Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Roy K, Hom"'
Autor:
Karin Regnström, Jiangli Yan, Lan Nguyen, Kari Callaway, Yanli Yang, Linnea Diep, Weimei Xing, Anirban Adhikari, Paul Beroza, Roy K Hom, Brigit Riley, Don Rudolph, Michael F Jobling, Jeanne Baker, Jennifer Johnston, Andrei Konradi, Michael P Bova, Dean R Artis
Publikováno v:
PLoS ONE, Vol 8, Iss 7, p e66879 (2013)
Surface Plasmon Resonance (SPR) is rarely used as a primary High-throughput Screening (HTS) tool in fragment-based approaches. With SPR instruments becoming increasingly high-throughput it is now possible to use SPR as a primary tool for fragment fin
Externí odkaz:
https://doaj.org/article/49e73ef974d742cb8de3fc7bf2fab6d1
Autor:
Karin Regnström, Jiangli Yan, Lan Nguyen, Kari Callaway, Yanli Yang, Linnea Diep, Weimei Xing, Anirban Adhikari, Paul Beroza, Roy K. Hom, Brigit Riley, Don Rudolph, Michael F. Jobling, Jeanne Baker, Jennifer Johnston, Andrei Konradi, Michael P. Bova, Dean R. Artis
Publikováno v:
PLoS ONE, Vol 8, Iss 7 (2013)
Externí odkaz:
https://doaj.org/article/35a65012167b4ec79e99546bbcc2addb
Autor:
David F. Nakamura, Hing L. Sham, John-Michael Sauer, Dean R. Artis, Lany Ruslim, Ted Yednock, Michael A. Pleiss, Gary Probst, Marc Adler, Minghua Sun, Louis Brogley, Michael S. Dappen, Roy K. Hom, Michel Maillard, Nanhua Yao, Simeon Bowers, Andrei W. Konradi, Jay S. Tung, Raymond A. Ng, Andrea Gailunas, Wes Zmolek, Kevin P. Quinn, Fang Lawrence Y, Varghese John, R. Jeffrey Neitz, Michael P. Bova
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4674-4679
The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the P1′ region provided selectivity over Cat-D with a series of 2,2-dioxo-isothiochromanes and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7bd8b1a206227969363800a4024a00c
https://doi.org/10.1016/j.bmcl.2013.06.006
https://doi.org/10.1016/j.bmcl.2013.06.006
Autor:
John P. Anderson, Dean R. Artis, Hing L. Sham, Roy K. Hom, Michael S. Dappen, Andrei W. Konradi, Simeon Bowers, Hu Pan, Robert A. Galemmo, Marc Adler, Pearl Tanaka, May Lin, Jeanne Baker, Lany Ruslim, Donald J. Fauss, Zhao Ren, Yong L. Zhu, Anh P. Truong, Danny Tam, Marcelle Bergeron, Lee H. Latimer, Paul Beroza, Jacek Jagodzinski, Heather Zhang, Michael P. Bova, George Tonn, Linnea Diep, Ruth Motter, Kent Fitzgerald, Nanhua Yao, Wayman Chan, Jennifer K. Hoffman, R. Jeffrey Neitz, Danielle L. Aubele
Publikováno v:
ChemMedChem. 8:1295-1313
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 hallmarks of Parkinson's disease neuropathology. Potent, selective, brain-penetrant inhibitors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9de472a2de2bc218c1224fe31845aba
https://doi.org/10.1002/cmdc.201300166
https://doi.org/10.1002/cmdc.201300166
Autor:
Anna Liao, Gary Probst, Pamela S. Keim, Kang Hu, Roy K. Hom, David A. Quincy, Michael S. Dappen, Grace T. Kwong, Jenifer Smith, Martin L. Neitzel, Ying-zi Xu, Elizabeth F. Brigham, Kevin P. Quinn, Frédérique Bard, Minghua Sun, Jing Wu, John-Michael Sauer, Dora Kholodenko, Hongbin Zhang, William Wallace, Matthew N. Mattson, Patricia Sacayon, Jacek Jagodzinski, Hing L. Sham, Brian T. Peterson, Simeon Bowers, Jennifer Marugg, Guriqbal S. Basi, Lee H. Latimer, Susanna S. Hemphill, Darren B. Dressen, Karina Wong, Kevin Tanaka, Michael P. Bova, Pamela Santiago, Daniel K. Ness, Anh P. Truong, Wes Zmolek, Lany Ruslim, Christopher Willits, Michael K. Lee, Andrei W. Konradi, Xiaocong M. Ye, Lam Nguyen, Chris M. Semko, Ted A. Yednock, Ruth N. Motter, Albert W. Garofalo, Erich Goldbach, Pearl Tanaka, Danielle L. Aubele
Publikováno v:
Journal of Medicinal Chemistry. 56:5261-5274
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c5b61686f688dd0abd9c5edac66d7201
https://doi.org/10.1021/jm301741t
https://doi.org/10.1021/jm301741t
Autor:
