Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Jacob I Stuckey"'
Autor:
Hagar F. Moussa, Daniel Bsteh, Ramesh Yelagandula, Carina Pribitzer, Karin Stecher, Katarina Bartalska, Luca Michetti, Jingkui Wang, Jorge A. Zepeda-Martinez, Ulrich Elling, Jacob I. Stuckey, Lindsey I. James, Stephen V. Frye, Oliver Bell
Publikováno v:
Nature Communications, Vol 10, Iss 1, Pp 1-12 (2019)
Polycomb Repressive Complexes PRC1 and PRC2 catalyse distinct chromatin modifications to promote gene silencing. Here the authors use reversible tethering of Polycomb proteins to ectopic sites in mouse ESCs and find that canonical but not variant PRC
Externí odkaz:
https://doaj.org/article/c3dcbf63ea4b486cbed795c1f715237f
Autor:
Ingrid Almeciga, Costa Salojin, Julian Levell, Anna Gardberg, Patrick Trojer, Lei Cui, Richard D. Cummings, Jennifer Rocnik, Valerie Vivat, Jacob I. Stuckey, Nico Cantone, Florence Poy, Jonathan E. Wilson, Jeffrey Lauer
Publikováno v:
Journal for ImmunoTherapy of Cancer, Vol 9, Iss Suppl 2 (2021)
BackgroundTREX1 is an exonuclease that functions as a negative regulator of innate immunity. TREX1 controls dsDNA sensing in tumor and immune cells by preventing aberrant dsDNA buildup that triggers STING-mediated Type 1 Interferon (IFN) induction le
Autor:
Venita G. Watson, Richard T. Cummings, Victor S. Gehling, Andrew C. Good, Brian K. Albrecht, Priyanka Sawant, John P. McGrath, James E. Audia, Jean-Christophe Harmange, Priyadarshini Iyer, Rishi G. Vaswani, Srividya Balasubramanian, Alexandre Côté, Avinash Khanna, Steven Bellon, Francois Brucelle, Julian Levell, Patrick Trojer, Jacob I. Stuckey, Martin Duplessis
Publikováno v:
ACS Med Chem Lett
[Image: see text] Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the
Autor:
Jorge A. Zepeda-Martinez, Luca Michetti, Lindsey I. James, Daniel Bsteh, Karin Stecher, Ulrich Elling, Katarina Bartalska, Stephen V. Frye, Hagar F. Moussa, Jingkui Wang, Jacob I. Stuckey, Oliver Bell, Ramesh Yelagandula, Carina Pribitzer
Publikováno v:
Nature Communications
Nature Communications, Vol 10, Iss 1, Pp 1-12 (2019)
Nature Communications, Vol 10, Iss 1, Pp 1-12 (2019)
Polycomb group (PcG) proteins play critical roles in the epigenetic inheritance of cell fate. The Polycomb Repressive Complexes PRC1 and PRC2 catalyse distinct chromatin modifications to enforce gene silencing, but how transcriptional repression is p
Autor:
Catherine Simpson, Jacqueline Norris-Drouin, Ryan Pasca, Nancy Cheng, Lindsey I. James, Jacob I. Stuckey, Junghyun Lee, Kenneth H. Pearce, Bradley M. Dickson, Stephanie H. Cholensky, Stephen V. Frye
Publikováno v:
Journal of Medicinal Chemistry. 59:8913-8923
To better understand the contribution of methyl-lysine (Kme) binding proteins to various disease states, we recently developed and reported the discovery of 1 (UNC3866), a chemical probe that targets two families of Kme binding proteins, CBX and CDY
Autor:
Valérie Vivat, Patrick Trojer, Jehrod Burnett Brenneman, James E. Audia, Jennifer A. Mertz, Victor S. Gehling, Shilpi Arora, Ashwin Ramakrishnan, Richard T. Cummings, Ludivine Moine, Jacob I. Stuckey, Robert J. Sims, Nico Cantone, Alexandre Côté, Avinash Khanna, Julian Levell
Publikováno v:
The Journal of Biological Chemistry
The histone methyltransferase EZH2 has been the target of numerous small-molecule inhibitor discovery efforts over the last 10+ years. Emerging clinical data have provided early evidence for single agent activity with acceptable safety profiles for f
Autor:
Kelsey N. Lamb, Daniel Bsteh, Stephen V. Frye, Hagar F. Moussa, Lindsey I. James, Sarah N. Dishman, Jacob I. Stuckey, Benjamin Z. Stanton, Huitao Fan, Jacqueline L. Norris, Dongxu Li, Mark T. Bedford, Cari A. Sagum, Terry P. Kenakin, Dmitri Kireev, Gang Greg Wang, Oliver Bell, Jingkui Wang, Stephanie H. Cholensky
Publikováno v:
SSRN Electronic Journal
Polycomb-directed repression of gene expression is frequently misregulated in human diseases. A quantitative and target-specific cellular assay was utilized to discover the first potent positive allosteric modulator (PAM), UNC4976, of nucleic acid bi
Autor:
Stephen V. Frye, Brian D. Strahl, Brian E. Watts, Mark T. Bedford, Eidarus Salah, Junghyun L. Suh, Lindsey I. James, Cari A. Sagum, Yi An, Dmitri Kireev, A. Ali Khan, Jacob I. Stuckey, Alexander T. Adams, Jacqueline Norris-Drouin, Bradley M. Dickson, Stephanie H. Cholensky, S. Mathea, Stefan Knapp
Multivalent binding is an efficient means to enhance the affinity and specificity of chemical probes targeting multidomain proteins in order to study their function and role in disease. While the theory of multivalent binding is straightforward, phys
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7604d7529092bfe3747ef9f87d4ecf27
https://europepmc.org/articles/PMC5937704/
https://europepmc.org/articles/PMC5937704/
Autor:
Brandi M. Baughman, Nancy Cheng, Masoud Vedadi, Jacob I. Stuckey, Bradley M. Dickson, Stephen V. Frye, Yanli Liu, Stephanie H. Cholensky, Karynne Black, Samantha G. Pattenden, Su Qin, Wolfram Tempel, Xi Ping Huang, Fengling Li, Peter Brown, Lindsey I. James, Katherine G. Huber, Jinrong Min, Bryan L. Roth, Cheryl H. Arrowsmith, Cari A. Sagum, Guillermo A. Senisterra, Jacqueline L. Norris, Mark T. Bedford
Publikováno v:
Nature chemical biology
We report the design and characterization of UNC3866, a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. Polycomb CBX proteins regulate gene expression by targeting Polycomb repressiv
Autor:
Peter Brown, Masoud Vedadi, Stephen V. Frye, Fengling Li, Jacqueline Norris-Drouin, Beau M. Worley, Stephanie H. Cholensky, Kimberly D. Barnash, Jacob I. Stuckey, Cheryl H. Arrowsmith, Lindsey I. James
Publikováno v:
ACS combinatorial science. 19(3)
The function of EED within Polycomb repressive complex 2 (PRC2) is mediated by a complex network of protein-protein interactions. Allosteric activation of PRC2 by binding of methylated proteins to embryonic ectoderm development (EED) aromatic cage is