Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Donna N. Petersen"'
Autor:
Liuqing Wei, Jun Xiao, Joseph S. Warmus, Jeffrey R. Chabot, Robert Dullea, Christopher T. Salatto, David W. Piotrowski, Benjamin A. Thuma, Donna N. Petersen, Chris Limberakis, Julien Genovino, Steven B. Coffey, Michael W. Bolt, Kim F. McClure, Kevin D. Hesp, Spiros Liras, Jamie H. D. Cate, Nathanael G. Lintner, Allyn T. Londregan, Gary Erik Aspnes, Benjamin Reidich
Publikováno v:
Journal of Medicinal Chemistry. 61:5704-5718
The optimization of a new class of small molecule PCSK9 mRNA translation inhibitors is described. The potency, physicochemical properties, and off-target pharmacology associated with the hit compound (1) were improved by changes to two regions of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46075104e513dd56e96e55dc41b689b9
https://doi.org/10.1021/acs.jmedchem.8b00650
https://doi.org/10.1021/acs.jmedchem.8b00650
Autor:
Kentaro Futatsugi, Mary Ellen Banker, David W. Piotrowski, Kun Song, Michael Herr, Jonathan N. Bauman, Steven B Co, Sophie Y. Lavergne, Stephen W. Wright, Paula M. Loria, Liuqing Wei, Agustin Casimiro-Garcia, Wenhua Jiao, Matthew F. Sammons, Donna N. Petersen
Publikováno v:
Journal of Medicinal Chemistry. 61:1086-1097
A novel series of morpholine-based nonsteroidal mineralocorticoid receptor antagonists is reported. Starting from a pyrrolidine HTS hit 9 that possessed modest potency but excellect selectivity versus related nuclear hormone receptors, a series of li
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::409210a1f6c1645c791b3128a178eec7
https://doi.org/10.1021/acs.jmedchem.7b01515
https://doi.org/10.1021/acs.jmedchem.7b01515
Autor:
Dennis O. Scott, Spiros Liras, Roger B. Ruggeri, Heather Eng, Adam S. Kamlet, Ryosuke Arakawa, David W. Piotrowski, Robert Dullea, Christopher T. Salatto, Karen Atkinson, Michael W. Bolt, Anne-Marie R. Dechert-Schmitt, Paul DaSilva-Jardine, Allyn T. Londregan, Brian Raymer, Kenneth Dahl, Daniel P. Canterbury, Donna N. Petersen, Paula M. Loria, Chris Limberakis, Emi Kimoto, Kim F. McClure, Kevin Beaumont, Liuqing Wei, Akihiro Takano, Kevin P. Maresca, Jun Xiao, Amanda King-Ahmad, Christer Halldin, Benjamin Reidich, Jeffrey R. Chabot
Publikováno v:
Angewandte Chemie International Edition. 56:16218-16222
Targeting of the human ribosome is an unprecedented therapeutic modality with a genome-wide selectivity challenge. A liver-targeted drug candidate is described that inhibits ribosomal synthesis of PCSK9, a lipid regulator considered undruggable by sm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::284063acd5910c34eb16ba576995a299
https://doi.org/10.1002/anie.201708744
https://doi.org/10.1002/anie.201708744
Autor:
Wanida Ruangsiriluk, Kimberly A. Stevens, Markus Boehm, Benjamin N. Rocke, Paula M. Loria, Julie Jia Li Hawkins, Thomas N. O'Connell, Tim Rolph, Roger B. Ruggeri, Philip A. Carpino, David Hepworth, Bruce A. Maguire, Donna N. Petersen
Publikováno v:
Cell Chemical Biology. 23:1362-1371
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secreted protein that downregulates low-density lipoprotein (LDL) receptor (LDL-R) levels on the surface of hepatocytes, resulting in decreased clearance of LDL-cholesterol (LDL-C). Phenotypi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53acfff7de0a3694bb598b1b57596dee
https://doi.org/10.1016/j.chembiol.2016.08.016
https://doi.org/10.1016/j.chembiol.2016.08.016
Autor:
Donna N. Petersen, David W. Piotrowski, Allyn T. Londregan, Brian Raymer, Paula M. Loria, Liuqing Wei, Kim F. McClure, Gary Erik Aspnes, Jun Xiao, Chris Limberakis, Roger B. Ruggeri
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(23-24)
