Zobrazeno 1 - 10
of 123
pro vyhledávání: '"Ernst, Schönbrunn"'
Autor:
Erik B. Faber, Luxin Sun, Jian Tang, Emily Roberts, Sornakala Ganeshkumar, Nan Wang, Damien Rasmussen, Abir Majumdar, Laura E. Hirsch, Kristen John, An Yang, Hira Khalid, Jon E. Hawkinson, Nicholas M. Levinson, Vargheese Chennathukuzhi, Daniel A. Harki, Ernst Schönbrunn, Gunda I. Georg
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-13 (2023)
Abstract Compared to most ATP-site kinase inhibitors, small molecules that target an allosteric pocket have the potential for improved selectivity due to the often observed lower structural similarity at these distal sites. Despite their promise, rel
Externí odkaz:
https://doaj.org/article/43490103b21742f1887f75facd34c438
Autor:
Erik B. Faber, Nan Wang, Kristen John, Luxin Sun, Henry L. Wong, David Burban, Rawle Francis, Defeng Tian, Kwon H. Hong, An Yang, Liming Wang, Mazen Elsaid, Hira Khalid, Nicholas M. Levinson, Ernst Schönbrunn, Jon E. Hawkinson, Gunda I. Georg
Publikováno v:
Journal of Medicinal Chemistry. 66:1928-1940
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e8f7407374916699833f89e391662359
https://doi.org/10.1021/acs.jmedchem.2c01731
https://doi.org/10.1021/acs.jmedchem.2c01731
Autor:
Yi Liao, Sean Chin Chan, Eric A. Welsh, Bin Fang, Luxin Sun, Ernst Schönbrunn, John M. Koomen, Derek R. Duckett, Eric B. Haura, Andrii Monastyrskyi, Uwe Rix
Publikováno v:
ACS Chemical Biology. 18:251-264
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3ddcc9b388b97530f774cf0574b653ed
https://doi.org/10.1021/acschembio.2c00587
https://doi.org/10.1021/acschembio.2c00587
Autor:
Bryce K. Allen, Saurabh Mehta, Stuart W. J. Ember, Jin-Yi Zhu, Ernst Schönbrunn, Nagi G. Ayad, Stephan C. Schürer
Publikováno v:
ACS Omega, Vol 2, Iss 8, Pp 4760-4771 (2017)
Externí odkaz:
https://doaj.org/article/8df1dfe0be9542f4a9457d8f0863abea
Autor:
Xianghong Guan, Narsihmulu Cheryala, Rezaul Md. Karim, Alice Chan, Norbert Berndt, Jun Qi, Gunda I. Georg, Ernst Schönbrunn
Publikováno v:
Journal of Medicinal Chemistry. 65:10441-10458
Bromodomain and extraterminal domain (BET) proteins are important regulators of gene transcription and chromatin remodeling. BET family members BRD4 and BRDT are validated targets for cancer and male contraceptive drug development, respectively. Due
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab74b365eaf0bfcd0748f0ae0b364609
https://doi.org/10.1021/acs.jmedchem.2c00453
https://doi.org/10.1021/acs.jmedchem.2c00453
Autor:
Jun Qi, A. Thomas Look, Kimberly Stegmaier, Brian J. Abraham, Martha L. Bulyk, Ernst Schönbrunn, John Easton, Olaf Wiest, Taylor R. Quinn, Melissa J. Bikowitz, Antonio R. Perez-Atayde, Amanda L. Robichaud, Amy Saur Conway, Ken Morita, Logan H. Sigua, Paul M.C. Park, Lily Maxham, Maya Mundada, Ying Shao, Anand G. Patel, Stephanie Nance, Noha A.M. Shendy, Luca Mariani, Neekesh V. Dharia, Deyao Li, Mark W. Zimmerman, Virangika K. Wimalasena, Tingjian Wang, Adam D. Durbin
Supplementary Data from EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::700913e64764f6e6c15c2df8eb0c5d30
https://doi.org/10.1158/2159-8290.22541228
https://doi.org/10.1158/2159-8290.22541228
Autor:
Jun Qi, A. Thomas Look, Kimberly Stegmaier, Brian J. Abraham, Martha L. Bulyk, Ernst Schönbrunn, John Easton, Olaf Wiest, Taylor R. Quinn, Melissa J. Bikowitz, Antonio R. Perez-Atayde, Amanda L. Robichaud, Amy Saur Conway, Ken Morita, Logan H. Sigua, Paul M.C. Park, Lily Maxham, Maya Mundada, Ying Shao, Anand G. Patel, Stephanie Nance, Noha A.M. Shendy, Luca Mariani, Neekesh V. Dharia, Deyao Li, Mark W. Zimmerman, Virangika K. Wimalasena, Tingjian Wang, Adam D. Durbin
Gene expression is regulated by promoters and enhancers marked by histone H3 lysine 27 acetylation (H3K27ac), which is established by the paralogous histone acetyltransferases (HAT) EP300 and CBP. These enzymes display overlapping regulatory roles in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61071f79f8085d7c8ad075581b3011bc
https://doi.org/10.1158/2159-8290.c.6549578.v1
https://doi.org/10.1158/2159-8290.c.6549578.v1
Autor:
Ernst Schönbrunn, Nicholas J. Lawrence, Gary W. Reuther, Harshani R. Lawrence, Cyril H. Benes, Conor C. Lynch, Patricia Greninger, Paula J. Cranfill, Jin-Yi Zhu, Marilena Tauro, Muhammad Ayaz, Steven Gunawan, Norbert Berndt, Que T. Lambert, Stuart W. Ember
Table S1: Crystallographic data collection and refinement statistics Table S2: Inhibitory activity against other BET bromodomains Table S3: Bromodomain profiling data Fig. S1: Detailed binding interactions of compounds 1 - 5 in BRD4-1 Fig. S2: Compar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3a8658e8c0c794a279fbf75d3faea43
https://doi.org/10.1158/1535-7163.22504383.v1
https://doi.org/10.1158/1535-7163.22504383.v1
Autor:
Ernst Schönbrunn, Nicholas J. Lawrence, Gary W. Reuther, Harshani R. Lawrence, Cyril H. Benes, Conor C. Lynch, Patricia Greninger, Paula J. Cranfill, Jin-Yi Zhu, Marilena Tauro, Muhammad Ayaz, Steven Gunawan, Norbert Berndt, Que T. Lambert, Stuart W. Ember
Synergistic action of kinase and BET bromodomain inhibitors in cell killing has been reported for a variety of cancers. Using the chemical scaffold of the JAK2 inhibitor TG101348, we developed and characterized single agents which potently and simult
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::174289931beab104a62e35bd2bf1cb33
https://doi.org/10.1158/1535-7163.c.6537717.v1
https://doi.org/10.1158/1535-7163.c.6537717.v1
Autor:
Ernst Schönbrunn, Nicholas J. Lawrence, Gary W. Reuther, Harshani R. Lawrence, Cyril H. Benes, Conor C. Lynch, Patricia Greninger, Paula J. Cranfill, Jin-Yi Zhu, Marilena Tauro, Muhammad Ayaz, Steven Gunawan, Norbert Berndt, Que T. Lambert, Stuart W. Ember
Table S4: Kinome profiling data (Microsoft Excel sheet) Table S5: Cell line screening data (Microsoft Excel sheet)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::229255a872f5f91718071196e1a1a877
https://doi.org/10.1158/1535-7163.22504377.v1
https://doi.org/10.1158/1535-7163.22504377.v1