin P., Sauer, John-Michael

“…The structure–activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and…”
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