Combination screen in multi-cell type tumor spheroids reveals interaction between aryl hydrocarbon receptor antagonists and E1 ubiquitin-activating enzyme inhibitor

Autor: Thomas S. Dexheimer, Nathan P. Coussens, Thomas Silvers, Eric M. Jones, Li Chen, Jianwen Fang, Joel Morris, Jeffrey A. Moscow, James H. Doroshow, Beverly A. Teicher

Publikováno v: SLAS Discovery, Vol 29, Iss 7, Pp 100186- (2024)

The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that regulates genes of drug transporters and metabolic enzymes to detoxify small molecule xenobiotics. It has a complex role in cancer biology, influencing both the progr

Externí odkaz: https://doaj.org/article/d5d6e57234014b9b957345d8f7354e31

Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space

Autor: Sara E. Kearney, Gergely Zahoránszky-Kőhalmi, Kyle R. Brimacombe, Mark J. Henderson, Caitlin Lynch, Tongan Zhao, Kanny K. Wan, Zina Itkin, Christopher Dillon, Min Shen, Dorian M. Cheff, Tobie D. Lee, Danielle Bougie, Ken Cheng, Nathan P. Coussens, Dorjbal Dorjsuren, Richard T. Eastman, Ruili Huang, Michael J. Iannotti, Surendra Karavadhi, Carleen Klumpp-Thomas, Jacob S. Roth, Srilatha Sakamuru, Wei Sun, Steven A. Titus, Adam Yasgar, Ya-Qin Zhang, Jinghua Zhao, Rodrigo B. Andrade, M. Kevin Brown, Noah Z. Burns, Jin K. Cha, Emily E. Mevers, Jon Clardy, Jason A. Clement, Peter A. Crooks, Gregory D. Cuny, Jake Ganor, Jesus Moreno, Lucas A. Morrill, Elias Picazo, Robert B. Susick, Neil K. Garg, Brian C. Goess, Robert B. Grossman, Chambers C. Hughes, Jeffrey N. Johnston, Madeleine M. Joullie, A. Douglas Kinghorn, David G.I. Kingston, Michael J. Krische, Ohyun Kwon, Thomas J. Maimone, Susruta Majumdar, Katherine N. Maloney, Enas Mohamed, Brian T. Murphy, Pavel Nagorny, David E. Olson, Larry E. Overman, Lauren E. Brown, John K. Snyder, John A. Porco, Fatima Rivas, Samir A. Ross, Richmond Sarpong, Indrajeet Sharma, Jared T. Shaw, Zhengren Xu, Ben Shen, Wei Shi, Corey R.J. Stephenson, Alyssa L. Verano, Derek S. Tan, Yi Tang, Richard E. Taylor, Regan J. Thomson, David A. Vosburg, Jimmy Wu, William M. Wuest, Armen Zakarian, Yufeng Zhang, Tianjing Ren, Zhong Zuo, James Inglese, Sam Michael, Anton Simeonov, Wei Zheng, Paul Shinn, Ajit Jadhav, Matthew B. Boxer, Matthew D. Hall, Menghang Xia, Rajarshi Guha, Jason M. Rohde

Publikováno v: ACS Central Science, Vol 4, Iss 12, Pp 1727-1741 (2018)

Externí odkaz: https://doaj.org/article/9f2975f36dd648f0b92b6e0f2b27c087

Discovery of Novel Small-Molecule Scaffolds for the Inhibition and Activation of WIP1 Phosphatase from a RapidFire Mass Spectrometry High-Throughput Screen

Autor: Victor Clausse, Yuhong Fang, Dingyin Tao, Harichandra D. Tagad, Hongmao Sun, Yuhong Wang, Surendra Karavadhi, Kelly Lane, Zhen-Dan Shi, Olga Vasalatiy, Christopher A. LeClair, Rebecca Eells, Min Shen, Samarjit Patnaik, Ettore Appella, Nathan P. Coussens, Matthew D. Hall, Daniel H. Appella

Publikováno v: ACS Pharmacology & Translational Science. 5:993-1006

Wild-type P53-induced phosphatase 1 (WIP1), also known as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a77d015aae85ddd0ddd8d9d272ae29f
https://doi.org/10.1021/acsptsci.2c00147

Complex Tumor Spheroids, a Tissue-Mimicking Tumor Model, for Drug Discovery and Precision Medicine

Autor: Beverly A. Teicher, Nathan P. Coussens, David Evans, Gurmeet Kaur

Publikováno v: SLAS Discovery. 26:1298-1314

Malignant tumors are complex tissues composed of malignant cells, vascular cells, structural mesenchymal cells including pericytes and carcinoma-associated fibroblasts, infiltrating immune cells, and others, collectively called the tumor stroma. The

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f64f935a3ab807a929d6a46aa11f76a
https://doi.org/10.1177/24725552211038362

Abstract 4555: Aryl-hydrocarbon receptor inhibitors in combination with anticancer agents, especially proteasome pathway inhibitors, in a complex spheroid screen using patient-derived cell lines can result in greater-than additive cytotoxicity

Autor: BEVERLY A. TEICHER, Jeffrey A. Moscow, Joel Morris, James H. Doroshow, Thomas S. Dexheimer, Nathan P. Coussens, Thomas Silvers, Rene Delosh, Zahra Davoudi, Russel Reinhart, Chad Ogle, Eric Jones

Publikováno v: Cancer Research. 83:4555-4555

Three aryl-hydrocarbon receptor (AhR) selective inhibitors, BAY-2416964, GNF351 and CH-223191, were assayed alone and in combination with 25 approved or investigational anticancer agents in complex spheroids including tumor cells, endothelial cells,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::35a28c3f7ec28caceaf45e1e4456fb5c
https://doi.org/10.1158/1538-7445.am2023-4555