Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Linghao Niu"'
Autor:
Andreas Kuglstatter, Allen John Lovey, Minh Diem Vu, John Menke, Parcharee Tivitmahaisoon, Douglas Roy, Vaishali Patel, Michael Soth, Javier DeVicente, Sue Jin, Linghao Niu, Stephen M. Lynch, Hongju Li, Calvin Yee, Saul Jaime-Figueroa, Johannes C. Hermann, Sandra Steiner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:2793-2800
Using a structure based design approach we have identified a series of indazole substituted pyrrolopyrazines, which are potent inhibitors of JAK3. Intramolecular electronic repulsion was used as a strategy to induce a strong conformational bias withi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47f780f500cb3dd415e00ba4d2d33eee
https://doi.org/10.1016/j.bmcl.2013.02.012
https://doi.org/10.1016/j.bmcl.2013.02.012
Autor:
R. Ursula Kammlott, Deborah Carol Reuter, Teresa Alejandra Trejo-Martin, Leyi Gong, Christophe Michoud, Andreas Kuglstatter, Patricia Tran, David Michael Goldstein, Yun-Chou Tan, Parcharee Tivitmahaisoon, Linghao Niu, Shao-Yong Wu, Sue Jin, Paul Weller, Gary Hsieh, Karin Ann Stein, Humberto Bartolome Arzeno, James Patrick Dunn, Ada Shao, Wylie Solang Palmer, J. Heather Hogg, Johannes C. Hermann, Kung-ching Chang, Bindu Goyal, Alam Jahangir, Cheryl Janson, Tania Silva, Christine Lukacs, Paul J. Wagner, Muzaffar Alam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1486-1492
A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and select
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b003a69164deb7db8c54e3d4d75bb7b
https://doi.org/10.1016/j.bmcl.2012.12.047
https://doi.org/10.1016/j.bmcl.2012.12.047
Autor:
Shirley Li, Kelly M. George, Shelley K. Gleason, Charles Wartchow, Binh Thanh Vu, Hong Qian, Ann C. Petersen, Qing-Fen Gan, Lin Gao, Gabriel Stephen Deems, Linghao Niu, Nanda Beatini, Johannes C. Hermann, Arjun Narayanan, John Menke, Nathan Robert Scott, Nancy-Ellen Haynes, Yingsi Chen
Publikováno v:
ACS Medicinal Chemistry Letters. 4:197-200
Organic impurities in compound libraries are known to often cause false-positive signals in screening campaigns for new leads, but organic impurities do not fully account for all false-positive results. We discovered inorganic impurities in our scree
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8ba9438c9107f86a17a7e7700489491
https://doi.org/10.1021/ml3003296
https://doi.org/10.1021/ml3003296
Autor:
Jim W. Barnett, Andreas Kuglstatter, Kyung Song, Armando G. Villaseñor, Linghao Niu, Simon W. Lee, David E. Shaw, Stan Tsing, Michelle F. Browner
Publikováno v:
The Journal of Immunology. 178:2641-2645
IL-1R-associated kinase (IRAK)4 plays a central role in innate and adaptive immunity, and is a crucial component in IL-1/TLR signaling. We have determined the crystal structures of the apo and ligand-bound forms of human IRAK4 kinase domain. These st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9fffe047704e2379c0394b880ca08635
https://doi.org/10.4049/jimmunol.178.5.2641
https://doi.org/10.4049/jimmunol.178.5.2641
Autor:
Mingyan Zhou, Andreas Kuglstatter, Preeti Yadava, Aruna Railkar, Johannes C. Hermann, Stephan Kirchner, Ying Peng, Linghao Niu, Christine Lukacs, Eric Chiao, Calvin Yee, Fernando Padilla, Daigen Xu, Matthew C. Lucas, Cheng Liao, Michelle Slade, David Michael Goldstein, Michael Soth, Pei-Yuan Hsu, Niala Bhagirath, John Menke, Joshua Kennedy-Smith, Liudmila Polonchuk
Publikováno v:
Journal of medicinal chemistry. 57(6)
