Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Markian Stec"'
Autor:
Bradley J. Herberich, Tian Wu, Paul E. Hughes, Claire L. M. Jackson, Nobuko Nishimura, Nancy Zhang, Ryan Wurz, Douglas A. Whittington, Shon Booker, Sean Caenepeel, Tisha San Miguel, Jian Jiang, Anthony B. Reed, Adrian L. Smith, Seifu Tadesse, Brian A. Lanman, Andrew Tasker, Erin L. Mullady, John D. McCarter, Fang-Tsao Hong, Liping H. Pettus, Divesh Aidasani, Victor J. Cee, Ling Wang, Bin Wu, Mark H. Norman, Daniel J. Freeman, Kevin Yang, Longbin Liu, Leeanne Zalameda, Yunxin Y. Bo, Xiaochun Zhu, Kristin L. Andrews, Markian Stec, Nuria A. Tamayo, Raju Subramanian, Noel D'angelo
Publikováno v:
Journal of Medicinal Chemistry. 55:7796-7816
The phosphoinositide 3-kinase family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger which plays a critical role in important cellular functions such as metabolis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7379e5002efb24d810fb0e1f33a3641
https://doi.org/10.1021/jm300846z
https://doi.org/10.1021/jm300846z
Autor:
Kristin L. Andrews, Kevin Yang, Markian Stec, Tisha San Miguel, Ling Wang, John McCarter, Mark H. Norman, Shon Booker, Jian Jiang, Nan Zhang, Daniel J. Freeman, Erin L. Mullady, Hongyu Liao, Paul E. Hughes, Leeanne Zalameda, Sean Caenepeel, Raju Subramanian, Nuria A. Tamayo
Publikováno v:
Journal of Medicinal Chemistry. 54:5174-5184
N-(6-(6-Chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)benzo[d]thiazol-2-yl)acetamide (1) is a potent and efficacious inhibitor of PI3Kα and mTOR in vitro and in vivo. However, in hepatocyte and in vivo metabolism studies, 1 was found to undergo d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47a9feddc793ad895a56aaf047e435fd
https://doi.org/10.1021/jm2004442
https://doi.org/10.1021/jm2004442
Autor:
Mqhele Ncube, Lillian Liao, Rami Tamir, Yunxin Bo, Narender R. Gavva, James J. S. Treanor, Partha P. Chakrabarti, Markian Stec, Nuria A. Tamayo, Mark H. Norman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5118-5122
Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15df16ed448a11ca22b2d95e3c1e3dc3
https://doi.org/10.1016/j.bmcl.2008.07.112
https://doi.org/10.1016/j.bmcl.2008.07.112
Autor:
Nuria A. Tamayo, Shimin Xu, Michael G. Kelly, Duncan M. Smith, Ning Chen, Michelle Carmouche, Mark H. Norman, Martin H. Goldberg, James Davis, Christopher H. Fotsch, Clarence Hale, Ning Xi, Markian Stec, James W. Baumgartner, Premilla Arasasingham, Nianhe Han, Feng-Yin Hsieh, Qingyian Liu, Yunxin Bo, Anthony W. Bannon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1623-1627
The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Compounds from this set had binding and functional activities at MC4R less than 30 nM.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7e26bb6cb3766754fe8c0250af2dfad
https://doi.org/10.1016/j.bmcl.2005.01.060
https://doi.org/10.1016/j.bmcl.2005.01.060
Autor:
Joan Helmering, Fang-Tsao Hong, Mark H. Norman, Jiandong Zhang, Klaus Michelsen, Markian Stec, Nobuko Nishimura, Steven R. Jordan, Lewis D. Pennington, Rod Cupples, David J. St. Jean, Darren L. Reid, Clarence Hale, Gwyneth Van, Jie Chen, Seifu Tadesse, Roxanne Kunz, Nuria A. Tamayo, Steve F. Poon, Kevin Yang, Christopher H. Fotsch, Longbin Liu, David Lloyd, Glenn Sivits, Elizabeth J. Galbreath, Michael D. Bartberger, Kate Ashton, Samer Chmait
Publikováno v:
Journal of medicinal chemistry. 57(2)
