Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Esther C.Y. Lee"'
Autor:
Shilpi Arora, Anna Kohlmann, Christopher D. Hupp, Julie Liu, Christelle Huguet, Allison Olszewski, Moritz von Rechenberg, John W. Cuozzo, Ying Zhang, Katy E Georgiadis, Matthew A. Clark, Esther C.Y. Lee, Charles J. Eyermann, Andrew J. McRiner, Paolo A. Centrella, Michael I Monteiro, Anthony D. Keefe, Benjamin Levin, Andrew D. Ferguson, Zooey Wang, Yanbin Liu
Publikováno v:
Journal of Medicinal Chemistry. 64:6730-6744
Inhibition of hydroxy acid oxidase 1 (HAO1) is a strategy to mitigate the accumulation of toxic oxalate that results from reduced activity of alanine-glyoxylate aminotransferase (AGXT) in primary hyperoxaluria 1 (PH1) patients. DNA-Encoded Chemical L
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ecd410b881fad4a6d7e1db049c6ba5c
https://doi.org/10.1021/acs.jmedchem.0c02271
https://doi.org/10.1021/acs.jmedchem.0c02271
Autor:
Diana Gikunju, John W. Cuozzo, Yelena A Arnautova, Sarah A Talcott, Neil Westlund, Andrew J. McRiner, Anthony D. Keefe, Yan Yu, Christelle Huguet, Moritz von Rechenberg, Fei Zhou, Jennifer M Duffy, Shilpi Arora, Esther C.Y. Lee, Ying Zhang, Benjamin Levin, Matthew A. Clark, Jeremy S. Disch, Junyi Zhang, Yanbin Liu, Anton Kozhushnyan, Betty Chan, Anthony C Lau, Michael I Monteiro, Patrick B. Mullins, Anna Kohlmann
Publikováno v:
Journal of Medicinal Chemistry. 64:5049-5066
Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat ER+ breast cancer. Information from DNA-encoded chemical library (DECL) screening provid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef7302cad9922daa210279c4d6224ee0
https://doi.org/10.1021/acs.jmedchem.1c00127
https://doi.org/10.1021/acs.jmedchem.1c00127
Autor:
Chris Limberakis, Allyn T. Londregan, Steven B. Coffey, Gary Erik Aspnes, Janice A. Brown, Kevin D. Hesp, Rhys M. Jones, Elnaz Menhaji-Klotz, Esther C.Y. Lee, Markus Boehm
Publikováno v:
Bioorganicmedicinal chemistry letters. 50
The atypical chemokine receptor C-X-C chemokine receptor type 7 (CXCR7) is an attractive therapeutic target for a variety of cardiac and immunological diseases. As a strategy to mitigate known risks associated with the development of higher molecular
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::814f75791497d041702db0bd1f7ff5db
https://pubmed.ncbi.nlm.nih.gov/34400299
https://pubmed.ncbi.nlm.nih.gov/34400299
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1ccac15ee02a34e6adc23a5d238341d
https://pubmed.ncbi.nlm.nih.gov/29466005
https://pubmed.ncbi.nlm.nih.gov/29466005
Autor:
Heather Eng, John Litchfield, William S. Denney, Esther C.Y. Lee, Theunis C. Goosen, Karen Atkinson, Raman Sharma, Jeffrey A. Pfefferkorn, Deepak Dalvie, John C. Pettersen, Li Di, Amit S. Kalgutkar, Neeta B. Amin
Publikováno v:
Drug Metabolism and Disposition. 42:1926-1939
The present article summarizes Metabolites in Safety Testing (MIST) studies on a glucokinase activator, N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide (PF-04937319), which is under developmen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7100b26922e65b60ec5cf194776dacff
https://doi.org/10.1124/dmd.114.060087
https://doi.org/10.1124/dmd.114.060087
Autor:
Steven B. Coffey, Joel T. Arcari, Paula M. Loria, Esther C.Y. Lee, Kentaro Futatsugi, Raman Sharma, David R. Derksen, Amit S. Kalgutkar, Kevin B. Bahnck
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(11)
Prostaglandin E receptor subtype 3 (EP3) antagonism may treat a variety of symptoms from inflammation to cardiovascular and metabolic diseases. Previously, most EP3 antagonists were large acidic ligands that mimic the substrate, prostaglandin E2 (PGE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bad0904c90a0e00a80a1a42da09da66
https://pubmed.ncbi.nlm.nih.gov/27107947
https://pubmed.ncbi.nlm.nih.gov/27107947
Autor:
Beijing Tan, Stephen W. Wright, Karen Atkinson, Janice A. Brown, Angel Guzman-Perez, Kevin J. Filipski, John Litchfield, Mary Theresa Didiuk, Esther C.Y. Lee, Christopher T. Salatto, Jian-Cheng Li, David Christopher Ebner, Meihua Tu, Jeffrey A. Pfefferkorn, Jianwei Bian, Christian Perreault, Matthew F. Sammons, Benjamin D. Stevens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:415-420
A novel series of glucagon receptor antagonists has been discovered. These pyrazole ethers and aminopyrazoles have lower molecular weight and increased polarity such that the molecules fall into better drug-like property space. This work has culminat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96e84026e85448c47076ca75b76b5fd9
https://doi.org/10.1016/j.bmcl.2011.10.113
https://doi.org/10.1016/j.bmcl.2011.10.113
Autor:
Matthew F. Sammons, Esther C.Y. Lee
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(19)
The endocrine hormone glucagon stimulates hepatic glucose output via its action at the glucagon receptor (GCGr) in the liver. In the diabetic state, dysregulation of glucagon secretion contributes to abnormally elevated hepatic glucose output. The in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af8e78d0996dfe9d8a57300c80517e3d
https://pubmed.ncbi.nlm.nih.gov/26271588
https://pubmed.ncbi.nlm.nih.gov/26271588
Autor:
Esther C.Y. Lee, Philip A. Carpino
Publikováno v:
Pharmaceutical patent analyst. 4(2)
The central melanocortin system and particularly the melanocortin-4 receptor (MC4R) subtype, plays an important role in the regulation of body weight. The discovery of orally active MC4R agonists suitable for evaluation in human clinical trials as we
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a0997bbfa53328639a2efe0c1a5ae6e
https://pubmed.ncbi.nlm.nih.gov/25853469
https://pubmed.ncbi.nlm.nih.gov/25853469
Publikováno v:
Organic Letters. 7:1489-1491
[reaction: see text] Pauson-Khand cyclization of dioxanone photoadduct 21 leads to the formation of a single product in good yield. However, retro-aldol fragmentation of the pentacyclic cyclopentenone 22 leads to the formation of 23, with cis C-8/C-1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9f488bb4a6341f4a630a2a7c088502c
https://doi.org/10.1021/ol050103s
https://doi.org/10.1021/ol050103s