Zobrazeno 1 - 10
of 36
pro vyhledávání: '"David J. Unett"'
Autor:
Thuy-Anh Tran, Bryan Kramer, Young-Jun Shin, Quyen-Quyen Do, Brett Ullman, Vasudeva Sagi, John W. Adams, Yunqing Shi, Hsin-Hui Shu, David J. Unett, Joel Gatlin, Michael E. Morgan, Jaimie Reuter, Anthony Blackburn, Carleton R. Sage, Graeme Semple
Publikováno v:
Results in Chemistry, Vol 4, Iss , Pp 100518- (2022)
The design of a new series of β3-Adrenergic receptor (β3-AdrR) antagonists is described. The use of a spiro building block in the core of the molecule provided novel compounds with reduced aromaticity and antagonist activity at the human β3-AdrR.
Externí odkaz:
https://doaj.org/article/6533cc49f4b54ba9916eb28cfabb9af8
Autor:
Xiaohua Chen, Ibragim Gaidarov, John W. Adams, John Frazer, Graeme Semple, Todd Anthony, Joel Gatlin, David J. Unett
Publikováno v:
Cellular Signalling. 50:9-24
Angiotensin (1-7) has been reported to be a ligand for the GPCR MAS1. Small molecule MAS1 modulators have also been recently characterized. Aside from convincing evidence for MAS1 activation of Gq signaling, little is known about MAS1 mediated signal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88d0aa4d723d7b93b7b5c2b7357d7616
https://doi.org/10.1016/j.cellsig.2018.06.007
https://doi.org/10.1016/j.cellsig.2018.06.007
Autor:
Sangdon Han, David J. Unett, Michelle Solomon, Ibragim Gaidarov, Joel Gatlin, Xiaohua Chen, Graeme Semple, Todd Anthony, David Mills
Publikováno v:
Pharmacological Research. 131:185-198
GPR84 is an orphan G-protein coupled receptor, expressed on monocytes, macrophages and neutrophils and is significantly upregulated by inflammatory stimuli. The physiological role of GPR84 remains largely unknown. Medium chain fatty acids (MCFA) acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88250de6e3a560c70af8b8635c3a0165
https://doi.org/10.1016/j.phrs.2018.02.021
https://doi.org/10.1016/j.phrs.2018.02.021
Autor:
Michelle Solomon, Lars Thoresen, Robert M. Jones, Andrew J. Grottick, David J. Unett, Abu J.M. Sadeque, Chuan Chen, Ibragim Gaidarov, Hussien A. Al-Shamma, Jayant Thatte, Graeme Semple, Jae-Kyu Jung, Amin Usmani, Jeremy Barden, Xiuwen Zhu, Woo Hyun Yoon, Sangdon Han, Christopher Ronald J
Publikováno v:
ACS Medicinal Chemistry Letters. 8:1309-1313
The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6 was efficacious in a rat model of osteoarthritis pain following oral administration and, in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f1f3e8c8d79ed5129b2137300ee1326f
https://doi.org/10.1021/acsmedchemlett.7b00396
https://doi.org/10.1021/acsmedchemlett.7b00396
Autor:
Albert, Ren, Xiuwen, Zhu, Konrad, Feichtinger, Juerg, Lehman, Michelle, Kasem, Thomas O, Schrader, Amy, Wong, Huong, Dang, Minh, Le, John, Frazer, David J, Unett, Andrew J, Grottick, Kevin T, Whelan, Michael E, Morgan, Carleton R, Sage, Graeme, Semple
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(5)
A series of potential new 5-HT
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::336846d4b5b2aaf0998d8ed90bb4d763
https://pubmed.ncbi.nlm.nih.gov/31952960
https://pubmed.ncbi.nlm.nih.gov/31952960
Autor:
Huong T. Dang, Ibragim Gaidarov, Anh-Tuan Ton, Paul Miller, David J. Unett, Xiaohua Chen, John W. Adams, Najah Abi-Gerges, Lisa Karimi-Naser, H. Kiyomi Komori, Tim Indersmitten, Karin Bruinsma
