Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Dean Stamos"'
Autor:
Ilze Bot, Natalia V. Ortiz Zacarías, Wilhelmus E. A. de Witte, Henk de Vries, Peter J. van Santbrink, Daniël van der Velden, Mara J. Kröner, Dirk-Jan van der Berg, Dean Stamos, Elizabeth C. M. de Lange, Johan Kuiper, Adriaan P. IJzerman, Laura H. Heitman
Publikováno v:
Scientific Reports, Vol 7, Iss 1, Pp 1-12 (2017)
Abstract CC Chemokine Receptor 2 (CCR2) and its endogenous ligand CCL2 are involved in a number of diseases, including atherosclerosis. Several CCR2 antagonists have been developed as potential therapeutic agents, however their in vivo clinical effic
Externí odkaz:
https://doaj.org/article/be41579bc6074a96b13bbf8097e120c1
Autor:
Kristen A. Baltgalvis, Vincent M. Crowley, Michael A. Schafroth, Brian E. Nordin, Benjamin F. Cravatt, Christie L Eissler, Joe L Rodriguez, Shota Kikuchi, Xiaoyu Zhang, Thomas G Wucherpfennig, Todd Kinsella, Kent T Symons, Melissa M. Dix, David S. Weinstein, Dean Stamos, Gabriel M. Simon, Yu Yamashita, Ludwig Bauer, Lena M Luukkonen
Publikováno v:
J Am Chem Soc
Ligand-induced protein degradation has emerged as a compelling approach to promote the targeted elimination of proteins from cells by directing these proteins to the ubiquitin-proteasome machinery. So far, only a limited number of E3 ligases have bee
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9801b3a3bafd3e374259ca9ad1a1524
https://doi.org/10.1021/jacs.1c00990
https://doi.org/10.1021/jacs.1c00990
Publikováno v:
Chemistry - A European Journal. 22:7059-7062
A Pd-catalyzed/N-heterocycle-directed C(sp(3) )-H olefination has been developed. The monoprotected amino acid ligand (MPAA) is found to significantly promote Pd-catalyzed C(sp(3) )-H olefination for the first time. Cu(OAc)2 instead of Ag(+) salts ar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56b2e867e65a8e91becfe385308ceab1
https://doi.org/10.1002/chem.201600704
https://doi.org/10.1002/chem.201600704
Publikováno v:
Chemistry - A European Journal. 22:4748-4752
Pd(II)-catalyzed C(sp(3))-H arylation of saturated heterocycles with a wide range of aryl iodides is enabled by an N-heterocyclic carbene (NHC) ligand. A C(sp(3))-H insertion step by the Pd(II)/NHC complex in the absence of ArI is demonstrated experi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f171571149e3d17e35ca2a839d07ff14
https://doi.org/10.1002/chem.201600191
https://doi.org/10.1002/chem.201600191
Autor:
Christie L Eissler, Todd Kinsella, Gabe Simon, Colin Walsh, Joseph Klebba, Joel Chick, Ali Tabatabaei, Lena M Luukkonen, Landon Whitby, Kent T Symons, Kristen A. Baltgalvis, Yuta Naro, Matthew P. Patricelli, Larry Burgess, Dean Stamos, Joon Chang, Shota Kikuchi, Jaclyn Brannon, Charles Chapman, Brian E. Nordin
Publikováno v:
Cancer Research. 80:6411-6411
Introduction: Targeted protein degradation is a novel therapeutic modality that holds great promise. Current bispecific degraders have been mostly built using reversible ligands against two well characterized E3 ligases, CRBN and VHL. Features unique
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0fd8700abc857dc43915d725ae6b6f54
https://doi.org/10.1158/1538-7445.am2020-6411
https://doi.org/10.1158/1538-7445.am2020-6411
Autor:
Shengqing Ye, Jin-Quan Yu, Timothy Coon, Dewey Fanning, Yvonne Schmidt, Paul Krenitsky, Weibo Yang, Dean Stamos
Publikováno v:
Angewandte Chemie International Edition. 54:2501-2504
