Zobrazeno 1 - 10
of 62
pro vyhledávání: '"Gary Park"'
Autor:
Yan Chen, Hui Li, Rose Yen, Thilo J. Heckrodt, Darren McMurtrie, Rajinder Singh, Vanessa Taylor, Esteban S. Masuda, Gary Park, Donald G. Payan
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1805-1811
Janus kinases (JAK) play a critical role in JAK/signal transducer and activator of transcription (STAT) signaling pathways that mediate immune response and cell growth. From high-throughput screening (HTS) hit to lead optimization, a series of pyrimi
Autor:
Simon J. Shaw, Dane A. Goff, David C. Carroll, Rajinder Singh, David J. Sweeny, Gary Park, Yonchu Jenkins, Vadim Markovtsov, Tian-Qiang Sun, Sarkiz D. Issakani, Yasumichi Hitoshi, Donald G. Payan
Publikováno v:
Bioorganicmedicinal chemistry. 71
Using an in-cell AMPK activation assay, we have developed structure-activity relationships around a hit pyridine dicarboxamide 5 that resulted in 40 (R419). A particular focus was to retain the on-target potency while also improving microsomal stabil
Autor:
Chenge An, Gary Parker, Jeremy G. Venditti, Michael P. Lamb, Marwan A. Hassan, Hiroshi Miwa, Xudong Fu
Publikováno v:
Geophysical Research Letters, Vol 51, Iss 17, Pp n/a-n/a (2024)
Abstract Riverbeds often fine downstream, with a gravel‐bedded reach, a relatively abrupt gravel‐sand transition (GST), and a sand‐bedded reach. Underlying this behavior, bed grain size distributions are often bimodal, with a relative paucity (
Externí odkaz:
https://doaj.org/article/0f2fc175a40b41dfb739cdcd98d1301f
Autor:
Yan Chen, Kin Tso, Thilo J. Heckrodt, Hui Li, Rose Yen, Nan Lin, Rajinder Singh, Vanessa Taylor, Esteban S. Masuda, Gary Park, Donald G. Payan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 73:128900
Interleukin-1 receptor-associated kinase 4 (IRAK4) plays a critical role in transduction of IL-1R/TLR signaling which is responsible for innate immune response. From HTS campaign, bicyclic-pyrimidine compounds have been identified as potent IRAK4 inh
Autor:
Yan Chen, Joshua M. Spin, Thomas Renné, James B Fink, Tobias Deuse, Evgenios Neofytou, Sonja Schrepfer, Gary Park, Vanessa Taylor, Robert C. Robbins, Hermann Reichenspurner, Rainer Kiefmann, Mandy Stubbendorff, Xiaoqin Hua, Martina Kiefmann
Publikováno v:
Transplantation. 100:1022-1031
Background The efficacy of selective Janus kinase 1/3 inhibitor R507 to prevent obliterative airway disease was analyzed in preclinical airway transplantation models. Methods Orthotopic trachea transplantations were performed between Lewis donors and
Publikováno v:
Organicbiomolecular chemistry. 14(39)
Matched molecular pair analysis was used to evaluate the ability of a tetrazolone group to act as a bioisostere of a carboxylic acid. Compound 7, a tetrazolone of the anti-hypertensive drug, telmisartan 6, was shown to be a potent AT1 antagonist (Kb
Autor:
Gergely T. Török, Gary Parker
Publikováno v:
Scientific Reports, Vol 12, Iss 1, Pp 1-15 (2022)
Abstract Exploring the effects of bank vegetation on fluvial morphodynamics has long been an essential part of fluvial morphodynamic-related research. In a practical sense, a central question is: does increased vegetation density increase or decrease
Externí odkaz:
https://doaj.org/article/6dc3845d6efd4afdb4c399148e89e7c0
Autor:
Joachim Velden, Muhammad Baluom, Robert C. Robbins, Yan Chen, Mandy Stubbendorff, Vanessa Taylor, Thomas Streichert, Xiaoqin Hua, Hermann Reichenspurner, Tobias Deuse, Sonja Schrepfer, Gary Park
Publikováno v:
Transplantation. 94:695-702
Selective inhibition of lymphocyte activation through abrogation of signal 3-cytokine transduction emerges as a new strategy for immunosuppression. This is the first report on the novel Janus kinase (JAK)1/3 inhibitors R507 and R545 for prevention of
Autor:
Hongbo Ma, Jeffrey A. Nittrouer, Xudong Fu, Gary Parker, Yuanfeng Zhang, Yuanjian Wang, Yanjun Wang, Michael P. Lamb, Julia Cisneros, Jim Best, Daniel R. Parsons, Baosheng Wu
Publikováno v:
Nature Communications, Vol 13, Iss 1, Pp 1-11 (2022)
Dams constructed on fine-grained rivers cause an increase in flow resistance downstream, thereby amplifying, rather than reducing, flood stage.
Externí odkaz:
https://doaj.org/article/a6d26c032ae94905b57c82c5a34fcdff