Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Simeon Bowers"'
Autor:
Tony Muchamuel, Andrea R. Fan, Dustin McMinn, Simeon Bowers, Christopher J. Kirk, Henry Johnson, Janet L. Anderl, David C. Moebius, Eric Lowe
Publikováno v:
Journal of Medicinal Chemistry. 61:11127-11143
Selective immunoproteasome inhibition is a promising approach for treating autoimmune disorders, but optimal proteolytic active site subunit inhibition profiles remain unknown. We reveal here our design of peptide epoxyketone-based selective low mole
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0e3c93b47a1faa5b8f7697f4892f7714
https://doi.org/10.1021/acs.jmedchem.8b01201
https://doi.org/10.1021/acs.jmedchem.8b01201
Autor:
Henry W B, Johnson, Eric, Lowe, Janet L, Anderl, Andrea, Fan, Tony, Muchamuel, Simeon, Bowers, David C, Moebius, Christopher, Kirk, Dustin L, McMinn
Publikováno v:
Journal of medicinal chemistry. 61(24)
Selective immunoproteasome inhibition is a promising approach for treating autoimmune disorders, but optimal proteolytic active site subunit inhibition profiles remain unknown. We reveal here our design of peptide epoxyketone-based selective low mole
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::35428405c924423ae1704f80a06959ee
https://pubmed.ncbi.nlm.nih.gov/30380863
https://pubmed.ncbi.nlm.nih.gov/30380863
Autor:
Randall L. Halcomb, Amanda Valdiosera, David Y. Jackson, Lawrence Chinn, Jonathan S. Melnick, Migone Thi Sau, Mark R. Flory, Derrick Houser, Edward H. van der Horst, Maureen Fitch-Bruhns, Simeon Bowers, Edward Ha, Jorge Monteon, Jan Willem Theunissen, Gary Probst, Tiffany Wong, Paul W. Sauer, Zoia Levashova, Kristy Venstrom, Abel Bermudez, Sindy Liao-Chan, Christopher R. Behrens
Publikováno v:
Mol Pharm
Conventional antibody–drug conjugates (ADCs) are heterogeneous mixtures of chemically distinct molecules that vary in both drugs/antibody (DAR) and conjugation sites. Suboptimal properties of heterogeneous ADCs have led to new site-specific conjuga
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d883318e923b6b79e4a53f04cf24bb2c
https://doi.org/10.1021/acs.molpharmaceut.5b00432
https://doi.org/10.1021/acs.molpharmaceut.5b00432
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:
Colin Lorentzen, Maurizio Franzini, Anh P. Truong, R. Jeffrey Neitz, Marc Adler, Danielle L. Aubele, Pam Santiago, Hing L. Sham, Albert W. Garofalo, Simeon Bowers, Xiaocong M. Ye, Danny Tam, Kevin P. Quinn, Gary Probst, Zhao Ren, Erich Goldbach
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:71-74
Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fde1033b8be37d0cb96bbb6c3ba3646b
https://doi.org/10.1016/j.bmcl.2012.11.021
https://doi.org/10.1016/j.bmcl.2012.11.021
Autor:
Chris M. Semko, Danielle L. Aubele, Guriqbal S. Basi, Wes Zmolek, Gary Probst, Matthew N. Mattson, Elizabeth F. Brigham, Erich Goldbach, Karina Wong, William A Wallace, John-Michael Sauer, Hing L. Sham, Lan K. Nguyen, Michael P. Bova, Andrei W. Konradi, Albert W. Garofalo, Susanna S. Hemphill, Darren B. Dressen, Kevin P. Quinn, Minghua Sun, Anh P. Truong, Simeon Bowers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5791-5794
The structure–activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate β-amyloid peptide synthesis via γ-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c797a2f9e3d425d83f37dc2fbd3a6ac
https://doi.org/10.1016/j.bmcl.2011.08.008
https://doi.org/10.1016/j.bmcl.2011.08.008
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