Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Felix Gonzalez-Lopez de Turiso"'
Publikováno v:
Expert Opinion on Therapeutic Patents. 32:365-379
Tyrosine kinase 2 (TYK2) is a member of the JAK family class of kinases that is responsible for mediating the immune response to IL-12, IL-23, and IFNα. The therapeutic value of targeting this pathway in autoimmune diseases is supported by human gen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f9bba064ea05054097663e27663bb59
https://doi.org/10.1080/13543776.2022.2026927
https://doi.org/10.1080/13543776.2022.2026927
Autor:
Terry Fang, Rab Gilfillan, Janaky Coomaraswamy, Dirk M. Walther, Martin K Himmelbauer, Zhili Xin, Kerri Spilker, Douglas Marcotte, Joseph C Santoro, Thomas Hesson, Istvan J. Enyedy, Ru Wei, Felix Gonzalez-Lopez de Turiso, J Howard Jones, Michael Dechantsreiter, Zheng Fengmei, Kristopher W King, Ying Liu, Paramasivam Murugan, P Rajesh Kumar, Joseph Hedde
Publikováno v:
Journal of medicinal chemistry. 64(20)
Apoptosis signal-regulating kinase 1 (ASK1) is one of the key mediators of the cellular stress response that regulates inflammation and apoptosis. To probe the therapeutic value of modulating this pathway in preclinical models of neurological disease
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69bdc613fadb1b6767798fc40d289b98
https://pubmed.ncbi.nlm.nih.gov/34653340
https://pubmed.ncbi.nlm.nih.gov/34653340
Autor:
Kristopher W King, Brenda Amaral, Eli Schuman, LaiYee Wong, Michael Rooney, Marta Nevalainen, Jun Feng, Paramasivam Murugan, Jayanth V. Chodaparambil, Thomas A. Patterson, Hannah Certo, Martin K Himmelbauer, Rab Gilfillan, Tamara Halkina, Sarah Lamore, J Howard Jones, Douglas Marcotte, Gregory M Dillon, Jaclyn L. Henderson, Thomas Hesson, P Rajesh Kumar, Edward Yin-Shiang Lin, Channa Bao, Felix Gonzalez-Lopez de Turiso, Joshua L Johnson, Michael Calhoun
Publikováno v:
Journal of medicinal chemistry. 64(9)
Structural analysis of the known NIK inhibitor 3 bound to the kinase domain of TTBK1 led to the design and synthesis of a novel class of azaindazole TTBK1 inhibitors exemplified by 8 (cell IC50: 571 nM). Systematic optimization of this series of anal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24de7147f81434a735de9781d30290ec
https://pubmed.ncbi.nlm.nih.gov/33944571
https://pubmed.ncbi.nlm.nih.gov/33944571
Autor:
Zhili Xin, Douglas Marcotte, Joseph C Santoro, Rab Gilfillan, J Howard Jones, Thomas Hesson, Istvan J. Enyedy, Martin K Himmelbauer, Paramasivam Murugan, Felix Gonzalez-Lopez de Turiso, Kristopher W King
Publikováno v:
ACS Med Chem Lett
[Image: see text] Apoptosis signal-regulating kinase 1 (ASK1) is a key mediator in the apoptotic and inflammatory cellular stress response. To investigate the therapeutic value of modulating this pathway in neurological disease, we have completed med
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cca9a306448f636bdc3b87bc3cb5c746
https://europepmc.org/articles/PMC7153032/
https://europepmc.org/articles/PMC7153032/
Autor:
Thomas Hesson, Istvan J. Enyedy, Kristopher W King, Martin K Himmelbauer, Joseph C. Santoro, Paramasivam Murugan, J. Howard Jones, Joshua L Johnson, Felix Gonzalez-Lopez de Turiso, Kerri Spilker, Douglas Marcotte, Rab Gilfillan, Zhili Xin, Michael Joseph Luzzio
Publikováno v:
Journal of medicinal chemistry. 62(23)
Structural analysis of a known apoptosis signal-regulating kinase 1 (ASK1) inhibitor bound to its kinase domain led to the design and synthesis of the novel macrocyclic inhibitor 8 (cell IC50 = 1.2 μM). The profile of this compound was optimized for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::150776d7925313644d75434a3c742926
https://pubmed.ncbi.nlm.nih.gov/31710475
https://pubmed.ncbi.nlm.nih.gov/31710475
Autor:
