Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Dominic, Suarez"'
Autor:
Christopher L. Carpenter, Eldridge N. Nartey, Dominic Suarez, Elisabeth A. Minthorn, Jesus R. Medina, Louis V. LaFrance, Ralph A. Rivero, James F. Mack, Charles F. McHugh, Xinrong Tian, Dirk A. Heerding, Christina Ng Di Marco, Thomas J. Berrodin, Aishwarya Bhaskar, Biju Mangatt, William Hoi Hong Li, Brackley James, Martyr Cuthbert, Lorena A. Kallal, Michael Butticello, Jacob Rubin
Publikováno v:
Journal of Medicinal Chemistry. 64:16056-16087
Elevated expression of the c-MYC oncogene is one of the most common abnormalities in human cancers. Unfortunately, efforts to identify pharmacological inhibitors that directly target MYC have not yet yielded a drug-like molecule due to the lack of an
Autor:
Xinrong Tian, Dominic Suarez, Douglas Thomson, William Li, Elizabeth A. King, Louis LaFrance, Jeffrey Boehm, Linda Barton, Christina Di Marco, Cuthbert Martyr, Reema Thalji, Jesus Medina, Steven Knight, Dirk Heerding, Enoch Gao, Eldridge Nartey, Ted Cecconie, Christopher Nixon, Guofeng Zhang, Thomas J. Berrodin, Christopher Phelps, Amish Patel, Xiaopeng Bai, Ken Lind, Ninad Prabhu, Jeffrey Messer, Zhengrong Zhu, Lisa Shewchuk, Rob Reid, Alan P. Graves, Charles McHugh, Biju Mangatt
Publikováno v:
Journal of medicinal chemistry. 65(21)
E1A binding protein (p300) and CREB binding protein (CBP) are two highly homologous and multidomain histone acetyltransferases. These two proteins are involved in many cellular processes by acting as coactivators of a large number of transcription fa
Autor:
Jesús R, Medina, Xinrong, Tian, William H, Li, Dominic, Suarez, James F, Mack, Louis, LaFrance, Cuthbert, Martyr, James, Brackley, Christina, Di Marco, Ralph, Rivero, Dirk A, Heerding, Charles, McHugh, Elisabeth, Minthorn, Aishwarya, Bhaskar, Jacob, Rubin, Michael, Butticello, Christopher, Carpenter, Eldridge N, Nartey, Thomas J, Berrodin, Lorena A, Kallal, Biju, Mangatt
Publikováno v:
Journal of medicinal chemistry. 64(21)
Elevated expression of the
Autor:
Sanchez Robert, Jeffrey M. Axten, Michael L. Moore, Allison K. McSherry, William Hoi Hong Li, Xinrong Tian, Dominic Suarez
Publikováno v:
Tetrahedron Letters. 60:151312
We describe an efficient synthesis of 2,4-substituted pyrido[4,3-d]pyrimidin-5(6H)-ones, which involves the acid-promoted cyclization of cyano enamine 15 to afford 2,4-bis(methylthio)pyrido[4,3-d]pyrimidin-5(6H)-one 17 as a key intermediate. Selectiv
Autor:
Christine Thompson, Daryl A. Scherzer, Ryan G. Kruger, Steven D. Knight, Louis V. LaFrance, Heidi M. Ott, Dashyant Dhanak, Stuart Paul Romeril, Celine Duquenne, Dominic Suarez, William H. Miller, Art Shu, Seth W. Grant, Carl A. Machutta, Joelle Lorraine Burgess, Brackley James, Caretha L. Creasy, Xinrong Tian, Yong Jiang, Sharad K. Verma, Peter J. Tummino, Alan P. Graves, Glenn S. Van Aller, Elsie Diaz, Kenneth A. Newlander, Johnson Neil W, Michael T. McCabe
Publikováno v:
ACS Medicinal Chemistry Letters. 3:1091-1096
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part of a drug discovery program targeting EZH2, we have ident
Autor:
Rosalie Matico, Michael L. Moore, Dennis Murphy, Paul M. Keller, Mark R. Harpel, John A. Krawiec, John J. Trill, Krista B. Goodman, Daryl A. Scherzer, Deyou Sha, Da-Yuan Wang, Thomas D. Sweitzer, Jeffrey A. Lieby, Maria Cichy-Knight, Dominic Suarez, Michael Jaye, Mui Cheung, Eric S. Manas, Dennis Lee, Sarah E. Dowdell, Dean E. McNulty, Benjamin K. Schwartz, Michael Jonathan Bury, Allison K. Dunn, Roland S. Annan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:27-30