Roy K. Hom, Hing L. Sham, Kyle Powell, Gary Probst, Irene Griswold-Prenner, Simeon Bowers, Brian T. Peterson, Heather Zhang, Gergely Tóth, Frederique Bard, Jennifer Sealy, Karina Wong, Wayman Chan, May Lin, R. Jeffrey Neitz, Lany Ruslim, Bhushan Samant, David A. Quincy, Anh P. Truong, Robert A. Galemmo, Colin Lorentzen, Zhao Ren, Andrei W. Konradi, Mark Dryer, Wes Zmolek, Ted Yednock, Nanhua Yao, Erich Goldbach, Sarah J Wright, Hu Pan, Kevin P. Quinn, John-Michael Sauer, Dean R. Artis, George Tonn, Linda Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5521-5527
The SAR of a series of brain penetrant, trisubstituted thiophene based JNK inhibitors with improved pharmacokinetic properties is described. These compounds were designed based on information derived from metabolite identification studies which led t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31b679a372a052f80d8da68c92b9b5f4
https://doi.org/10.1016/j.bmcl.2011.06.100
https://doi.org/10.1016/j.bmcl.2011.06.100
Autor:
Hing L. Sham, Gergley Tóth, Karina Wong, Ann Qin, Kyle Powell, David A. Quincy, Andrei W. Konradi, Nanhua Yao, Jennifer Sealy, David Chereau, Lany Ruslim, Gary Probst, Sarah J Wright, May Lin, Ted Yednock, Irene Griswold-Prenner, Wes Zmolek, Kevin P. Quinn, Hu Pan, Roy K. Hom, Simeon Bowers, Colin Lorentzen, Frederique Bard, John P. Anderson, Anh P. Truong, Zhao Ren, Robert A. Galemmo, John-Michael Sauer, Dean R. Artis, David F. Nakamura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:315-319
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 >1000-fold selectivity over related MAPKs, p38α and ERK2. Substitution of the naphthalene ring aff
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a612c27c0d960510e5c57743328c54cf
https://doi.org/10.1016/j.bmcl.2010.11.010
https://doi.org/10.1016/j.bmcl.2010.11.010
Autor:
Gergley Tóth, Hu Pan, Gary Probst, John-Michael Sauer, Dean R. Artis, Anh P. Truong, Michael P. Bova, Wes Zmolek, Ted Yednock, Jose Aquino, Michael S. Dappen, Kevin P. Quinn, Sukanto Sinha, Varghese John, Hing L. Sham, Michael A. Pleiss, Roy K. Hom, Lany Ruslim, Louis Brogley, Jennifer Sealy, Nanhua Yao, Larry Fang, Jay S. Tung, John A. Tucker, Eric Brecht, Andrei W. Konradi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4789-4794
Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2' position of the inhibitor with more polar substituents led to compounds 19 a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be5850a2826857f906d4175d1b9a311a
https://doi.org/10.1016/j.bmcl.2010.06.112
https://doi.org/10.1016/j.bmcl.2010.06.112
Autor:
Karina Wong, Erich Goldbach, Gary Probst, John-Michael Sauer, Andrei W. Konradi, Michael P. Bova, Hing L. Sham, Susanna S. Hemphill, Kevin P. Quinn, Guriqbal S. Basi, Simeon Bowers, Anh P. Truong, William Wallace, Roy K. Hom, Lan K. Nguyen, Albert W. Garofalo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6952-6956
The structural modification of a series of [3.3.1] bicyclic sulfonamide based gamma-secretase inhibitors is described. Appropriate substitution on the bicyclic scaffold provides a significant increase in the metabolic stability of the compounds resul
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f0f68b5faee06e48ea31b81668abdf3
https://doi.org/10.1016/j.bmcl.2009.10.060
https://doi.org/10.1016/j.bmcl.2009.10.060
Autor:
Roy K. Hom
Publikováno v:
Expert Opinion on Therapeutic Patents. 17:737-740
This application describes the further evolution of non-peptidic inhibitors of β-amyloid cleaving enzyme (BACE1) for the treatment of Alzheimer's disease. While this is part of a significant effort at Wyeth, these compounds are only moderately poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a743a0e7aafe38b8019de28d6034f5f1
https://doi.org/10.1517/13543776.17.6.737
https://doi.org/10.1517/13543776.17.6.737