Zobrazeno 1 - 10
of 111
pro vyhledávání: '"Daniel F, Ortwine"'
Autor:
Marc Kschonsak, Christine C Jao, Christopher P Arthur, Alexis L Rohou, Philippe Bergeron, Daniel F Ortwine, Steven J McKerrall, David H Hackos, Lunbin Deng, Jun Chen, Tianbo Li, Peter S Dragovich, Matthew Volgraf, Matthew R Wright, Jian Payandeh, Claudio Ciferri, John C Tellis
Publikováno v:
eLife, Vol 12 (2023)
The voltage-gated sodium (NaV) channel NaV1.7 has been identified as a potential novel analgesic target due to its involvement in human pain syndromes. However, clinically available NaV channel-blocking drugs are not selective among the nine NaV chan
Externí odkaz:
https://doaj.org/article/1b1793fee7d349608601029e46d0c8cd
Autor:
Christine C Jao, Marc Kschonsak, Christopher P Arthur, Alexis L Rohou, Philippe Bergeron, Daniel F Ortwine, Steven J McKerrall, David H Hackos, Lunbin Deng, Jun Chen, Tianbo Li, Peter S Dragovich, Matthew Volgraf, Matthew R Wright, Jian Payandeh, Claudio Ciferri, John C Tellis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fd282fdd94d6f54f454fbf1d90a6ee32
https://doi.org/10.7554/elife.84151.sa2
https://doi.org/10.7554/elife.84151.sa2
Autor:
Sultan Chowdhury, Christoph Martin Dehnhardt, Tao Sheng, Clint Young, Rainbow Kwan, Michael Scott Wilson, Jun Chen, Matthew Waldbrook, Dinah Misner, C. Lee Robinette, Rebecca M. Reese, Elaine Chang, Henry Verschoof, Tanja S. Zabka, Girish Bankar, Philippe Bergeron, Luis Sojo, Karen Nelkenbrecher, Daniel P. Sutherlin, Amy Kim, Ivan William Hemeon, Andrea Lindgren, Jae H. Chang, Alla Yurevna Zenova, Shaoyi Sun, Jonathan Maher, Shannon D. Shields, Jun Li, Daniel F. Ortwine, David H. Hackos, Zhiwei Xie, Thilo Focken, Charles J. Cohen, Richard T. Dean, Shannon Decker, Janette Mezeyova, Kuldip Khakh, Antonio G. DiPasquale, Chien-An Chen, Andrew D. White, Brian Safina, Jodie Pang, Qi Jia, Sophia Lin, Jean-Christophe Andrez, J. P. Johnson, Steven J. McKerrall
Publikováno v:
Journal of Medicinal Chemistry. 64:2953-2966
Nav1.7 is an extensively investigated target for pain with a strong genetic link in humans, yet in spite of this effort, it remains challenging to identify efficacious, selective, and safe inhibitors. Here, we disclose the discovery and preclinical p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1a8a9431d81bf8ca2eed0fbbfbb36905
https://doi.org/10.1021/acs.jmedchem.1c00049
https://doi.org/10.1021/acs.jmedchem.1c00049
Autor:
Martin O'Rourke, Nicholas Charles Ray, Thomas Gelzleichter, Leah Schutt, Ellen Ingalla, Neville James Mclean, Xiaojing Wang, Stephen Daly, Yingqing Ran, Jiangpeng Liao, Tommy Lai, Yu Zhong, Jun Liang, Sharada Labadie, Lori Friedman, Amy Sambrone, Jun Li, Robert A. Blake, Tao Wang, Liu Zhiguo, Birong Zhang, Steven J. Hartman, Jae H. Chang, Wei Zhou, Jane Guan, Vidhi Mody, Jonathan White, Fabien Roussel, Antonio G. DiPasquale, Jason R. Zbieg, Daniel F. Ortwine, Amy Young, James R. Kiefer, Maia Vinogradova, Simon Charles Goodacre, Deepak Sampath, Tracy Kleinheinz, Xiaoping Zheng, Jennifer M. Giltnane, Lorn Kategaya, Ingrid E. Wertz, Matthew Gill, Ciara Metcalfe, Siew Kuen Yeap, John S. Wai, Jason Oeh, Michelle Nannini
