Zobrazeno 1 - 10
of 29
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
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
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
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
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
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
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
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.