Zobrazeno 1 - 10
of 71
pro vyhledávání: '"Brian K. Albrecht"'
Autor:
Alexander M. Taylor, Chris Bailey, Lisa D. Belmont, Robert Campbell, Nico Cantone, Alexandre Côté, Terry D. Crawford, Richard Cummings, Kevin DeMent, Martin Duplessis, Megan Flynn, Andrew C. Good, Hon-Ren Huang, Shivangi Joshi, Yves Leblanc, Jeremy Murray, Christopher G. Nasveschuk, Adrianne Neiss, Florence Poy, F. Anthony Romero, Peter Sandy, Yong Tang, Vickie Tsui, Laura Zawadzke, Robert J. Sims, James E. Audia, Steven F. Bellon, Steven R. Magnuson, Brian K. Albrecht, Andrea G. Cochran
Publikováno v:
Journal of medicinal chemistry. 65(16)
Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with acetyllysine, and therefore bromodomains have been targets for drug discovery efforts. Highly potent an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e88d18fd974b18b10231a436e2238a9
https://pubmed.ncbi.nlm.nih.gov/35930799
https://pubmed.ncbi.nlm.nih.gov/35930799
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb8bd700da48c22429c52efbf950d81b
https://pubmed.ncbi.nlm.nih.gov/32551003
https://pubmed.ncbi.nlm.nih.gov/32551003
Autor:
Shumei Wang, Peter Sandy, Christopher G. Nasveschuk, Terry Crawford, Brian K. Albrecht, Andrea G. Cochran, Steffan Vartanian, Hon-Ren Huang, Vickie Tsui, David Stokoe, Steve Bellon, Yong Tang, E. Megan Flynn, Jian Wang, James R. Kiefer, Jeremy Murray, F. Anthony Romero, Laura Zawadzke, Michael C. Hewitt, Martin Duplessis, Alexander M. Taylor, Eneida Pardo, Alexandre Côté, Steven Magnuson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:3534-3541
Bromodomain-containing protein 9 (BRD9), an epigenetic "reader" of acetylated lysines on post-translationally modified histone proteins, is upregulated in multiple cancer cell lines. To assess the functional role of BRD9 in cancer cell lines, we iden
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8525424a9e42e8118660fc4dcf374c9
https://doi.org/10.1016/j.bmcl.2017.05.063
https://doi.org/10.1016/j.bmcl.2017.05.063
Autor:
Arianne Neiss, Martin Duplessis, Hariharan Jayaram, Shumei Wang, F. Anthony Romero, Christopher G. Nasveschuk, Daniel J. Burdick, James E. Audia, Terry Crawford, Steve Bellon, Hon-Ren Huang, Zhaowu Xu, Yongyun Wang, Ying Jiang, Michael C. Hewitt, Jeremy Murray, Andrea G. Cochran, Peter Sandy, Yong Tang, Brian K. Albrecht, E. Megan Flynn, James R. Kiefer, Archana Bommi-Reddy, Jian Wang, Laura Zawadzke, Shivangi Joshi, Vickie Tsui, Xiaoqin Zhu, Alexander M. Taylor, Robert J. Sims, Eneida Pardo, Alexandre Côté, Steven Magnuson, Richard T. Cummings
Publikováno v:
ACS Medicinal Chemistry Letters. 8:737-741
The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of cat eye syndrome chromosome region can
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34adc0dbe643caf51d004a4e038645f9
https://doi.org/10.1021/acsmedchemlett.7b00132
https://doi.org/10.1021/acsmedchemlett.7b00132
Autor:
Srividya Balasubramanian, Robert K. Campbell, Patrick Trojer, Christina O. Lee, Jon R. Wilson, Emmanuel Normant, Les A. Dakin, Martin Duplessis, Brian K. Albrecht, Jean-Christophe Harmange, Rishi G. Vaswani, James E. Audia, Priyadarshini Iyer, Andrew Simon Cook, Neil Justin, Steven J. Gamblin, Nico Cantone, Andrew C. Good, Feng Zhao, Richard T. Cummings, Steven F. Bellon, Christopher G. Nasveschuk, Shuyang Chen, Ying Zhang, Victor S. Gehling
Publikováno v:
Journal of Medicinal Chemistry. 59:9928-9941
Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of PRC2 function correlates with certain malignancies and poor prog
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3b439dd2f817b39a50f28ca2f51086f0
https://doi.org/10.1021/acs.jmedchem.6b01315
https://doi.org/10.1021/acs.jmedchem.6b01315
Autor:
Karen Rex, Douglas A. Whittington, David Bauer, Steven F. Bellon, Jean-Christophe Harmange, Martin A. Broome, Alessandro Boezio, Christiane Boezio, Karina R. Vaida, Deborah Choquette, Isabelle Dussault, Katrina W. Copeland, Emily A. Peterson, Yohannes Teffera, Roman Shimanovich, Brian K. Albrecht, Richard T. Lewis, Michele Potashman, Jingzhou Liu, Julia Lohman, Angela Coxon, Min-Hwa Jasmine Lin, Satoko Hirai
