Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Yisong Xiao"'
Autor:
Katherine L. Schutt, Katelyn A. Queen, Kira Fisher, Olivia Budington, Weifeng Mao, Wei Liu, Xiaohui Gu, Yisong Xiao, Fred Aswad, James Joseph, Jason Stumpff
Publikováno v:
Frontiers in Molecular Biosciences, Vol 11 (2024)
Background: The mitotic kinesin, KIF18A, is required for proliferation of cancer cells that exhibit chromosome instability (CIN), implicating it as a promising target for treatment of a subset of aggressive tumor types. Determining regions of the KIF
Externí odkaz:
https://doaj.org/article/cc433fd5932f40ad91df8b3c7b187486
Autor:
Schutt, Katherine L., Queen, Katelyn A., Fisher, Kira, Budington, Olivia, Weifeng Mao, Wei Liu, Xiaohui Gu, Yisong Xiao, Aswad, Fred, Joseph, James, Stumpff, Jason
Publikováno v:
Frontiers in Molecular Biosciences; 2024, p1-15, 15p
Autor:
James D. Joseph, Katherine Schutt, Kira Fisher, Katelyn Queen, Olivia Budington, Weifeng Mao, Wei Liu, Zhengqing Zhu, Xiangping Zhang, Yisong Xiao, Kunmin Lai, Xiaohui Gu, Jason Stumpff, Fred Aswad
Publikováno v:
Cancer Research. 83:4965-4965
Background: Chromosome instability (CIN), characterized by frequent and ongoing loss or gain of chromosome number, is commonly observed in tumor cells. Although long recognized as a vulnerability of cancer cells, potential CIN-selective therapeutic t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::34634a671a73d252a82829d41aa81ea8
https://doi.org/10.1158/1538-7445.am2023-4965
https://doi.org/10.1158/1538-7445.am2023-4965
Publikováno v:
AdvM @ ACM Multimedia
Deepfake, a well-known face forgery technique, has raised serious concerns about personal privacy and social media security. Therefore, a plenty of deepfake detection methods come out and achieve outstanding performance in the single dataset case. Ho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::51aee4d7dbb9edf8be153292749d700b
https://doi.org/10.1145/3475724.3483603
https://doi.org/10.1145/3475724.3483603
Autor:
Steve Magnuson, Michael Siu, Christopher A. Hurley, Mark Ultsch, Joseph P. Lyssikatos, Wade S. Blair, Rebecca Pulk, Paul Gibbons, Charles Eigenbrot, Vickie Tsui, Bing-Yan Zhu, Deepak Sampath, Liu Wendy, Kathy Barrett, S. Cyrus Khojasteh, Leslie Lee, Nico Ghilardi, Richard Pastor, Yisong Xiao, Megan Berry, Jane R. Kenny, Jacob Z. Chen, Hoa Le, Christine Chang, Haiying He
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5014-5021
The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2 inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed. Download : Downlo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::681fd99055683a4b0d3829fed9eaeb2f
https://doi.org/10.1016/j.bmcl.2013.06.008
https://doi.org/10.1016/j.bmcl.2013.06.008
Autor:
Wade S. Blair, Sue Sohn, Stanley Mark S, Pawan Bir Kohli, Leo Berezhkovskiy, Lawren C. Wu, James P. Driscoll, Charles Eigenbrot, Adam R. Johnson, Vickie Tsui, Birong Zhang, Paul Gibbons, Nico Ghilardi, Yingjie Lai, Jun Liang, Marya Liimatta, Amy Sambrone, Jeremy Murray, Young G. Shin, Jason Halladay, Yisong Xiao, Kathy Barrett, Christine Chang, Maureen Beresini, Steven Shia, Mark Ultsch, Bao Liang, Kapil Menghrajani, Jan Smith, Priscilla Mantik, Anne van Abbema, Steven Magnuson
Publikováno v:
European Journal of Medicinal Chemistry. 67:175-187
A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as psoriasis and inflammatory bowel diseases (IBD), by selective targeting of TYK2. Hit triage, following a high-throughput screen for TYK2 inhibitors, revealed pyri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff9840f93ecfc565558fed60291d4ac2
https://doi.org/10.1016/j.ejmech.2013.03.070
https://doi.org/10.1016/j.ejmech.2013.03.070
Autor:
