Zobrazeno 1 - 10
of 16
pro vyhledávání: '"C Lee, Robinette"'
Autor:
Girish Bankar, Samuel J. Goodchild, Sarah Howard, Karen Nelkenbrecher, Matthew Waldbrook, Michelle Dourado, Noah G. Shuart, Sophia Lin, Clint Young, Zhiwei Xie, Kuldip Khakh, Elaine Chang, Luis E. Sojo, Andrea Lindgren, Sultan Chowdhury, Shannon Decker, Michael Grimwood, Jean-Christophe Andrez, Christoph M. Dehnhardt, Jodie Pang, Jae H. Chang, Brian S. Safina, Daniel P. Sutherlin, James P. Johnson, Jr., David H. Hackos, C. Lee Robinette, Charles J. Cohen
Publikováno v:
Cell Reports, Vol 24, Iss 12, Pp 3133-3145 (2018)
Summary: Selective block of NaV1.7 promises to produce non-narcotic analgesic activity without motor or cognitive impairment. Several NaV1.7-selective blockers have been reported, but efficacy in animal pain models required high multiples of the IC50
Externí odkaz:
https://doaj.org/article/751235f9fe504fde8c6781b6215d87d8
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:
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:
Christoph Martin Dehnhardt, Karen Nelkenbrecher, Jean-Christophe Andrez, Zhiwei Xie, David H. Hackos, Michael Edward Grimwood, Jae H. Chang, Sultan Chowdhury, Clint Young, Charles J. Cohen, J. P. Johnson, Elaine Chang, Michelle Dourado, Kuldip Khakh, Noah G. Shuart, Jodie Pang, Matthew Waldbrook, C. Lee Robinette, Sarah Howard, Daniel P. Sutherlin, Girish Bankar, Luis Sojo, Andrea Lindgren, Shannon Decker, Brian Safina, Samuel J. Goodchild, Sophia Lin
Publikováno v:
Cell Reports, Vol 24, Iss 12, Pp 3133-3145 (2018)
Summary: Selective block of NaV1.7 promises to produce non-narcotic analgesic activity without motor or cognitive impairment. Several NaV1.7-selective blockers have been reported, but efficacy in animal pain models required high multiples of the IC50
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c4c353367cd516b2db1286adedfe344
https://doi.org/10.1016/j.celrep.2018.08.063
https://doi.org/10.1016/j.celrep.2018.08.063
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:
Charles J. Cohen, Brian Safina, Daniel P. Sutherlin, Michael Edward Grimwood, Thilo Focken, J. P. Johnson, Shifeng Liu, Maxim Dauphinais, Matthew Waldbrook, C. Lee Robinette, Girish Bankar, Ivan William Hemeon, Noah G. Shuart, Jae H. Chang, Sultan Chowdhury, David Bogucki, Luis Sojo, Clint Young, Rainbow Kwan, Paul Robert Bichler, Renata Oballa, Tarek S. Mansour, Sophia Lin, Christoph Martin Dehnhardt, Jodie Pang, Navjot Chahal
Publikováno v:
ACS Medicinal Chemistry Letters. 7:277-282
We report on a novel series of aryl sulfonamides that act as nanomolar potent, isoform-selective inhibitors of the human sodium channel hNaV1.7. The optimization of these inhibitors is described. We aimed to improve potency against hNaV1.7 while mini
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d2edc92a10b757ea1080ec9a9cb99aa
https://doi.org/10.1021/acsmedchemlett.5b00447
https://doi.org/10.1021/acsmedchemlett.5b00447
Autor:
Shaoyi, Sun, Qi, Jia, Alla Y, Zenova, Michael S, Wilson, Sultan, Chowdhury, Thilo, Focken, Jun, Li, Shannon, Decker, Michael E, Grimwood, Jean-Christophe, Andrez, Ivan, Hemeon, Tao, Sheng, Chien-An, Chen, Andy, White, David H, Hackos, Lunbin, Deng, Girish, Bankar, Kuldip, Khakh, Elaine, Chang, Rainbow, Kwan, Sophia, Lin, Karen, Nelkenbrecher, Benjamin D, Sellers, Antonio G, DiPasquale, Jae, Chang, Jodie, Pang, Luis, Sojo, Andrea, Lindgren, Matthew, Waldbrook, Zhiwei, Xie, Clint, Young, James P, Johnson, C Lee, Robinette, Charles J, Cohen, Brian S, Safina, Daniel P, Sutherlin, Daniel F, Ortwine, Christoph M, Dehnhardt
Publikováno v:
Journal of medicinal chemistry. 62(2)
Herein, we report the discovery and optimization of a series of orally bioavailable acyl sulfonamide Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::038f23a54877cc0c450b0a4b2689f99c
https://pubmed.ncbi.nlm.nih.gov/30499663
https://pubmed.ncbi.nlm.nih.gov/30499663
Autor:
Thilo, Focken, Sultan, Chowdhury, Alla, Zenova, Michael E, Grimwood, Christine, Chabot, Tao, Sheng, Ivan, Hemeon, Shannon M, Decker, Michael, Wilson, Paul, Bichler, Qi, Jia, Shaoyi, Sun, Clint, Young, Sophia, Lin, Samuel J, Goodchild, Noah G, Shuart, Elaine, Chang, Zhiwei, Xie, Bowen, Li, Kuldip, Khakh, Girish, Bankar, Matthew, Waldbrook, Rainbow, Kwan, Karen, Nelkenbrecher, Parisa, Karimi Tari, Navjot, Chahal, Luis, Sojo, C Lee, Robinette, Andrew D, White, Chien-An, Chen, Yi, Zhang, Jodie, Pang, Jae H, Chang, David H, Hackos, J P, Johnson, Charles J, Cohen, Daniel F, Ortwine, Daniel P, Sutherlin, Christoph M, Dehnhardt, Brian S, Safina
Publikováno v:
Journal of medicinal chemistry. 61(11)
The sodium channel Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::41b8d0a60c84d4f1a2c37587e6288037
https://pubmed.ncbi.nlm.nih.gov/29737846
https://pubmed.ncbi.nlm.nih.gov/29737846
Autor:
Girish, Bankar, Samuel J, Goodchild, Sarah, Howard, Karen, Nelkenbrecher, Matthew, Waldbrook, Michelle, Dourado, Noah G, Shuart, Sophia, Lin, Clint, Young, Zhiwei, Xie, Kuldip, Khakh, Elaine, Chang, Luis E, Sojo, Andrea, Lindgren, Sultan, Chowdhury, Shannon, Decker, Michael, Grimwood, Jean-Christophe, Andrez, Christoph M, Dehnhardt, Jodie, Pang, Jae H, Chang, Brian S, Safina, Daniel P, Sutherlin, James P, Johnson, David H, Hackos, C Lee, Robinette, Charles J, Cohen
Publikováno v:
Cell reports. 24(12)
Selective block of Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::24df3eb486dfed5a4642cc263e273e3f
https://pubmed.ncbi.nlm.nih.gov/30231997
https://pubmed.ncbi.nlm.nih.gov/30231997