Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Nathan E, Genung"'
Autor:
Brendon E. Cook, Jonathan Archbold, Khaled Nasr, Sara Girmay, Stanley I. Goldstein, Pei Li, Sivaraman Dandapani, Nathan E. Genung, Sac-Pham Tang, Stuart McClusky, Christophe Plisson, Megan E. Afetian, Chrissa A. Dwyer, Michael Fazio, William J. Drury, Frank Rigo, Laurent Martarello, Maciej Kaliszczak
Publikováno v:
Molecular imaging and biology. 24(6)
The treatment of complex neurological diseases often requires the administration of large therapeutic drugs, such as antisense oligonucleotide (ASO), by lumbar puncture into the intrathecal space in order to bypass the blood-brain barrier. Despite th
Autor:
Daniel W. Widlicka, Nathan E. Genung, Jana Polivkova, Daniel W. Kung, Wiglesworth Kristin, Thomas Andrew Brandt, Jun Xiao, Matthew S. Dowling, Yingxin Zhang, Paul M. Herrinton, David J. Edmonds, Todd Zahn, Ka Ning Yip, Colin R. Rose, Qifang Li, Jane Panteleev, Shawn Cabral, Andre Shavnya, Nandell F. Keene, John D. Weaver, Benjamin A. Thuma, Michael Herr, Ian Edmonds, Gary Erik Aspnes, Guoqiang Wang, Philip D. Dent, Dilinie P. Fernando, Aaron C. Smith, Michael G. Vetelino, Sophie Y. Lavergne, Edward L. Conn
Publikováno v:
Organic Process Research & Development. 22:681-696
Indole acids 1, 2, and 3 are potent 5′-adenosine monophosphate-activated protein kinase (AMPK) activators for the potential treatment of diabetic nephropathy. Compounds 1–3 were scaled to supply material for preclinical studies, and indole 3 was
Autor:
Paul DaSilva-Jardine, Jessica Ward, Katherine Cialdea, Matthew F. Calabrese, Marina Amaro, Harmeet Gandhok, Francis Rajamohan, Alan C. Opsahl, Mara Monetti, Kimberly O. Cameron, Tim Rolph, Eliza Bollinger, Benjamin S. Maciejewski, Ravi G. Kurumbail, Christopher T. Salatto, Timothy M. Coskran, David A. Tess, Aditi Jatkar, Nathan E. Genung, Emily Cokorinos, Allan R. Reyes, Morris J. Birnbaum, Germaine Boucher, John M. Kreeger, Andre Shavnya, David J. Edmonds, Russell A. Miller, Amit S. Kalgutkar
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 361:303-311
Diabetic nephropathy remains an area of high unmet medical need, with current therapies that slow down, but do not prevent, the progression of disease. A reduced phosphorylation state of adenosine monophosphate-activated protein kinase (AMPK) has bee
Publikováno v:
Organic Letters. 18:6136-6139
The convergent total synthesis of the manzamine alkaloid (−)-nakadomarin A (1) is described. The retrosynthetic analysis recognized spirocycle 3, assembled via an organocatalyst-promoted Michael addition/cyclization between bicyclic lactam 4 and fu
Autor:
Kimberly O. Cameron, Kevin J. Filipski, Jana Polivkova, Matthew S. Dowling, Andre Shavnya, Gary Erik Aspnes, David Christopher Ebner, Allan R. Reyes, Qifang Li, Michael Herr, Jun Xiao, Jessica Ward, Shawn Cabral, Heather Eng, Sophie Y. Lavergne, Ravi G. Kurumbail, Jane M. Withka, Samit Kumar Bhattacharya, Dilinie P. Fernando, Meihua Tu, Edward L. Conn, Bo Feng, Janice A. Brown, Daniel W. Kung, Francis Rajamohan, Esther C.Y. Lee, Russell A. Miller, Emily Cokorinos, Christopher T. Salatto, Nicole Caspers, Nathan E. Genung, Jane Panteleev, Benjamin A. Thuma, Matthew F. Calabrese, Sumathy Mathialagan, Aaron C. Smith, Kris A. Borzilleri, David J. Edmonds, Amit S. Kalgutkar
Publikováno v:
Journal of medicinal chemistry. 61(6)
Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described. Derivatives of the previously described 5-aryl-indole-3-carboxylic acid clinical candidate (1) were
Autor:
Michael Herr, Daniel P. Canterbury, Derek M. Erion, Janice A. Brown, Mark Niosi, Bhagyashree Khunte, Matthew Gorgoglione, Jaclyn Siderewicz, Jana Polivkova, Carmen N. Garcia-Irizarry, Nathan E. Genung, Adam M. Gilbert, Justin I. Montgomery, Daniel P. Uccello, Timothy P. Rolph, Adhiraj Lanba, Qifang Li, Nicholas B. Vera, Kentaro Futatsugi, Gary Erik Aspnes, Zhenhong Li, James R. Gosset, Kim Huard, Matthew Merrill Hayward, Shawn Cabral, Magee Thomas Victor, Julie Purkal, Kevin B. Bahnck
Publikováno v:
Journal of Medicinal Chemistry. 59:1165-1175
Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of metabolic diseases. In a previous report, we discovered dicarboxylate 1a (PF-06649298) which inhibi
Autor:
Christopher T, Salatto, Russell A, Miller, Kimberly O, Cameron, Emily, Cokorinos, Allan, Reyes, Jessica, Ward, Matthew F, Calabrese, Ravi G, Kurumbail, Francis, Rajamohan, Amit S, Kalgutkar, David A, Tess, Andre, Shavnya, Nathan E, Genung, David J, Edmonds, Aditi, Jatkar, Benjamin S, Maciejewski, Marina, Amaro, Harmeet, Gandhok, Mara, Monetti, Katherine, Cialdea, Eliza, Bollinger, John M, Kreeger, Timothy M, Coskran, Alan C, Opsahl, Germaine G, Boucher, Morris J, Birnbaum, Paul, DaSilva-Jardine, Tim, Rolph
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 361(2)
Diabetic nephropathy remains an area of high unmet medical need, with current therapies that slow down, but do not prevent, the progression of disease. A reduced phosphorylation state of adenosine monophosphate-activated protein kinase (AMPK) has bee
Autor:
Matthew Gorgoglione, Keith Riccardi, James R. Gosset, Cecile Vernochet, Mark Niosi, Adhiraj Lanba, Daniel P. Uccello, Li Di, Magee Thomas Victor, Yimin Zhu, Nathan E. Genung, Jeffrey A. Pfefferkorn, David Pirman, Gary Erik Aspnes, Nicholas B. Vera, Yingjiang Zhou, David Hepworth, Timothy P. Rolph, Michael Herr, Derek M. Erion, Janice A. Brown, Shawn Cabral, Jessica E. C. Jones, Paula M. Loria, Kim Huard, Kentaro Futatsugi, Qingyun Yan, Angela Wolford
Publikováno v:
Scientific Reports
Citrate is a key regulatory metabolic intermediate as it facilitates the integration of the glycolysis and lipid synthesis pathways. Inhibition of hepatic extracellular citrate uptake, by blocking the sodium-coupled citrate transporter (NaCT or SLC13
Publikováno v:
ChemInform. 45
An operationally simple and mild method for the synthesis of a range of structurally diverse indazoles from commercially available reagents is reported.