Endothelial lipase (EL) activity has been implicated in HDL catabolism, vascular inflammation, and atherogenesis, and inhibitors are therefore expected to be useful for the treatment of cardiovascular disease. Sulfonylfuran urea 1 was identified in a
Autor:
Dominic Suarez, BaoChau Le, Louis V. LaFrance, James J. Foley, Celine Duquenne, Ryan G. Kruger, Heidi M. Ott, Charles F. McHugh, Mei Li, Charles W. Blackledge, Kenneth A. Newlander, Johnson Neil W, Steven D. Knight, Joelle Lorraine Burgess, Xinrong Tian, Susan Korenchuk, Cynthia M. Rominger, Mcnulty Kenneth C, Stuart Paul Romeril, Jessica Ward, Kasparec Jiri, Michael T. McCabe, Schmidt Stanley J, Dai-Shi Su, Brackley James, Juan I. Luengo, Mark J. Schulz, Glenn S. Van Aller, Michael Butticello, Christopher L. Carpenter
Publikováno v:
Cancer Research. 75:5379-5379
The EZH2 histone methyltransferase is frequently mutated in diffuse large B-cell lymphoma leading to increased trimethylation of histone H3 lysine 27 (H3K27me3). Drug discovery efforts have previously identified a pyridone-based chemical series of EZ
Autor:
Dominic Suarez, Glenn S. Van Aller, Jess Schneck, Kasparec Jiri, Kimberly N. Smitheman, Xinrong Tian, Yan Liu, Patrick McDevitt, Ryan G. Kruger, Helai P. Mohammad, William H. Miller, Christine L. Hann, Melissa B. Pappalardi, Johnson Neil W, Kelly Federowicz, James J. Foley, Jeffrey D. Carson, Monica Cusan, Thau F. Ho, Shekhar Kamat, Scott A. Armstrong, Michael Butticello, Charles F. McHugh
Publikováno v:
Cancer Research. 75:3513-3513
Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase found in various transcriptional co-repressor complexes. LSD1 mediated H3K4 demethylation can result in a repressive chromatin environment that silences gene expression and has b
Autor:
Jessica L. Schneck, Dominic Suarez, Peter J. Tummino, Scott A. Armstrong, Yan Liu, Patrick McDevitt, Helai P. Mohammad, Glenn S. Van Aller, Xinrong Tian, William H. Miller, Kimberly N. Smitheman, Kelly Federowicz, Thau F. Ho, Jeffrey D. Carson, Melissa B. Pappalardi, Johnson Neil W, Monica Cusan, Kasparec Jiri, Rouse Meagan B, Charles F. McHugh, Ryan G. Kruger
Publikováno v:
Blood. 122:3964-3964
Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase found in various transcriptional co-repressor complexes. These complexes include Histone Deacetylases (HDAC1/2) and Co-Repressor for Element-1-Silencing Transcription factor (CoR
Autor:
Michael T. McCabe, Christine Thompson, Ryan G. Kruger, Caretha L. Creasy, Louis V. LaFrance, Stuart Paul Romeril, Mellinger Mark, Charles F. McHugh, Xinrong Tian, Peter J. Tummino, Dash Dhanak, Ken A. Newlander, Dominic Suarez, Alan P. Graves, Celine Duquenne, Brackley James, Sharad K. Verma, BaoChau Le, Daryl A. Scherzer, Steven D. Knight, Johnson Neil W, William H. Miller, Elsie Diaz, Seth W. Grant, Art Shu, Heidi Morgan-Ott, Joelle Lorraine Burgess
Publikováno v:
Cancer Research. 72:2939-2939
The histone methyltransferases are a group of enzymes which catalyze the transfer of a methyl group from the co-factor S-Adenosylmethionine (SAM) to the lysine and arginine residues of histone tails. This post-translational modification is a key even