Sue Sohn, Nico Ghilardi, Priscilla Mantik, Christine Chang, Mercedesz Balazs, Paul Gibbons, Jan Smith, Ivan Peng, Jason DeVoss, Bing-Yan Zhu, Kathy Barrett, Wade S. Blair, Yisong Xiao, Steven Shia, Birong Zhang, Jim Driscoll, Donnie Delarosa, Young G. Shin, Jeremy Murray, Steven Magnuson, Leo Berezhkovsky, Wenqian Yang, Anne van Abbema, Charles Eigenbrot, Lawren C. Wu, Adam R. Johnson, Pawan Bir Kohli, Vickie Tsui, Mark Ultsch, Jason Halladay, Amy Sambrone, Yingjie Lai, Joseph P. Lyssikatos, Yanzhou Liu, Kapil Menghrajani, Jun Liang, Judy Young
Publikováno v:
Journal of Medicinal Chemistry. 56:4521-4536
Herein we report our lead optimization effort to identify potent, selective, and orally bioavailable TYK2 inhibitors, starting with lead molecule 3. We used structure-based design to discover 2,6-dichloro-4-cyanophenyl and (1R,2R)-2-fluorocyclopropyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91486c8bd1e5cbb09b64ed7bef1646df
https://doi.org/10.1021/jm400266t
https://doi.org/10.1021/jm400266t
Autor:
Yisong Xiao, Yamin Zhang, Christine Tam, David A. Roberts, Lori Friedman, Adrian Kotey, Hartmut Koeppen, Antonio G. DiPasquale, Marcia Belvin, Jason Burch, Angela Oh, Weiru Wang, Karen Lyle, Jason Boggs, Lionel Rouge, Klaus P. Hoeflich, Robert Mintzer, Steven T. Staben, Amy E. Young, Jianwen A. Feng, Joachim Rudolph, Ching-ching Chua, Christopher E. Heise, Hai-Feng Cui
Publikováno v:
Journal of medicinal chemistry. 57(3)
Structure-based methods were used to design a potent and highly selective group II p21-activated kinase (PAK) inhibitor with a novel binding mode, compound 17. Hydrophobic interactions within a lipophilic pocket past the methionine gatekeeper of grou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::245fbcc6094e3c442d4f7457a0aa98fd
https://pubmed.ncbi.nlm.nih.gov/24432870
https://pubmed.ncbi.nlm.nih.gov/24432870
Autor:
Kathy Barrett, Paul Gibbons, Steven Shia, Jane R. Kenny, Mark Zak, Charles Ellwood, Sharada Labadie, Richard James Bull, Chris Hamman, Peter H. Crackett, Peter Gribling, Peter S. Dragovich, Scott Savage, Jiangpeng Liao, Jason DeVoss, Christine Chang, Paroma Chakravarty, Mercedesz Balazs, Wyne P. Lee, Tony Johnson, Rebecca Pulk, Michael F. T. Koehler, Gauri Deshmukh, Marya Liimatta, Janusz J. Kulagowski, Pawan Bir Kohli, Anne van Abbema, Austin John Reeve, Rohan Mendonca, Adam R. Johnson, Ignacio Aliagas, Simon Gaines, Charles Eigenbrot, Yisong Xiao, Nico Ghilardi, Jing Yang, Christopher A. Hurley, Philippe Bergeron, Wade S. Blair, Peter Hewitt, Stuart Ward, Eric Harstad, Micah Steffek, Barbara Avitabile-Woo, Stefan Gradl, Raman Narukulla, Savita Ubhayakar
Publikováno v:
Journal of medicinal chemistry. 56(11)
Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the imidazopyrrolopyridine series of JAK1 inhibitors. X-ray structures of a C-2 hydroxyethyl a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53d0d607376d7e1e01099fe1e9376df8
https://pubmed.ncbi.nlm.nih.gov/23659214
https://pubmed.ncbi.nlm.nih.gov/23659214
Autor:
Philippe Bergeron, Sharada Labadie, Nico Ghilardi, Jeremy Murray, Stuart Ward, Charles Eigenbrot, Pawan Bir Kohli, Scott Savage, Ling Xiao, Janusz J. Kulagowski, Wade S. Blair, Micah Steffek, Tony Johnson, Gauri Deshmukh, Emily J. Hanan, Chris Hamman, Mark Zak, Jiangpeng Liao, Michael F. T. Koehler, Kathy Barrett, Madeleine Rodriguez, Robert James Maxey, Jason DeVoss, Peter S. Dragovich, Rebecca Pulk, Steven Shia, Mark Ultsch, Rohan Mendonca, Anne van Abbema, Yisong Xiao, Zhonghua Lin, Patrick J. Lupardus, Tian Jin, Adam R. Johnson, Stefan Gradl, Christopher A. Hurley, Paul Gibbons, Jane R. Kenny, Marya Liimatta, Savita Ubhayakar, Eric Harstad, Christine Chang, Mercedesz Balazs, Peter Hewitt
Publikováno v:
Journal of medicinal chemistry. 55(13)
Herein we report the discovery of the C-2 methyl substituted imidazopyrrolopyridine series and its optimization to provide potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. The C-2 methyl substituted inhibitor 4 exhibited not
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d48cbc66dd34e22ab1d4c6150296c9f4
https://pubmed.ncbi.nlm.nih.gov/22698084
https://pubmed.ncbi.nlm.nih.gov/22698084