In the previous report , we described the discovery and optimization of novel small molecule disruptors of the GK-GKRP interaction culminating in the identification of 1 (AMG-1694). Although this analogue possessed excellent in vitro potency and was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4d2a8943c3198375b234ab664a4fed0
https://pubmed.ncbi.nlm.nih.gov/24405213
https://pubmed.ncbi.nlm.nih.gov/24405213
Autor:
Partha P. Chakrabarti, Xianghong Wang, Narender R. Gavva, Hongyu Liao, Mark H. Norman, Nuria A. Tamayo, Dan Retz, Anthony W. Bannon, Elizabeth M. Doherty, Markian Stec, Sekhar Surapaneni, Rami Tamir
Publikováno v:
Journal of medicinal chemistry. 51(9)
Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clinical utility for the treatment of chronic nociceptive and neuropathic pain. We recently advanced a TRPV1 antagonist, 3 (AMG 517), into clinical trials as a new therapy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c40c3d2fe206f2a9d600977d27d0431b
https://pubmed.ncbi.nlm.nih.gov/18386885
https://pubmed.ncbi.nlm.nih.gov/18386885
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides
Autor:
Thomas Nixey, Rami Tamir, Narender R. Gavva, Mark H. Norman, Partha P. Chakrabarti, Robert M. Rzasa, Vellarkad N. Viswanadhan, Yunxin Bo, Ning Chen, Jiawang Zhu, Nobuko Nishimura, James J. S. Treanor, Christopher H. Fotsch, Vassil I. Ognyanov, Sekhar Surapaneni, Elizabeth M. Doherty, Markian Stec
Publikováno v:
Journal of medicinal chemistry. 50(15)
The vanilloid receptor-1 (VR1 or TRPV1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role as an integrator of multiple pain-producing stimuli. From a high-throughput screening assay, measuring calcium uptak
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7cfb18a5a5bacea5ac1afc790ad57e32
https://pubmed.ncbi.nlm.nih.gov/17585749
https://pubmed.ncbi.nlm.nih.gov/17585749
Autor:
James J. S. Treanor, Vassil I. Ognyanov, Liping H. Pettus, Christopher H. Fotsch, Sekhar Surapaneni, Anthony W. Bannon, Markian Stec, Mark H. Norman, Yunxin Bo, Ning Chen, Jiawang Zhu, James R. Falsey, Elizabeth M. Doherty, Narender R. Gavva, Robert M. Rzasa, Celia Dominguez, Jodie Katon, Thomas Nixey, Rami Tamir
Publikováno v:
Journal of medicinal chemistry. 50(15)
A series of novel 4-oxopyrimidine TRPV1 antagonists was evaluated in assays measuring the blockade of capsaicin or acid-induced influx of calcium into CHO cells expressing TRPV1. The investigation of the structure-activity relationships in the hetero
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3cd8eec48ea80d8e7c25b53fbe45391c
https://pubmed.ncbi.nlm.nih.gov/17585750
https://pubmed.ncbi.nlm.nih.gov/17585750
Autor:
Shimin Xu, Markian Stec, Mark H. Norman, Michael G. Kelly, Christopher H. Fotsch, Ning Xi, Clarence Hale, James W. Baumgartner
Publikováno v:
ChemInform. 35
A novel series of piperazines appended to a succinamide backbone were synthesized and found to have a high affinity for the melanocortin-4 receptor (IC(50)s ranging from
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e70093877e73bcf208ee8fc962abd06
https://doi.org/10.1002/chin.200418159
https://doi.org/10.1002/chin.200418159
Autor:
Elizabeth M. Doherty, Christopher Fotsch, Anthony W. Bannon, Yunxin Bo, Ning Chen, Celia Dominguez, James Falsey, Narender R. Gavva, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping Pettus, Robert M. Rzasa, Markian Stec, Sekhar Surapaneni, Rami Tamir, Jiawang Zhu, James J. S. Treanor, Mark H. Norman
Publikováno v:
Journal of Medicinal Chemistry; Jul2007, Vol. 50 Issue 15, p3515-3527, 13p