Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Charles F McHugh"'
Autor:
Paul B. Noto, Timothy W. Sikorski, Francesca Zappacosta, Craig D. Wagner, Rocio Montes de Oca, Matthew E. Szapacs, Roland S. Annan, Yan Liu, Charles F. McHugh, Helai P. Mohammad, Steven P. Piccoli, Caretha L. Creasy
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-19 (2020)
Abstract Arginine methylation has been recognized as a post-translational modification with pleiotropic effects that span from regulation of transcription to metabolic processes that contribute to aberrant cell proliferation and tumorigenesis. This h
Externí odkaz:
https://doaj.org/article/414cd6e4587d4953aac439af4a476cd3
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:
Peter A. Jones, Ashley K. Wiseman, Helai P. Mohammad, Christopher S. Kershaw, Bryan W. King, Ian D. Waddell, Thau F. Ho, Stephen B. Baylin, Morris Muliaditan, Marcus Bantscheff, Elisabeth A. Minthorn, Thilo Werner, Alan P. Graves, Wendy A. Kellner, Phil Chapman, Mehul Patel, Anthony J. Jurewicz, Allan M. Jordan, Emma E. Fairweather, Rab K. Prinjha, Nino Campobasso, Anna Rutkowska, H. Christian Eberl, Ryan G. Kruger, Charles F. McHugh, Michael T. McCabe, Kristin M. Goldberg, Jon Paul Jaworski, Christopher L. Carpenter, Michael Steidel, Stuart Paul Romeril, Dirk A. Heerding, Lourdes Rueda, David T. Fosbenner, Amy N. Taylor, Jacques Briand, Shawn W. Foley, Arthur Groy, Andrew B. Benowitz, Xiaodong Cheng, Donald J. Ogilvie, Paola Grandi, Cunyu Zhang, Mei Li, Sarath Pathuri, Aidan G. Gilmartin, Christian S. Sherk, Juan I. Luengo, Mark Cockerill, Ali Raoof, Alexandra Stowell, Kathryn Keenan, Melissa B. Pappalardi, Makda Mebrahtu, Kristen Wong, Xing Zhang, Jessica L. Handler, Roger J. Butlin, John R. Horton, Susan Merrihew, Charlotte Burt, Dean E. McNulty
Publikováno v:
Nature Cancer. 2:1002-1017
DNA methylation, a key epigenetic driver of transcriptional silencing, is universally dysregulated in cancer. Reversal of DNA methylation by hypomethylating agents, such as the cytidine analogs decitabine or azacytidine, has demonstrated clinical ben
Autor:
Helai P. Mohammad, Francesca Zappacosta, Steven P. Piccoli, Craig D. Wagner, Paul B. Noto, Charles F. McHugh, Caretha L. Creasy, Matthew Szapacs, Timothy W. Sikorski, Yan Liu, Rocio Montes de Oca, Roland S. Annan
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-19 (2020)
Scientific Reports
Scientific Reports
Arginine methylation has been recognized as a post-translational modification with pleiotropic effects that span from regulation of transcription to metabolic processes that contribute to aberrant cell proliferation and tumorigenesis. This has brough
Autor:
Anastasia Wyce, Gopinath Ganji, Kimberly N Smitheman, Chun-Wa Chung, Susan Korenchuk, Yuchen Bai, Olena Barbash, BaoChau Le, Peter D Craggs, Michael T McCabe, Karen M Kennedy-Wilson, Lydia V Sanchez, Romain L Gosmini, Nigel Parr, Charles F McHugh, Dashyant Dhanak, Rab K Prinjha, Kurt R Auger, Peter J Tummino
Publikováno v:
PLoS ONE, Vol 8, Iss 8, p e72967 (2013)
BET family proteins are epigenetic regulators known to control expression of genes involved in cell growth and oncogenesis. Selective inhibitors of BET proteins exhibit potent anti-proliferative activity in a number of hematologic cancer models, in p
Externí odkaz:
https://doaj.org/article/edc29a7e49b54f8688b20ca3340035d5
Autor:
