Search Results - "Ted A. Yednock"

The Classical Complement Pathway Mediates Microglia-Dependent Remodeling of Spinal Motor Circuits during Development and in SMA by Vukojicic, Aleksandra, Delestrée, Nicolas, Fletcher, Emily V., Pagiazitis, John G., Sankaranarayanan, Sethu, Yednock, Ted A., Barres, Ben A., Mentis, George Z.

“…Movement is an essential behavior requiring the assembly and refinement of spinal motor circuits. However, the mechanisms responsible for circuit refinement…”
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Targeting the intrinsically disordered structural ensemble of α-synuclein by small molecules as a potential therapeutic strategy for Parkinson's disease by Tóth, Gergely, Gardai, Shyra J, Zago, Wagner, Bertoncini, Carlos W, Cremades, Nunilo, Roy, Susan L, Tambe, Mitali A, Rochet, Jean-Christophe, Galvagnion, Celine, Skibinski, Gaia, Finkbeiner, Steven, Bova, Michael, Regnstrom, Karin, Chiou, San-San, Johnston, Jennifer, Callaway, Kari, Anderson, John P, Jobling, Michael F, Buell, Alexander K, Yednock, Ted A, Knowles, Tuomas P J, Vendruscolo, Michele, Christodoulou, John, Dobson, Christopher M, Schenk, Dale, McConlogue, Lisa

“…The misfolding of intrinsically disordered proteins such as α-synuclein, tau and the Aβ peptide has been associated with many highly debilitating…”
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C1q-targeted inhibition of the classical complement pathway prevents injury in a novel mouse model of acute motor axonal neuropathy by McGonigal, Rhona, Cunningham, Madeleine E, Yao, Denggao, Barrie, Jennifer A, Sankaranarayanan, Sethu, Fewou, Simon N, Furukawa, Koichi, Yednock, Ted A, Willison, Hugh J

“…Guillain-Barré syndrome (GBS) is an autoimmune disease that results in acute paralysis through inflammatory attack on peripheral nerves, and currently has…”
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Novel approaches to treating inflammatory bowel disease: targeting alpha-4 integrin by Sandborn, William J, Yednock, Ted A

“…Crohn's disease involves persistent recruitment of leukocytes into gut tissue, coupled with dysregulated activation of specific immune cell function. Adhesion…”
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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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PEG conjugates of potent α4 integrin inhibitors, maintaining sustained levels and bioactivity in vivo, following subcutaneous administration by Smith, Jenifer L., Rossiter, Kassandra I., Semko, Christopher M., Xu, Ying-Zi, Quincy, David A., Jagodzinski, Jacek, Dappen, Michael S., Konradi, Andrei W., Vandevert, Christopher, Garrido, Caroline, Mao, Wenxian, San Pablo, F. Bong, Wipke, Brian, Dofiles, Lilibeth, Wadsworth, Angie, Peterson, Eric, Lorenzana, Carlos, Simmonds, Stellanie, Messersmith, Elizabeth K., Bard, Frederique, Pleiss, Michael A., Yednock, Ted A.

“…Mitsunobu reactions were employed to link t-butyl esters of α4 integrin inhibitors at each of the termini of a three-arm, 40kDa, branched PEG. Cleavage of the…”
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Targeting the Intrinsically Disordered Structural Ensemble of [alpha]-Synuclein by Small Molecules as a Potential Therapeutic Strategy for Parkinson's Disease by Tóth, Gergely, Gardai, Shyra J, Zago, Wagner, Bertoncini, Carlos W, Cremades, Nunilo, Roy, Susan L, Tambe, Mitali A, Rochet, Jean-Christophe, Galvagnion, Celine, Skibinski, Gaia, Finkbeiner, Steven, Bova, Michael, Regnstrom, Karin, Chiou, San-San, Johnston, Jennifer, Callaway, Kari, Anderson, John P, Jobling, Michael F, Buell, Alexander K, Yednock, Ted A, Knowles, Tuomas P. J, Vendruscolo, Michele, Christodoulou, John, Dobson, Christopher M, Schenk, Dale, McConlogue, Lisa

