Zobrazeno 1 - 10
of 50
pro vyhledávání: '"Roger B. Ruggeri"'
Publikováno v:
Journal of Lipid Research, Vol 47, Iss 3, Pp 537-552 (2006)
We have identified a series of potent cholesteryl ester transfer protein (CETP) inhibitors, one member of which, torcetrapib, is undergoing phase 3 clinical trials. In this report, we demonstrate that these inhibitors bind specifically to CETP with 1
Externí odkaz:
https://doaj.org/article/65964bfc21ea4844aa60df2bb08c7a77
Autor:
Jordan M. Mattheisen, Chris Limberakis, Roger B. Ruggeri, Matthew S. Dowling, Christopher W. am Ende, Emilie Ceraudo, Thomas Huber, Christopher L. McClendon, Thomas P. Sakmar
Publikováno v:
Journal of the American Chemical Society. 145:11173-11184
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7cc5b00c6a565fcfee5f02177fdc5ebb
https://doi.org/10.1021/jacs.3c00972
https://doi.org/10.1021/jacs.3c00972
Autor:
Allyn T. Londregan, Karlygash Aitmakhanova, James Bennett, Laura J. Byrnes, Daniel P. Canterbury, Xiayun Cheng, Thomas Christott, Jennifer Clemens, Steven B. Coffey, João M. Dias, Matthew S. Dowling, Gillian Farnie, Oleg Fedorov, Kimberly F. Fennell, Vicki Gamble, Carina Gileadi, Charline Giroud, Michael R. Harris, Brett D. Hollingshead, Kilian Huber, Magdalena Korczynska, Kimberly Lapham, Paula M. Loria, Arjun Narayanan, Dafydd R. Owen, Brigitt Raux, Parag V. Sahasrabudhe, Roger B. Ruggeri, Laura Díaz Sáez, Ingrid A. Stock, Benjamin A. Thuma, Andy Tsai, Alison E. Varghese
Publikováno v:
Journal of medicinal chemistry.
A series of small-molecule YEATS4 binders have been discovered as part of an ongoing research effort to generate high-quality probe molecules for emerging and/or challenging epigenetic targets. Analogues such as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f200505c5effa14e470509072c0e10b
https://pubmed.ncbi.nlm.nih.gov/36562986
https://pubmed.ncbi.nlm.nih.gov/36562986
Autor:
David A. Griffith, David J. Edmonds, Jean-Philippe Fortin, Amit S. Kalgutkar, J. Brent Kuzmiski, Paula M. Loria, Aditi R. Saxena, Scott W. Bagley, Clare Buckeridge, John M. Curto, David R. Derksen, João M. Dias, Matthew C. Griffor, Seungil Han, V. Margaret Jackson, Margaret S. Landis, Daniel Lettiere, Chris Limberakis, Yuhang Liu, Alan M. Mathiowetz, Jayesh C. Patel, David W. Piotrowski, David A. Price, Roger B. Ruggeri, David A. Tess
Publikováno v:
Journal of medicinal chemistry. 65(12)
Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized diabetes therapy, but their use has been limited because they require injection. Herein, we describe the discovery of the orally bioavailable, small-molecule, GLP-1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff991134db369ff3aa7ceaecc2f6263e
https://pubmed.ncbi.nlm.nih.gov/35647711
https://pubmed.ncbi.nlm.nih.gov/35647711
Autor:
J. Brent Kuzmiski, João M. Dias, Seungil Han, Chris Limberakis, David Price, David J. Edmonds, John M. Curto, Amit S. Kalgutkar, Daniel J. Lettiere, David A. Tess, Clare Buckeridge, Matthew C. Griffor, David R. Derksen, Alan M. Mathiowetz, Roger B. Ruggeri, Paula M. Loria, Aditi R. Saxena, Scott W. Bagley, Yuhang Liu, Margaret S. Landis, David W. Piotrowski, V. Margaret Jackson, David A. Griffith, Jean-Phillipe Fortin
Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized diabetes therapy, but their use has been limited by the requirement for injection. Here we describe the first effective, orally bioavailable small molecule GLP-1R a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::064b771366df377937229b83ffb7a9bf
https://doi.org/10.1101/2020.09.29.319483
https://doi.org/10.1101/2020.09.29.319483
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:
Ingo Hilgendorf, Filip K. Swirski, Amit Kalgukar, Leonard Buckbinder, Roger B. Ruggeri, Stefan Schob, John W. Chen, Matthew Sebas, Benoit Tricot, Yoshiko Iwamoto, Christian Cortes, Benjamin Pulli, Gabriel Courties, Anping Dong, Wei Zheng, Athanasia Skoura, Muhammad Ali, Matthias Nahrendorf
Publikováno v:
JACC: Basic to Translational Science, Vol 1, Iss 7, Pp 633-643 (2016)
JACC: Basic to Translational Science
JACC: Basic to Translational Science
Visual Abstract
Highlights • The inflammatory enzyme MPO is a potential therapeutic target in cardiovascular diseases. • PF-1355 is an orally bioavailable mechanism-based inhibitor of MPO enzymatic activity. PF-1355 treatment successfully in
Highlights • The inflammatory enzyme MPO is a potential therapeutic target in cardiovascular diseases. • PF-1355 is an orally bioavailable mechanism-based inhibitor of MPO enzymatic activity. PF-1355 treatment successfully in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f865d2b9a48e7c50f62499fffc36ea2c
https://doi.org/10.1016/j.jacbts.2016.09.004
https://doi.org/10.1016/j.jacbts.2016.09.004
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:
Angela Wolford, Heather Eng, Li Di, Amit S. Kalgutkar, Deepak Dalvie, Roger B. Ruggeri, Raman Sharma, Leonard Buckbinder, Edward L. Conn
Publikováno v:
Drug Metabolism and Disposition. 44:1262-1269
N1-Substituted-6-arylthiouracils, represented by compound 1 [6-(2,4-dimethoxyphenyl)-1-(2-hydroxyethyl)-2-thioxo-2,3-dihydropyrimidin-4(1H)-one], are a novel class of selective irreversible inhibitors of human myeloperoxidase. The present account is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5a3f704ca958ecb409d06f83a0de310
https://doi.org/10.1124/dmd.116.070185
https://doi.org/10.1124/dmd.116.070185
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