Publikováno v:
Journal of medicinal chemistry. 64(16)
Breast cancer remains a leading cause of cancer death in women, representing a significant unmet medical need. Here, we disclose our discovery efforts culminating in a clinical candidate, 35 (GDC-9545 or giredestrant). 35 is an efficient and potent s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee86fe3f8068fbb2ff9647a59eadb710
https://pubmed.ncbi.nlm.nih.gov/34251202
https://pubmed.ncbi.nlm.nih.gov/34251202
Autor:
Jodie Pang, Lunbin Deng, Girish Bankar, Jun Chen, Sultan Chowdhury, William R Proctor, Philippe Bergeron, Jennifer Vogt, Daniel F. Ortwine, Daniel P. Sutherlin, Jian Payandeh, Lilia Schumann, Shannon D. Shields, Christoph Martin Dehnhardt, Jae H. Chang, David H. Hackos, Elisa Ballini, Teresa Nguyen, Pengfei Ji, Glauco Tarozzo, Charles J. Cohen, Antonio G. DiPasquale, Kwong Wah Lai, Jonathan Maher, Kuldip Khakh, Steven J. McKerrall, Tania Chernov-Rogan, Wenfeng Liu, Brian Safina, Sophia Lin, Abid Hasan, J. P. Johnson
Publikováno v:
Journal of Medicinal Chemistry. 62:4091-4109
Using structure- and ligand-based design principles, a novel series of piperidyl chromane arylsulfonamide Nav1.7 inhibitors was discovered. Early optimization focused on improvement of potency through refinement of the low energy ligand conformation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::824349f727cab11e6b607d5268a59967
https://doi.org/10.1021/acs.jmedchem.9b00141
https://doi.org/10.1021/acs.jmedchem.9b00141
Autor:
Xiaojing Wang, Yanzhou Liu, Jun Liang, Shao-Xiong Luo, Jason R. Zbieg, Jun Li, Daniel F. Ortwine, Michael J. Lambrecht, Antonio G. DiPasquale
Publikováno v:
Organic & Biomolecular Chemistry. 17:9510-9513
Nucleophilic addition of Grignard reagents to tetrahydro-β-carboline (THC) N-sulfonyl N,S-acetal generates exclusively cis-1,3-disubstituted THCs with a unique 1,3-diaxial conformation. The stereochemical relationship of the 1,3-substituents was con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43b951d76a29ce9301ea83760fb1670c
https://doi.org/10.1039/c9ob01796h
https://doi.org/10.1039/c9ob01796h
Autor:
Brian S, Safina, Steven J, McKerrall, Shaoyi, Sun, Chien-An, Chen, Sultan, Chowdhury, Qi, Jia, Jun, Li, Alla Y, Zenova, Jean-Christophe, Andrez, Girish, Bankar, Philippe, Bergeron, Jae H, Chang, Elaine, Chang, Jun, Chen, Richard, Dean, Shannon M, Decker, Antonio, DiPasquale, Thilo, Focken, Ivan, Hemeon, Kuldip, Khakh, Amy, Kim, Rainbow, Kwan, Andrea, Lindgren, Sophia, Lin, Jonathan, Maher, Janette, Mezeyova, Dinah, Misner, Karen, Nelkenbrecher, Jodie, Pang, Rebecca, Reese, Shannon D, Shields, Luis, Sojo, Tao, Sheng, Henry, Verschoof, Matthew, Waldbrook, Michael S, Wilson, Zhiwei, Xie, Clint, Young, Tanja S, Zabka, David H, Hackos, Daniel F, Ortwine, Andrew D, White, J P, Johnson, C Lee, Robinette, Christoph M, Dehnhardt, Charles J, Cohen, Daniel P, Sutherlin
Publikováno v:
Journal of medicinal chemistry. 64(6)
Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::d744b2a5894fa87236be1caf92c75b8b
