Search Results - "Iben, Lawrence G"

Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780 by Toyn, Jeremy H., Thompson, Lorin A., Lentz, Kimberley A., Meredith, Jere E., Burton, Catherine R., Sankaranararyanan, Sethu, Guss, Valerie, Hall, Tracey, Iben, Lawrence G., Krause, Carol M., Krause, Rudy, Lin, Xu-Alan, Pierdomenico, Maria, Polson, Craig, Robertson, Alan S., Denton, R. Rex, Grace, James E., Morrison, John, Raybon, Joseph, Zhuo, Xiaoliang, Snow, Kimberly, Padmanabha, Ramesh, Agler, Michele, Esposito, Kim, Harden, David, Prack, Margaret, Varma, Sam, Wong, Victoria, Zhu, Yingjie, Zvyaga, Tatyana, Gerritz, Samuel, Marcin, Lawrence R., Higgins, Mendi A., Shi, Jianliang, Wei, Cong, Cantone, Joseph L., Drexler, Dieter M., Macor, John E., Olson, Richard E., Ahlijanian, Michael K., Albright, Charles F.

“…Alzheimer’s disease is the most prevalent cause of dementia and is associated with accumulation of amyloid-β peptide (Aβ), particularly the 42-amino acid…”
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Synergistic inhibition of Aβ production by combinations of γ-secretase modulators by Robertson, Alan S., Iben, Lawrence G., Wei, Cong, Meredith, Jere E., Drexler, Dieter M., Banks, Martyn, Vite, Gregory D., Olson, Richard E., Thompson, Lorin A., Albright, Charles F., Ahlijanian, Michael K., Toyn, Jeremy H.

“…Alzheimer's disease is associated with the accumulation of amyloid-β (Aβ) in the brain. In particular, the 42-amino acid form, Aβ1-42, is thought to play a key…”
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Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis by Gerritz, Samuel W, Zhai, Weixu, Shi, Shuhao, Zhu, Shirong, Toyn, Jeremy H, Meredith, Jere E, Iben, Lawrence G, Burton, Catherine R, Albright, Charles F, Good, Andrew C, Tebben, Andrew J, Muckelbauer, Jodi K, Camac, Daniel M, Metzler, William, Cook, Lynda S, Padmanabha, Ramesh, Lentz, Kimberley A, Sofia, Michael J, Poss, Michael A, Macor, John E, Thompson, Lorin A

“…This report describes the discovery and optimization of a BACE-1 inhibitor series containing an unusual acyl guanidine chemotype that was originally…”
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The Amyloid-β Rise and γ-Secretase Inhibitor Potency Depend on the Level of Substrate Expression by Burton, Catherine R., Meredith, Jere E., Barten, Donna M., Goldstein, Margi E., Krause, Carol M., Kieras, Cathy J., Sisk, Lisa, Iben, Lawrence G., Polson, Craig, Thompson, Mark W., Lin, Xu-Alan, Corsa, Jason, Fiedler, Tracey, Pierdomenico, Maria, Cao, Yang, Roach, Arthur H., Cantone, Joseph L., Ford, Michael J., Drexler, Dieter M., Olson, Richard E., Yang, Michael G., Bergstrom, Carl P., McElhone, Kate E., Bronson, Joanne J., Macor, John E., Blat, Yuval, Grafstrom, Robert H., Stern, Andrew M., Seiffert, Dietmar A., Zaczek, Robert, Albright, Charles F., Toyn, Jeremy H.

“…The amyloid-β (Aβ) peptide, which likely plays a key role in Alzheimer disease, is derived from the amyloid-β precursor protein (APP) through consecutive…”
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Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist by Luo, Guanglin, Chen, Ling, Hu, Shuanghua, Huang, Yazhong, Mattson, Gail, Iben, Lawrence G., Russell, John W., Clarke, Wendy J., Hogan, John B., Antal-Zimanyi, Ildiko, Poindexter, Graham S.

“…A convergent synthesis route for the heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 antagonist 2 was developed and the structure activity…”
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Cloning, pharmacological characterization and distribution of a novel galanin receptor by Fathi, Zahra, Cunningham, Anne M, Iben, Lawrence G, Battaglino, Peter B, Ward, Sally A, Nichol, Kerry A, Pine, Kathryn A, Wang, Jiancheng, Goldstein, Margi E, Iismaa, Tiina P, Zimanyi, Ildiko Antal

“…The neuropeptide galanin mediates a diverse spectrum of biological activities by interacting with specific G-protein-coupled receptors. Through expression…”
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Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y1 receptor antagonist by ANTAL-ZIMANYI, Ildiko, BRUCE, Marc. A, ORTIZ, Astrid A, POINDEXTER, Graham S, LEBOULLUEC, Karen L, IBEN, Lawrence G, MATTSON, Gail K, MCGOVERN, Rachel T, HOGAN, John B, LEAHY, Christina L, FLOWERS, Sharon C, STANLEY, Jennifer A

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Signal Peptide Peptidase and γ-Secretase Share Equivalent Inhibitor Binding Pharmacology by Iben, Lawrence G., Olson, Richard E., Balanda, Lynn A., Jayachandra, Sukhanya, Robertson, Barbara J., Hay, Vanessa, Corradi, John, Prasad, C.V.C., Zaczek, Robert, Albright, Charles F., Toyn, Jeremy H.

“…The enzyme γ-secretase has long been considered a potential pharmaceutical target for Alzheimer disease. Presenilin (the catalytic subunit of γ-secretase) and…”
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[ 3H]BMS-599240 — A novel tritiated ligand for the characterization of BACE1 inhibitors by Iben, Lawrence G., Kopcho, Lisa, Marcinkeviciene, Jovita, Zheng, Changsheng, Thompson, Lorin A., Albright, Charles F., Toyn, Jeremy H.