Andrew Tasker, Andreas Reichelt, Yi-Ling Hu, Deanna Mohn, John McCarter, Ben Fisher, Robert M. Rzasa, Yi Chen, Julio C. Medina, Gang Yu, Sharon Wannberg, Brian Lucas, Ron C. Kelly, Jennifer Seganish, Felix Gonzalez-Lopez de Turiso, Xiaolin Hao, Kristin L. Andrews, Douglas A. Whittington, Matthew Frank Brown, Dawei Zhang, Youngsook Shin, Mario G. Cardozo, Jason Duquette, Robert C. Wahl, Leeanne Zalameda, Daniela Metz, Vatee Pattaropong, Michael G. Johnson, Tisha San Miguel, Randall W. Hungate, John Whoriskey, Lawrence R. McGee, Timothy D. Cushing, Kirk Henne, Liping H. Pettus, Xiao He
Publikováno v:
Journal of Medicinal Chemistry. 58:480-511
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41f464b8458b3d559ce036ed30580e01
https://doi.org/10.1021/jm501624r
https://doi.org/10.1021/jm501624r
Autor:
Felix, Gonzalez-Lopez de Turiso, Xiaolin, Hao, Youngsook, Shin, Minna, Bui, Iain D G, Campuzano, Mario, Cardozo, Michelle C, Dunn, Jason, Duquette, Benjamin, Fisher, Robert S, Foti, Kirk, Henne, Xiao, He, Yi-Ling, Hu, Ron C, Kelly, Michael G, Johnson, Brian S, Lucas, John, McCarter, Lawrence R, McGee, Julio C, Medina, Daniela, Metz, Tisha, San Miguel, Deanna, Mohn, Thuy, Tran, Christine, Vissinga, Sharon, Wannberg, Douglas A, Whittington, John, Whoriskey, Gang, Yu, Leeanne, Zalameda, Xuxia, Zhang, Timothy D, Cushing
Publikováno v:
Journal of medicinal chemistry. 59(15)
Optimization of the potency and pharmacokinetic profile of 2,3,4-trisubstituted quinoline, 4, led to the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 6a (AM-0687) and 7 (AM-1430). On the basis of their improved profi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::a242cbf7d7efba8c63b94dcec247686e
https://pubmed.ncbi.nlm.nih.gov/27411843
https://pubmed.ncbi.nlm.nih.gov/27411843
Autor:
Julia Winslow Lohman, David Fong, Michael G. Johnson, Xiaolin Hao, Gang Yu, Douglas A. Whittington, Helen J. McBride, Yi-Ling Hu, Vatee Pattaropong, Lawrence R. McGee, Sharon Wannberg, Kirk Henne, Jillian L. Simard, Xiao He, Deanna Mohn, Julio C. Medina, Kent Miner, Todd J. Kohn, Yi Chen, Felix Gonzalez-Lopez de Turiso, Jennifer Seganish, Mario G. Cardozo, Matthew Frank Brown, Daniela Metz, Youngsook Shin, Timothy D. Cushing
Publikováno v:
Journal of Medicinal Chemistry. 55:7667-7685
Structure-based rational design led to the synthesis of a novel series of potent PI3K inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ dual inhibitor that displayed suitable physicochemical properties and pha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10d2206b5014d0cdfd1a496b0d1339bc
https://doi.org/10.1021/jm300679u
https://doi.org/10.1021/jm300679u
Autor:
Zice Fu, Yongli Su, Xuemei Wang, Hua Lucy Tang, Timothy J. Sullivan, Lisa Seitz, Felix Gonzalez-Lopez de Turiso, Julio C. Medina, Mark P. Grillo, Shanna Lawlis, Ying Sun, Wang Shen, M.J. Schmitt, Qiuping Ye, Sarah E. Lively, Matthew L. Brown, An-Rong Li, Yingcai Wang, Bettina Van Lengerich, Jill Wait, Sujen Lai, Jiwen Liu, Michael G. Johnson, Jay Danao, Tassie L. Collins, Qingge Xu
Publikováno v:
ACS Medicinal Chemistry Letters. 2:326-330
Prostaglandin D2 (PGD2) plays a key role in mediating allergic reactions seen in asthma, allergic rhinitis, and atopic dermatitis. PGD2 exerts its activity through two G protein-coupled receptors (GPCRs), prostanoid D receptor (DP or DP1), and chemoa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1412c5f0cb7a55fd9ce712791e8a8c0f
https://doi.org/10.1021/ml1002234
https://doi.org/10.1021/ml1002234
Autor:
Hua Tu, Lisa Julian, Nigel Walker, Maren Gulsrud Willcockson, Yosup Rew, Michael DeGraffenreid, Zhulun Wang, Juan C. Jaen, Daqing Sun, Ron C. Kelly, Athena Sudom, Seb Caille, Jacob Kaizerman, Jay P. Powers, Xuelei Yan, Qiuping Ye, Stefania Ursu, Ben Jiang, Felix Gonzalez-Lopez de Turiso, Randall W. Hungate, Dustin McMinn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:405-410
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-huma
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d541a6a690483f033c76a34f9400098
https://doi.org/10.1016/j.bmcl.2010.10.129
https://doi.org/10.1016/j.bmcl.2010.10.129