https://pubmed.ncbi.nlm.nih.gov/33682420
https://pubmed.ncbi.nlm.nih.gov/33682420
Autor:
Qi Jia, Jean-Christophe Andrez, Charles J. Cohen, Jae H. Chang, Kuldip Khakh, J. P. Johnson, Chien-An Chen, Jun Li, Karen Nelkenbrecher, Thilo Focken, Zhiwei Xie, Daniel F. Ortwine, Brian Safina, Michael Edward Grimwood, Andrew D. White, Christoph Martin Dehnhardt, Shannon Decker, Ivan William Hemeon, David H. Hackos, Sophia Lin, Jodie Pang, Luis Sojo, Girish Bankar, Andrea Lindgren, Matthew Waldbrook, Elaine Chang, C. Lee Robinette, Shaoyi Sun, Antonio G. DiPasquale, Tao Sheng, Clint Young, Rainbow Kwan, Benjamin D. Sellers, Sultan Chowdhury, Michael Scott Wilson, Lunbin Deng, Daniel P. Sutherlin, Alla Yurevna Zenova
Publikováno v:
Journal of Medicinal Chemistry. 62:908-927
Herein, we report the discovery and optimization of a series of orally bioavailable acyl sulfonamide NaV1.7 inhibitors that are selective for NaV1.7 over NaV1.5 and highly efficacious in in vivo models of pain and hNaV1.7 target engagement. An analys
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7f65c95248ff36af0807edf4a8f95cad
https://doi.org/10.1021/acs.jmedchem.8b01621
https://doi.org/10.1021/acs.jmedchem.8b01621
Autor:
Girish Bankar, Charles J. Cohen, Bowen Li, Kuldip Khakh, Sultan Chowdhury, Elaine Chang, Paul Robert Bichler, Christoph Martin Dehnhardt, Daniel P. Sutherlin, Jodie Pang, Michael D. Wilson, Yi Zhang, Zhiwei Xie, Matthew Waldbrook, C. Lee Robinette, Jae H. Chang, Karen Nelkenbrecher, Ivan William Hemeon, Alla Yurevna Zenova, Tao Sheng, Samuel J. Goodchild, Clint Young, Navjot Chahal, Rainbow Kwan, Daniel F. Ortwine, Brian Safina, Sophia Lin, Andrew D. White, Parisa Karimi Tari, Qi Jia, J. P. Johnson, Thilo Focken, Chien-An Chen, David H. Hackos, Shannon Decker, Noah G. Shuart, Luis Sojo, Christine Chabot, Shaoyi Sun, Michael Edward Grimwood
Publikováno v:
Journal of Medicinal Chemistry. 61:4810-4831
The sodium channel NaV1.7 has emerged as a promising target for the treatment of pain based on strong genetic validation of its role in nociception. In recent years, a number of aryl and acyl sulfonamides have been reported as potent inhibitors of Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::301a3d7aee1781be0e40a336f69ca411
https://doi.org/10.1021/acs.jmedchem.7b01826
https://doi.org/10.1021/acs.jmedchem.7b01826
Autor:
Steven W. Jones, Chang Liu, Daniel F. Ortwine, David H. Hackos, Maureen Beresini, Henry Verschoof, Tianbo Li, Steven J. McKerrall, Jun Chen, Daniel P. Sutherlin, Charles J. Cohen, Kuldip Khakh, Gang Lu, Tania Chernov-Rogan
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America
Significance Subtype-selective modulation of ion channels is often important, but extremely difficult to achieve for drug development. Using Nav1.7 as an example, we show that this challenge could be attributed to poor design in ion channel assays, w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a61efe267f7dcc33ea85b5750295e6b
http://europepmc.org/articles/PMC5789920
http://europepmc.org/articles/PMC5789920