Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Dashyant Dhanak"'
Autor:
Dirk Roymans, Wim Bert Griet Schepens, Danielle Peeters, Jaap Goudsmit, Maria J. P. van Dongen, Wenli Yu, Ronald Vogels, Bart Stoops, Boerries Brandenburg, J.M. Klap, Edward C. Lawson, Tim H. M. Jonckers, Mandy Jongeneelen, Harry A. van Diepen, Sven Blokland, Chan Tang, Wouter Goutier, Christophe Buyck, Ellen Lanckacker, Ian A. Wilson, Jan Vermond, P. Roevens, Wouter Koudstaal, Jin Wu, Frederike Schmitz, Rameshwar U. Kadam, Jarek Juraszek, Alida van Eijgen-Obregoso Real, Dashyant Dhanak, Pierre Jean-Marie Bernard Raboisson, Robert Heinz Edward Friesen, Divita Garg
Publikováno v:
Science. 363
A small molecule that targets influenza Many of us rely on seasonal vaccines for protection against influenza and are only too aware of their limited breadth. Broadly neutralizing antibodies (bnAbs) that target the conserved hemagglutinin (HA) stem o
Autor:
Martin Brandt, Caretha L. Creasy, Elsie Diaz, Benjamin Schwartz, Peter J. Tummino, Melissa B. Pappalardi, William H. Miller, Glenn S. Van Aller, Ryan G. Kruger, Sharad K. Verma, Heidi M. Ott, Dashyant Dhanak, Michael T. McCabe
Publikováno v:
ACS Chemical Biology. 9:622-629
EZH2/PRC2 catalyzes transcriptionally repressive methylation at lysine 27 of histone H3 and has been associated with numerous cancer types. Point mutations in EZH2 at Tyr641 and Ala677 identified in non-Hodgkin lymphomas alter substrate specificity a
Autor:
Kristian Helin, Dashyant Dhanak
Publikováno v:
Helin, K & Dhanak, D 2013, ' Chromatin proteins and modifications as drug targets ', Nature, vol. 502, no. 7472, pp. 480-8 . https://doi.org/10.1038/nature12751
A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal deve
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:
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:
Nannan Liu, Michael N. Zimmerman, Richard M. Keenan, Victor K. Johnston, Deping Chai, Rosanna Tedesco, Duke M. Fitch, Juili Lin-Goerke, Kenneth Wiggall, Antony N. Shaw, Nestor O. Concha, Ramesh Bambal, Michael G. Darcy, Robert T. Sarisky, Dashyant Dhanak, Kevin J. Duffy, Adam T. Gates
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4350-4353
The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Re
Autor:
William F. Huffman, Ken A. Newlander, Amita M. Chaudhari, Shu-Yun Zhang, Michael L. Moore, Jeffrey T. Finer, Kevin J. Duffy, Antony N. Shaw, Melody Diamond, David Sutton, Robert A. Copeland, Michael N. Zimmerman, Chiu-Mei M Sung, Leo F. Faucette, Roman Sakowicz, Jeffrey R. Jackson, Lusong Luo, Kurt R. Auger, Kenneth W. Wood, Jeffrey D. Carson, Carla A. Donatelli, Cynthia A. Parrish, Erin D. Hugger, Steven D. Knight, Lance Ridgers, Nicholas D. Adams, Joelle Lorraine Burgess, Dashyant Dhanak
Publikováno v:
Journal of Medicinal Chemistry. 50:4939-4952
Kinesin spindle protein (KSP), an ATPase responsible for spindle pole separation during mitosis that is present only in proliferating cells, has become a novel and attractive anticancer target with potential for reduced side effects compared to curre
Autor:
Thomas J. Carr, Dashyant Dhanak, David Haigh, George Burton, Victor K. Johnson, Pia Thommes, Glenn A. Hofmann, Robert T. Sarisky, Martin John Slater, Juili Lin-Goerke, Thomas W. Ku, Nigel R. Parry, Terry Kiesow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1930-1933
The SAR development is described for a series of N -acyl pyrrolidine inhibitors of the Hepatitis C virus RNA-dependent RNA polymerase, NS5B, from tractable Δ21 enzyme inhibitors to an example with antiviral activity in a cellular assay (HCV replicon
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
Enhancer of Zeste homolog 2 (EZH2) is the catalytic subunit of the polycomb repressive complex 2 (PRC2) responsible for the methylation of lysine 27 of histone 3 (H3K27) resulting in chromatin compaction and gene repression. Overexpression of EZH2 to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::071e22abdab964603a270023a2884297
https://doi.org/10.1016/b978-0-12-800206-3.00019-7
https://doi.org/10.1016/b978-0-12-800206-3.00019-7