Zobrazeno 1 - 10
of 63
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
Publikováno v:
Vadose Zone Journal, Vol 23, Iss 5, Pp n/a-n/a (2024)
Abstract Linkages between the micro‐scale of soil water and landscape scale of hydrological data could be improved with the analysis of soil factors in preferential flow rates. This rearrangement of the terminology on soil pore size from published
Externí odkaz:
https://doaj.org/article/74d9e8c6e7734402a68a030afaf5dc1a
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
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
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:
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