Publikováno v:
Journal of Medicinal Chemistry. 59:2328-2342
Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of compound 23 (AM
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d16401f5e9358f2456fce2725cd044c7
https://doi.org/10.1021/acs.jmedchem.5b01716
https://doi.org/10.1021/acs.jmedchem.5b01716
Autor:
Robert M. Campbell, Yves Leblanc, James E. Audia, Jennifer A. Mertz, Brian K. Albrecht, Michael R. Cooper, Jeffrey G. Supko, Emmanuel Normant, Florence Poy, Christopher G. Nasveschuk, Richard T. Cummings, Michael C. Hewitt, Adrianne Neiss, Victor S. Gehling, Louise Bergeron, Jean-Christophe Harmange, Peter Sandy, Michael O'Meara, Alexander M. Taylor, Robert J. Sims, Nico Cantone, Eneida Pardo, Alexandre Côté, Shivangi Joshi, Hariharan Jayaram, Rishi G. Vaswani, Steve Bellon
Publikováno v:
Journal of Medicinal Chemistry. 59:1330-1339
In recent years, inhibition of the interaction between the bromodomain and extra-terminal domain (BET) family of chromatin adaptors and acetyl-lysine residues on chromatin has emerged as a promising approach to regulate the expression of important di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a9c61f62ece4a112dbbc1ba0de53887
https://doi.org/10.1021/acs.jmedchem.5b01882
https://doi.org/10.1021/acs.jmedchem.5b01882
Autor:
Shumei Wang, Vickie Tsui, Terry D. Crawford, James E. Audia, Daniel J. Burdick, Maureen H. Beresini, Alexandre Côté, Richard Cummings, Martin Duplessis, E. Megan Flynn, Michael C. Hewitt, Hon-Ren Huang, Hariharan Jayaram, Ying Jiang, Shivangi Joshi, Jeremy Murray, Christopher G. Nasveschuk, Eneida Pardo, Florence Poy, F. Anthony Romero, Yong Tang, Alexander M. Taylor, Jian Wang, Zhaowu Xu, Laura E. Zawadzke, Xiaoyu Zhu, Brian K. Albrecht, Steven R. Magnuson, Steve Bellon, Andrea G. Cochran
Publikováno v:
Journal of medicinal chemistry. 61(20)
The biological functions of the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1(1,2)) remain unknown, although TAF1 has been identified as a potential target for oncology research. Here, we describe the discovery of a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::608b00b850e4a2287fb36f7aa68c18f2
https://pubmed.ncbi.nlm.nih.gov/30289257
https://pubmed.ncbi.nlm.nih.gov/30289257
Autor:
Jennifer A. Mertz, Michael C. Hewitt, Hari Jayaram, Yves Leblanc, Richard T. Cummings, Robert J. Sims, Eneida Pardo, Alexandre Côté, Alex M. Taylor, Christopher G. Nasveschuk, Jeremy W. Setser, Brian K. Albrecht, Steve Bellon, Jean-Christophe Harmange, James E. Audia, Jose M. Lora, Florence Poy, Shivangi Joshi, Rishi G. Vaswani, Yong Tang, Peter Sandy, Victor S. Gehling, Adrianne Neiss
Publikováno v:
ACS Medicinal Chemistry Letters. 7:145-150
Inhibition of the bromodomains of the BET family, of which BRD4 is a member, has been shown to decrease myc and interleukin (IL) 6 in vivo, markers that are of therapeutic relevance to cancer and inflammatory disease, respectively. Herein we report s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90d678aa93a9be92a8c569f477f58989
https://doi.org/10.1021/ml500411h
https://doi.org/10.1021/ml500411h
Autor:
Jane L. Grogan, Ruina Li, Edna F. Choo, Sarah M. Bronner, Maureen Beresini, Jonathan Maher, Patrick Cyr, Yingjie Li, Thomas Hunsaker, Brian K. Albrecht, Colin Masui, Kevin R Clark, Yingqing Ran, Jeremy Murray, Terry Crawford, Xiaorong Liang, Fei Wang, F. Anthony Romero, Xiaocang Wei, Alexander M. Taylor, Georgia Hatzivassiliou, Kyle Clagg, Kwong Wah Lai, Karen E. Gascoigne, Le An, Steven Magnuson, Mark Merchant, John S. Wai, Zhongguo Chen, Jiangpeng Liao, Vickie Tsui, Emily Chan, Kevin X. Chen, Wenfeng Liu, Wei Huang, Dong Yu, Stefan G. Koenig, Susan Kaufman, Xiaoyu Zhu, Gladys de Leon Boenig, Justin Ly, Denise E. de Almeida Nagata, Bing-Yan Zhu
Publikováno v:
Journal of medicinal chemistry. 60(22)
Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderately potent a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4920e6fdb48509b8406537a8dcd45287
https://pubmed.ncbi.nlm.nih.gov/28892380
https://pubmed.ncbi.nlm.nih.gov/28892380