“…The misfolding of intrinsically disordered proteins such as [alpha]-synuclein, tau and the A[beta] peptide has been associated with many highly debilitating…”
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Anti-Mcam Monoclonal Antibody PRX003 Inhibits the Unique Migratory Potential of Pathogenic IL-17–Producing T Cells by Flanagan, Kenneth, Tam, Stephen J, Li, Lauri, Dolan, Philip J, Barbour, Robin M, Higaki, Jeffrey N, Liu, Yue, Nijjar, Tarlochan, Skov, Michael, Zago, Wagner, Yednock, Ted A, Kinney, Gene F, Ness, Dan

“…Rationale Melanoma cell adhesion molecule (MCAM) expression on a small subset of memory CD4+/CD8+ T cells defines their ability to secrete IL-17 and identifies…”
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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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Development and validation of immunoassays to quantify the half-antibody exchange of an IgG4 antibody, natalizumab (Tysabri ®) with endogenous IgG4 by Shapiro, Renée I., Plavina, Tatiana, Schlain, Brian R., Pepinsky, R. Blake, Garber, Ellen A., Jarpe, Matthew, Hochman, Paula S., Wehner, Nancy G., Bard, Frederique, Motter, Ruth, Yednock, Ted A., Taylor, Frederick R.

“…Natalizumab is a humanized IgG4 monoclonal antibody which binds human α4 integrin and is approved for treatment of multiple sclerosis and Crohn's disease…”
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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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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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Orally available and efficacious α4β1/α4β7 integrin inhibitors by Xu, Ying-zi, Smith, Jenifer L., Semko, Christopher M., Rossiter, Kassandra I., Fukuda, Juri Y., Dappen, Michael S., Quincy, David A., Konradi, Andrei W., Mao, Wenxian, Welch, Brent, Dreyer, Mark L., Samant, Bhushan, Zhang, Hongbin, Lugar, Judevin, Liao, Zhenmei, Henschel, Carrol, Petersen, Eric, Vandevert, Christopher, Shoemaker, Mark, Wehner, Nancy, Mutter, Linda, Shopp, George, Krimm, Michael, Chen, Linda, Wipke, Brian, Dofiles, Lilibeth, Gallager, Ian, Sauer, John-Michael, Messersmith, Elizabeth K., Pleiss, Michael A., Bard, Frederique, Yednock, Ted A.

“…A series of potent α4β1/α4β7 integrin inhibitors is reported, including an inhibitor 12d with remarkable oral exposure and efficacy in rat models of rheumatoid…”
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Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK by Hom, Roy K., Bowers, Simeon, Sealy, Jennifer M., Truong, Anh P., Probst, Gary D., Neitzel, Martin L., Neitz, R. Jeffrey, Fang, Larry, Brogley, Louis, Wu, Jing, Konradi, Andrei W., Sham, Hing L., Tóth, Gergely, Pan, Hu, Yao, Nanhua, Artis, Dean R., Quinn, Kevin, Sauer, John-Michael, Powell, Kyle, Ren, Zhao, Bard, Frédérique, Yednock, Ted A., Griswold-Prenner, Irene

“…From high throughput screening, we discovered compound 1, the prototype for a series of disubstituted thiophene inhibitors of JNK which is selective towards…”
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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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Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model by Semko, Christopher M., Chen, Linda, Dressen, Darren B., Dreyer, Mark L., Dunn, Whitney, Farouz, Francine S., Freedman, Stephen B., Holsztynska, Elizabeth J., Jefferies, Michael, Konradi, Andrei W., Liao, Anna, Lugar, Judevin, Mutter, Linda, Pleiss, Michael A., Quinn, Kevin P., Thompson, Thomas, Thorsett, Eugene D., Vandevert, Christopher, Xu, Ying-Zi, Yednock, Ted A.

“…A series of N-(pyrimidin-4-yl)-phenylalanine VLA-4 antagonists is described. Optimization of substituents at the 2 and 5 positions of the pyrimidine ring gave…”
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Involvement of Sialic Acid on Endothelial Cells in Organ-Specific Lymphocyte Recirculation by Rosen, Steven D., Singer, Mark S., Yednock, Ted A., Stoolman, Lloyd M.

“…Mouse lymphocytes incubated on cryostat-cut sections of lymphoid organs (lymph nodes and Peyer's patches) specifically adhere to the endothelium of high…”
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