“…In this report we describe a novel radioligand, [ 3H](S)-2-((S)-3-Acetylamino-3- sec-butyl-2-oxo-pyrrolidin-1-yl)-…”
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Molecular characterization, pharmacological properties and chromosomal localization of the human GALR2 galanin receptor by Fathi, Zahra, Battaglino, Peter M, Iben, Lawrence G, Li, Hui, Baker, Elizabeth, Zhang, Donglu, McGovern, Rachel, Mahle, Cathy D, Sutherland, Grant R, Iismaa, Tiina P, Dickinson, Kenneth E.J, Antal Zimanyi, Ildiko

“…The neuropeptide galanin mediates a diverse spectrum of biological activities by interacting with specific G protein-coupled receptors. We have used homology…”
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Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists by Hu, Shuanghua, Huang, Yazhong, Deshpande, Milind, Luo, Guanglin, Bruce, Marc A, Chen, Ling, Mattson, Gail, Iben, Lawrence G, Zhang, Jie, Russell, John W, Clarke, Wendy J, Hogan, John B, Ortiz, Astrid, Flint, Oliver, Henwood, Andrew, Gao, Qi, Antal-Zimanyi, Ildiko, Poindexter, Graham S

“…A novel class of bicyclo[3.1.0]­hexanylpiperazine neuropeptide Y (NPY) Y1 antagonists has been designed and synthesized. Scatchard binding analysis showed…”
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Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists by Gillman, Kevin W., Higgins, Mendi A., Poindexter, Graham S., Browning, Marc, Clarke, Wendy J., Flowers, Sharon, Grace, James E., Hogan, John B., McGovern, Rachel T., Iben, Lawrence G., Mattson, Gail K., Ortiz, Astrid, Rassnick, Stefanie, Russell, John W., Antal-Zimanyi, Ildiko

“…A series of novel 5,5-diphenylimidazolones was synthesized and evaluated for activity against the human neuropeptide Y5 receptor. The 3-pyridyl analog 46…”
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4-Substituted anilides as selective melatonin MT2 receptor agonists by EPPERSON, James R, DESKUS, Jeffrey A, GENTILE, Anthony J, IBEN, Lawrence G, RYAN, Elaine, SARBIN, Nathan S

“…A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2)…”
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Differentially functionalized diamines as novel ligands for the NPY2 receptor by ANDRES, Charles J, ZIMANYI, Ildiko Antal, DESHPANDE, Milind S, IBEN, Lawrence G, GRANT-YOUNG, Katharine, MATTSON, Gail K, WEIXU ZHAI

“…The synthesis of novel ligands for the NPY(2) receptor using solid phase split pool methodology is described. One of the analogues, diamine 16, was found to be…”
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Cloning, expression, and tissue distribution of a fifth melanocortin receptor subtype by ZAHRA FATHI, IBEN, L. G, PARKER, E. M

“…The melanocortin (MC) peptides mediate a diverse spectrum of biological activities in both the central nervous system and peripheral tissues by interacting…”
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A single amino acid difference accounts for the pharmacological distinctions between the rat and human 5-hydroxytryptamine1B receptors by Parker, E M, Grisel, D A, Iben, L G, Shapiro, R A

“…Molecular cloning of the rat and human 5-hydroxytryptamine1B (5-HT1B) receptors has revealed that the primary amino acid sequence of these two receptors is >…”
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Cloning and characterization of the rat GALR1 galanin receptor from Rin14B insulinoma cells by Parker, Eric M., Izzarelli, Darcy G., Nowak, Henry P., Mahle, Cathy D., Iben, Lawrence G., Wang, Jiancheng, Goldstein, Margi E.

“…Galanin is a ubiquitous neuropeptide that regulates a wide array of physiological processes via interaction with specific G protein-coupled receptors. A rat…”
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Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y 1 receptor antagonist by Antal-Zimanyi, Ildiko, Bruce, Marc. A., LeBoulluec, Karen L., Iben, Lawrence G., Mattson, Gail K., McGovern, Rachel T., Hogan, John B., Leahy, Christina L., Flowers, Sharon C., Stanley, Jennifer A., Ortiz, Astrid A., Poindexter, Graham S.

“…Treatment of obesity is still a large unmet medical need. Neuropeptide Y is the most potent orexigenic peptide in the animal kingdom. Its five cloned G-protein…”
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Identification and Preclinical Pharmacology of the [gamma] -Secretase Modulator BMS-869780 by Toyn, Jeremy H, Thompson, Lorin A, Lentz, Kimberley A, Meredith, Jere E, Burton, Catherine R, Sankaranararyanan, Sethu, Guss, Valerie, Hall, Tracey, Iben, Lawrence G, Krause, Carol M, Krause, Rudy, Xu-Alan, Lin, Pierdomenico, Maria, Polson, Craig

“…Alzheimer's disease is the most prevalent cause of dementia and is associated with accumulation of amyloid-β peptide (Aβ), particularly the 42-amino acid…”
Get full text

Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist by Antal-Zimanyi, Ildiko, Bruce, Marc A, Leboulluec, Karen L, Iben, Lawrence G, Mattson, Gail K, McGovern, Rachel T, Hogan, John B, Leahy, Christina L, Flowers, Sharon C, Stanley, Jennifer A, Ortiz, Astrid A, Poindexter, Graham S

“…Treatment of obesity is still a large unmet medical need. Neuropeptide Y is the most potent orexigenic peptide in the animal kingdom. Its five cloned G-protein…”
Get full text