Inhibition of spleen tyrosine kinase has attracted much attention as a mechanism for the treatment of cancers and autoimmune diseases such as asthma, rheumatoid arthritis, and systemic lupus erythematous. We report the structure-guided optimization o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9aafe6ed7b9994002fcfb297182da51
https://pubmed.ncbi.nlm.nih.gov/24520947
https://pubmed.ncbi.nlm.nih.gov/24520947
Publikováno v:
Blood. 95:3357-3362
The human granulocyte-macrophage colony-stimulating factor (GM-CSF) receptor consists of 2 glycoprotein subunits, GMR and GMRβ. GMR in isolation binds to GM-CSF with low affinity. GMRβ does not bind GM-CSF by itself, but forms a high-affinity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98171e79b511e9b1da435357e1c0d076
https://doi.org/10.1182/blood.v95.11.3357
https://doi.org/10.1182/blood.v95.11.3357
Publikováno v:
Blood. 94:3748-3753
Granulocyte-macrophage colony-stimulating factor (GM-CSF) is an important hematopoietic cytokine that exerts its effects by interaction with the GM-CSF receptor (GMR) on the surface of responsive cells. The GM-CSF receptor consists of two subunits: G
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c367c80f4b35eaefab83039979e5eb0
https://doi.org/10.1182/blood.v94.11.3748
https://doi.org/10.1182/blood.v94.11.3748
Publikováno v:
RNA. 5:751-763
The gene for RsuA, the pseudouridine synthase that converts U516 to pseudouridine in 16S ribosomal RNA of Escherichia coli, has been deleted in strains MG1655 and BL21/DE3. Deletion of this gene resulted in the specific loss of pseudouridine516 in bo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::300ec3d1725110226fdeb15935cd6a38
https://doi.org/10.1017/s1355838299990167
https://doi.org/10.1017/s1355838299990167
Autor:
Xiaochun Han, Yun-Chou Tan, Sue Jin, Paul J. Wagner, Alejandra Trejo, Parch Tivitmahaisoon, David Mark Rotstein, Bindu Goyal, Andreas Kuglstatter, Wylie Solang Palmer, Leyi Gong, Brian Wong, Patricia Tran, Alam Jahagir, Alice Chang, Joseph Dal Porto, Linghao Niu, Johaness Hermann, Fengrong Zuo, James Patrick Dunn, Karin Ann Stein, Heather Hogg, Muzaffar Alam, Ada Shao, David Michael Goldstein, Deborah Carol Reuter, Ferenc Makra, Gary Hsieh, Brad Loe, Lubov Filonova, Lubica Rapatova, Tania Silva
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(12)
A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was used to optimize the series resulting in a signifi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e1d571f35d6a4f78286cd06b8fa7d5d
https://pubmed.ncbi.nlm.nih.gov/23664880
https://pubmed.ncbi.nlm.nih.gov/23664880
Autor:
Ann F. Hoffman, Michael Soth, Cheng Liao, Mohammad Hekmat-Nejad, Pei-Yuan Hsu, Yang He, Seng-Lai Tan, John Menke, Hoangdung Ho, Linghao Niu, Stephen M. Lynch, Sandra Steiner, Ada Shao, Calvin Yee, Ramona Hilgenkamp, Dong-Qing Hu, Seth F. Harris, Andreas Kuglstatter, Michelle F. Browner, Johannes C. Hermann, Aruna Railkar, Sandra Frauchiger, Andrea Itano, Saul Jaime-Figueroa, Alan K. Kutach, Yongliang Sun, Alam Jahangir, Jim W. Barnett, Douglas Roy, David E. Shaw, Vaishali Patel, Than Hendricks, Pamela Berry, Minh Diem Vu, Muzaffar Alam, Sue Jin, Karl Frank, Sandra M. Wang, Robert Henningsen
Publikováno v:
Journal of medicinal chemistry. 56(1)
The Janus kinases (JAKs) are involved in multiple signaling networks relevant to inflammatory diseases, and inhibition of one or more members of this class may modulate disease activity or progression. We optimized a new inhibitor scaffold, 3-amido-5
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae25b0d3cce1e989701d774b6efbb4a6
https://pubmed.ncbi.nlm.nih.gov/23214979
https://pubmed.ncbi.nlm.nih.gov/23214979