Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Jianhua Chao"'
Autor:
Justin A. Caravella, Daliya Banerjee, Noel A. Powell, Jason D. Fontenot, Andres McKenzie, Istvan J. Enyedy, Victor Sukbong Hong, Douglas Marcotte, Laura Silvian, Jianhua Chao, Kurt Van Vloten
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2459-2463
RORγ plays a critical role in controlling a pro-inflammatory gene expression program in several lymphocyte lineages including T cells, γδ T cells, and innate lymphoid cells. RORγ-mediated inflammation has been linked to susceptibility to Crohn's
Autor:
Robert H. Scannevin, Geoffrey O. Gillard, John Anderson, Jianhua Chao, David J. Huss, Jason D. Fontenot, Brian Collette
Publikováno v:
Journal of Neuroimmunology. 283:74-85
Fumarate-containing pharmaceuticals are potent therapeutic agents that influence multiple cellular pathways. Despite proven clinical efficacy, there is a significant lack of data that directly defines the molecular mechanisms of action of related, ye
Autor:
Lin Zhang, Annie Raditsis, Istvan J. Enyedy, Jianhua Chao, Ishchenko Alexey, Brian Elenbaas, Laura Silvian, Jer Hong Chong, Victor Sukbong Hong, Douglas Marcotte, Junhua Fan, Aparna Hingway, Jean-Yves Le Brazidec, Latika Singh
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:474-480
PIM kinases are implicated in variety of cancers by promoting cell survival and proliferation and are targets of interest for therapeutic intervention. We have identified a low-nanomolar pan-PIM inhibitor (PIM1/2/3 potency 5:14:2nM) using structure b
Autor:
Matvey E. Lukashev, Victor Hong, Hernan Cuervo, Ping Jin, Douglas Marcotte, Alexey Lugovskoy, Valérie Vivat, C Hession, Deping Wang, Joachim Kraemer, Jean-Christophe Hus, Chris Bergeron, Dominique Roecklin, Weike Zeng, Malgorzata M. Vecchi, Dirk Winkler, Istvan J. Enyedy, Cédric Atmanene, Laura Silvian, Andres McKenzie, Jianhua Chao
Publikováno v:
Bioorganic & Medicinal Chemistry. 21:4011-4019
Keap1 binds to the Nrf2 transcription factor to promote its degradation, resulting in the loss of gene products that protect against oxidative stress. While cell-active small molecules have been identified that modify cysteines in Keap1 and effect th
Autor:
Victor Hong, Andres McKenzie, Jianhua Chao, Erin K Harning, Ping Li, Francis Burrows, Jiandong Shi, Rachel Lough, Theodore J. Yun, Marcus F. Boehm, Gerardo Ibanez, Ryan Lamer, Kenneth W Weichert, Christina Boykin, Anthone W. Dunah, Istvan J. Enyedy, Christine Ambrose, Noelito Timple, Ryan Van de Water, Marilyn R. Kehry, Marco A. Biamonte, Joseph Arndt, Jeffrey Thompson, Srinivas Rao Kasibhatla, Cristina M Sandoval, Karen Lundgren, Kevin Hong, Pamela A. Snodgrass-Belt, Sarah A. Bixler
Publikováno v:
Journal of Medicinal Chemistry. 55:7786-7795
Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol (EC144), is a second generation inhibitor of heat shock protein 90 (Hsp90) and is substantially more potent in vitro
Autor:
Lin Zhang, Art Taveras, Jer-Hong Chong, Jianhua Chao, Min Teng, Nuzhat Pathan, Angela Pasis, Betty Tam, Jean-Yves Le Brazidec, Michael J. Choi, Junhua Fan, Leona E. Ling, Deping Wang, Christina Boykin, Cheryl Black, Tony Li, Khanh Nguyen, Shuo Zhao, Laura Silvian, Gisela Claassen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2070-2074
Since the early 2000s, the Aurora kinases have become major targets of oncology drug discovery particularly Aurora-A and Aurora-B kinases (AKA/AKB) for which the selective inhibition in cells lead to different phenotypes. In addition to targeting the
Autor:
Andrew J. King, David Rodríguez, Zhengfeng Jiang, Kenji Kozuka, Jeremy S. Caldwell, Lily Hu, Limin He, Qumber H. Jafri, Samantha Koo-McCoy, Rakesh K. Jain, Ying He, Matthew Siegel, Jianhua Chao, Patricia Finn
Publikováno v:
Gastroenterology. 154:S-1176
Publikováno v:
Tetrahedron Letters. 50:5005-5008
Novel highly substituted hydroxy thiophene motifs were designed and synthesized as viable amido phenol and sulfonamido phenol bioisosteres. Hydroxy group-directed regioselective bromination and palladium-catalyzed amination of thienyl bromide via Buc
Autor:
Jay S. Fine, James Fossetta, Minglang Wu, Waldemar Gonsiorek, Carol Terminelli, Richard W. Bond, Daniel Lundell, J. Robert Merritt, Aki Cynthia J, Jianhua Chao, Zhenmin He, R. William Hipkin, James Jakway, Younong Yu, Taveras Arthur G, Diane Rindgen, Gaifa Lai, Rosemary Mayer-Ezel, Xuedong Fan, Michael P. Dwyer, Chao Jianping, Hongchen Qiu, Biju J. Purakkattle, Hong Bian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1318-1322
Comprehensive SAR studies were undertaken in the 3,4-diaminocyclobut-3-ene-1,2-dione class of CXCR2/CXCR1 receptor antagonists to explore the role of the heterocycle on chemokine receptor binding affinities, functional activity, as well as oral expos
Autor:
Art Taveras, Daniel Lundell, Xuedong Fan, James Fossetta, Michael P. Dwyer, Jianhua Chao, Hongchen Qiu, M. Motasim Billah, R. William Hipkin, Waldemar Gonsiorek, James Jakway, David Hesk, Gregory Deno
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 322:477-485
In neutrophils, growth-related protein-alpha (CXCL1) and interleukin-8 (CXCL8), are potent chemoattractants (Cytokine 14:27-36, 2001; Biochemistry 42:2874-2886, 2003) and can stimulate myeloperoxidase release via activation of the G protein-coupled r