A sequential triple C–H activation reaction directed by a pyrazole and an amide group leads to the well-controlled construction of sterically congested dihydrobenzo[e]indazole derivatives. This cascade reaction demonstrates that the often problemat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93d4a0f0889222f31d6c2f9dd478e0df
https://doi.org/10.1002/anie.201410462
https://doi.org/10.1002/anie.201410462
Autor:
Mara J. Kröner, Adriaan P. IJzerman, Henk de Vries, Dean Stamos, Elizabeth C. M. de Lange, Ilze Bot, Daniël van der Velden, Wilhelmus E. A. de Witte, Peter J. van Santbrink, Laura H. Heitman, Natalia V. Ortiz Zacarías, Dirk-Jan van der Berg, Johan Kuiper
Publikováno v:
Scientific Reports
Scientific Reports, 2017(7), 52
Scientific Reports, Vol 7, Iss 1, Pp 1-12 (2017)
Scientific Reports, 2017(7), 52
Scientific Reports, Vol 7, Iss 1, Pp 1-12 (2017)
CC Chemokine Receptor 2 (CCR2) and its endogenous ligand CCL2 are involved in a number of diseases, including atherosclerosis. Several CCR2 antagonists have been developed as potential therapeutic agents, however their in vivo clinical efficacy was l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8557e1fd3f6a6e2bca8a2b652d9b06a1
https://hdl.handle.net/1887/49661
https://hdl.handle.net/1887/49661
Autor:
Heather Twin, Chau Mak, Francoise Pierard, Juan-Miguel Jimenez, Jeremy J. Clemens, Sam Sperry, John Studley, Andrew Miller, Dean Stamos, Andreas Termin, Philip N. Collier, Guy Brenchley, Juliana L. Asgian, Brett B. Busch, Jeffrey Abt, Sandra Lechner, Roger Heim, Tina B. Flores, Ray Gross, Dao Tran, Vadims Dvornikovs, Peggy Chiang, Timothy Coon, Sarah Hudson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3398-3402
Extensive phase II metabolism of an advanced PKCε inhibitor resulted in sub-optimal pharmacokinetics in rat marked by elevated clearance. Synthesis of the O-glucuronide metabolite as a standard was followed by three distinct strategies to specifical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76338524c1b4881c748508cd81b19f7b
https://doi.org/10.1016/j.bmcl.2014.05.082
https://doi.org/10.1016/j.bmcl.2014.05.082
Autor:
Dean Stamos, Michael Liu, Beth Fleck, Lance Goulet, Weichao Chen, Harmon J. Zuccola, Phillip W. Snyder, Dao Tran, Peggy Chiang, James Reynolds, Azin Nezami, Samuel Sperry, Khisal Ahmed Alvi, Alcacio Timothy, Lisa Woody, William Kargo, Amy Turnbull, Timothy Neubert, Justin T. Ernst
Publikováno v:
Journal of Medicinal Chemistry. 57:3382-3400
A structure-based drug design strategy was used to optimize a novel benzolactam series of HSP90α/β inhibitors to achieve >1000-fold selectivity versus the HSP90 endoplasmic reticulum and mitochondrial isoforms (GRP94 and TRAP1, respectively). Selec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83ca6703412658299afbc7f2df9948d1
https://doi.org/10.1021/jm500042s
https://doi.org/10.1021/jm500042s
Autor:
Harmon J. Zuccola, Bryan W. Vought, Michael Liu, Justin T. Ernst, E. Adam Kallel, Timothy Neubert, Amy Turnbull, Kevin Beaumont, Dean Stamos
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:204-208
HSP90 continues to be a target of interest for neurodegeneration indications. Selective knockdown of the HSP90 cytosolic isoforms α and β is sufficient to reduce mutant huntingtin protein levels in vitro. Chemotype-dependent binding conformations o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::504a8638af20fbe0e48512d5bc9afbe3
https://doi.org/10.1016/j.bmcl.2013.11.036
https://doi.org/10.1016/j.bmcl.2013.11.036