Publikováno v:
The FASEB Journal. 34:1-1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::240ecb346301126d641e3ed838a08812
https://doi.org/10.1096/fasebj.2020.34.s1.04933
https://doi.org/10.1096/fasebj.2020.34.s1.04933
Autor:
Albert S. Ren, Kevin Whelan, Konrad Feichtinger, Xiuwen Zhu, Michael Morgan, David J. Unett, Graeme Semple, Andrew J. Grottick, Amy Siu-Ting Wong, Michelle Kasem, Huong T. Dang, Juerg Lehman, Minh Le, Thomas O. Schrader, John Frazer, Carleton R. Sage
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:126929
A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a0c6c9d2b6e9f953cfc42198cdb93d7b
https://doi.org/10.1016/j.bmcl.2019.126929
https://doi.org/10.1016/j.bmcl.2019.126929
Autor:
Khawja A. Usmani, Dawei Yue, Zhi-Liang Chu, Abu J.M. Sadeque, Chris Carroll, Chuan Chen, Hsin-Hui Shu, Sanju Narayanan, Hussein Al-Sharmma, Dominic P. Behan, Robert M. Jones, Graeme Semple, James N. Leonard, David J. Unett, Daniel J. Buzard, Michael Morgan, Juerg Lehmann, Imelda Calderon, Shiu-Feng Tung, Woo Hyun Yoon, Xiuwen Zhu, Sangdon Han, Andrew M. Kawasaki, Amy Siu-Ting Wong, Sun Hee Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3034-3038
The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a potent and efficacious GPR119 agonist across species, and possessed overall favorable pharmaceutical properties
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2f3b9e4db6f1603a99df66761f2f277
https://doi.org/10.1016/j.bmcl.2015.04.102
https://doi.org/10.1016/j.bmcl.2015.04.102
Autor:
Hussien A. Al-Shamma, Michael Morgan, Ibragim Gaidarov, Huong T. Dang, Joel Gatlin, Marc Decaire, David J. Unett, Karoline Choi, Jeff Edwards, Dawei Yue, Abu J.M. Sadeque, Kevin Whelan, Yifeng Xiong, Lixia Fu, Jayant Thatte, Graeme Semple, Sonja Strah-Pleynet, Sangdon Han, Michelle Solomon, Dominic P. Behan, Jae-Kyu Jung, Sanju Narayanan, Lars Thoresen, Robert M. Jones, Chuan Chen, Xiuwen Zhu, Khawja A. Usmani, Cameron Pride, Ruoping Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:322-326
The design and synthesis of novel 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamide CB2 selective ligands for the potential treatment of pain is described. Compound (R,R)-25 has good balance between CB2 agonist potency and selecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b59f936b671e7316d482a837b15c5aa1
https://doi.org/10.1016/j.bmcl.2014.11.040
https://doi.org/10.1016/j.bmcl.2014.11.040
Autor:
Ben Johnson, Tawfik Gharbaoui, Moody Jeanne, David J. Unett, Kevin Whelan, Ibragim Gaidarov, Michael Morgan, Lars Thoresen, Michelle Kasem, Abu J.M. Sadeque, Robert M. Jones, Chuan Chen, Sun Hee Kim, Hussien A. Al-Shamma, Minh Le, Joel Gatlin, Lorene Calvano, Andrew M. Kawasaki, Lixia Fu, Yinghong Gao, Scott Stirn, Weichao Chen, Jeremy Barden, Dominic P. Behan, Krishnan Ashwin M, Xiuwen Zhu, Graeme Semple, Dipanjan Sengupta, Christopher Ronald J, Jeff Edwards, Luis Lopez, Jayant Thatte, Daniel J. Buzard, Anthony C. Blackburn, Michelle Solomon, Todd Anthony, Thomas O. Schrader, Khawja A. Usmani
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1334-1339
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fc0ba742321c1acedff3bc45fe90e44
https://doi.org/10.1021/ml500422m
https://doi.org/10.1021/ml500422m