Ryan G. Kruger, Junya Qu, Dai-Shi Su, Helai P. Mohammad, Melissa B. Pappalardi, Patricia A. Elkins, Alan P. Graves, Dirk A. Heerding, William G. Bonnette, Joelle Lorraine Burgess, Juan I. Luengo, Jenny Zeng, Beth Anne Knapp-Reed, Mark J. Schulz, Alexander Joseph Reif, Jeffrey D. Carson, Raman P. Nagarajan, Caretha L. Creasy, Chuck W Blackledge, Kristen Wong, Melissa Stern, Charles F. McHugh, Hongyi Yu, Liping Wang
Publikováno v:
ACS Med Chem Lett
[Image: see text] We report herein the discovery of isoxazole amides as potent and selective SET and MYND Domain-Containing Protein 3 (SMYD3) inhibitors. Elucidation of the structure–activity relationship of the high-throughput screening (HTS) lead
Autor:
Kristen Wong, Jessica L. Handler, Michael T. McCabe, Helai P. Mohammad, Bryan W. King, Dirk A. Heerding, Melissa B. Pappalardi, Ryan G. Kruger, Lourdes Rueda, Mehul Patel, David T. Fosbenner, Allan M. Jordan, Elisabeth A. Minthorn, Andrew B. Benowitz, Kathryn Keenan, Christian S. Sherk, Ali Raoof, Charlotte Burt, Alexandra Stowell, Mark Cockerill, Jacques Briand, Charles F. McHugh, Rab K. Prinjha
Publikováno v:
Cancer Research. 78:2994-2994
Aberrant DNA hypermethylation within promoter regions and subsequent gene silencing are near universal hallmarks of human cancer. Reversal of DNA methylation by a hypomethylating agent, such as decitabine (Dacogen) or azacytidine (Vidaza), has shown
Autor:
BaoChau Le, Robert L. Vessella, Anastasia Wyce, Peter J. Tummino, Caretha L. Creasy, Susan Korenchuk, Yuchen Bai, Yan Degenhardt, Olena Barbash, Ming-Chih Crouthamel, Charles F. McHugh
Publikováno v:
Oncotarget
BET (bromodomain and extra-terminal) proteins regulate gene expression through their ability to bind to acetylated chromatin and subsequently activate RNA PolII-driven transcriptional elongation. Small molecule BET inhibitors prevent binding of BET p
Autor:
Ryan G. Kruger, William H. Miller, Louis V. LaFrance, Celine Duquenne, Alan P. Graves, Heidi M. Ott, Dashyant Dhanak, Christine Thompson, Xinrong Tian, Martin Brandt, Michael T. McCabe, Charles F. McHugh, Mellinger Mark, Susan Korenchuk, Anthony Della Pietra, Peter J. Tummino, Yan Liu, Caretha L. Creasy, Sharad K. Verma, Elsie Diaz, Gopinath Ganji, Glenn S. Van Aller
Publikováno v:
Nature. 492:108-112
EZH2, the catalytic subunit of the polycomb repressive complex 2 (PRC2), is involved in repressing gene expression through methylation of histone H3 on lysine 27 (H3K27). Overexpression of EZH2 is implicated in tumorigenesis, and mutations within its
Autor:
Thau F. Ho, Yan Liu, Xinrong Tian, Patrick McDevitt, Michael Butticello, Timothy K. Hart, Kimberly N. Smitheman, David Soong, Jessica L. Schneck, Peter J. Tummino, Christine L. Hann, Glenn S. Van Aller, Yuchen Bai, Nestor O. Concha, Kasparec Jiri, Melissa B. Pappalardi, Christopher L. Carpenter, Mcnulty Kenneth C, Kelly Federowicz, Jeffrey D. Carson, William H. Miller, Johnson Neil W, Chandrashekhar D. Kamat, Rouse Meagan B, Charles F. McHugh, Michael T. McCabe, Ryan G. Kruger, Dashyant Dhanak, Helai P. Mohammad, Michelle Crouthamel, Yan Degenhardt, William G. Bonnette, Shelby A. Gorman
Publikováno v:
Cancer cell. 28(1)
SummaryEpigenetic dysregulation has emerged as an important mechanism in cancer. Alterations in epigenetic machinery have become a major focus for targeted therapies. The current report describes the discovery and biological activity of a cyclopropyl