A series of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides were identified as small molecule PCSK9 mRNA translation inhibitors. Analogues from this new chemical series, such as 4d and 4g, exhibited improved PCSK9 potency, ADM
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58e0977a375ad322edf956fc104b143f
https://pubmed.ncbi.nlm.nih.gov/30482620
https://pubmed.ncbi.nlm.nih.gov/30482620
Autor:
Anthony Carlo, Matthew S. Dowling, Michael John Munchhof, Robert L. Dow, David Price, Aaron C. Smith, Donna N. Petersen, Athanasia Skoura, Christian Cortes, Allyn T. Londregan, Leonard Buckbinder, Jian Wang, Shenping Liu, Kristen Ford, Samit Kumar Bhattacharya, Paula M. Loria, David Hepworth, Cristiano Ruch Werneck Guimarães, Mark Ammirati, Alan M. Mathiowetz, Wenhua Jiao, Jennifer L. LaPerle, Scott W. Bagley, Ayman El-Kattan, Suvi T. M. Orr, Rebecca Conrad
Publikováno v:
ACS Medicinal Chemistry Letters. 6:1128-1133
Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, a tool compo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9c7dc48671313aa67336c68fdaefade
https://doi.org/10.1021/acsmedchemlett.5b00215
https://doi.org/10.1021/acsmedchemlett.5b00215
Autor:
David W. Piotrowski, Jennifer A. Doudna, Kim F. McClure, Spiros Liras, Michael W. Bolt, Bruce A. Maguire, Austin Huang, Robert Dullea, Donna N. Petersen, Jun Xiao, Tim Rolph, Liuqing Wei, Jamie H. D. Cate, Allyn T. Londregan, Kieran F. Geoghegan, Nathanael G. Lintner, Paula M. Loria
Publikováno v:
PLoS biology, vol 15, iss 3
PLoS Biology
PLoS Biology, Vol 15, Iss 3, p e2001882 (2017)
PLoS Biology
PLoS Biology, Vol 15, Iss 3, p e2001882 (2017)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a key role in regulating the levels of plasma low-density lipoprotein cholesterol (LDL-C). Here, we demonstrate that the compound PF-06446846 inhibits translation of PCSK9 by inducing the ri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cce1f6bc26417b37506fac86c75c8950
https://escholarship.org/uc/item/3p3893k1
https://escholarship.org/uc/item/3p3893k1
Autor:
Jun Xiao, Tim Rolph, Spiros Liras, David W. Piotrowski, Nathanael G. Lintner, Austin Huang, Robert Dullea, Allyn T. Londregan, Paula M. Loria, Bruce A. Maguire, Jamie H. D. Cate, Kieran F. Geoghegan, Liuqing Wei, Michael W. Bolt, Jennifer A. Doudna, Kim F. McClure, Donna N. Petersen
Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) plays a key role in regulating the levels of plasma low density lipoprotein cholesterol (LDL-C). Here we demonstrate that the compound PF-06446846 inhibits translation of PCSK9 by inducing the rib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4892b7d80ed1ed142fe4beea7b0f500
Publikováno v:
Journal of Bone and Mineral Research. 3:173-179
We characterized the effect of the tumor promoter phorbol 12-myristate 13-acetate (PMA) on osteoblast function and DNA synthesis in 21-day-old fetal rat calvaria maintained in organ culture. Protein synthesis was determined by measuring the incorpora
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::982be0b107004c4b40d358c0af6628e4
https://doi.org/10.1002/jbmr.5650030208
https://doi.org/10.1002/jbmr.5650030208
Autor:
Oicheng Ng, Thomas A. Brown, Robert F. Day, Amy Brault, Robert L. Rosati, Bruce Allen Lefker, Pia Perry, Bihong Lu, Thomas A. Owen, Michael P. Zawistoski, Richard Chesworth, Tessa A. Castleberry, Kimberly O. Cameron, Lydia C. Pan, David D. Thompson, Paul DaSilva-Jardine, F.Michael Mangano, Stacy Colella, Donna N. Petersen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2729-2733
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER alpha and ER beta selective analogs.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19ab8b698587572775e155590995ad59
https://doi.org/10.1016/j.bmcl.2004.03.077
https://doi.org/10.1016/j.bmcl.2004.03.077