Zobrazeno 1 - 9 of 9 pro vyhledávání: '"Matthew D. Falk"'
1
Cancer-Associated Mutations Enhance The Sensitivity Of The Trupath GαQ/11 System
Autor: Dewi Safitri, Matthew Harris, Abigail Pearce, Xianglin Huang, Matthew Rosa, Kerry Barkan, Edward Wills, Maria Marti-Solano, Matthew D. Falk, Graham Ladds
G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors and are a common drug target. They can be stabilised in different conformational states by ligands to activate multiple transducers and effectors leading to a variet
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9b190e886edf3c9b677c806c5dd5adaa
https://doi.org/10.1101/2022.09.01.506210
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2
Prokinetic actions of luminally acting 5‐HT 4 receptor agonists
Autor: Melody M. Haag, Emily J. Joyce, Jun Matsukawa, Brigitte Lavoie, Grant W. Hennig, Luana Griffin, Colleen B. Kerrigan, Steve Swann, Alisha A. Linton, Jill Wykosky, Molly C. Hurd, Matthew D. Falk, Gary M. Mawe, Stephan C. Bischoff, John R. Konen, Daria Guseva, Tony Gibson
Publikováno v: Neurogastroenterology & Motility. 33
BACKGROUND 5-HT4 receptor (5-HT4 R) agonists exert prokinetic actions in the GI tract, but non-selective actions and potential for stimulation of non-target 5-HT4 Rs have limited their use. Since 5-HT4 Rs are expressed in the colonic epithelium and t
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::abd7fded891fa1991524991f0e96741e
https://doi.org/10.1111/nmo.14026
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3
Prokinetic actions of luminally acting 5-HT
Autor: John R, Konen, Melody M, Haag, Daria, Guseva, Molly, Hurd, Alisha A, Linton, Brigitte, Lavoie, Colleen B, Kerrigan, Emily, Joyce, Stephan C, Bischoff, Steve, Swann, Luana, Griffin, Jun, Matsukawa, Matthew D, Falk, Tony S, Gibson, Grant W, Hennig, Jill, Wykosky, Gary M, Mawe
Publikováno v: Neurogastroenterol Motil
BACKGROUND: 5-HT(4) receptor (5-HT(4)R) agonists exert prokinetic actions in the GI tract, but non-selective actions and potential for stimulation of non-target 5-HT(4)Rs have limited their use. Since 5-HT(4)Rs are expressed in the colonic epithelium
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::5c474f4a18f2298351a0efea9b5e47db
https://pubmed.ncbi.nlm.nih.gov/33185015
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4
PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations
Autor: Melissa West, Victoria A. Appleman, Valeria Fantin, Michele McTigue, Sergei Timofeevski, Matthew D. Falk, Alexei Brooun, Scott Rp McDonnell, Tod Smeal, Al Charest, Wenyue Hu, Wei Liu, Ya-Li Deng, Katy A. Wong, Timothy C. Nichols, Justine L. Lam, Ping Jiang, Helen Y. Zou, Qiuhua Li, Lars D. Engstrom, Timothy Affolter, Ted William Johnson, Patrick B. Lappin
Publikováno v: Proceedings of the National Academy of Sciences. 112:3493-3498
Oncogenic c-ros oncogene1 (ROS1) fusion kinases have been identified in a variety of human cancers and are attractive targets for cancer therapy. The MET/ALK/ROS1 inhibitor crizotinib (Xalkori, PF-02341066) has demonstrated promising clinical activit
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5769ead600f455be1dcabb5bf6780f26
https://doi.org/10.1073/pnas.1420785112
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5
Engineering of an isolated p110α subunit of PI3Kα permits crystallization and provides a platform for structure-based drug design
Autor: Matthew D. Falk, Simon Bergqvist, Ya-Li Deng, Ping Chen, Sergei Timofeevski, Alexei Brooun, Wei Liu
Publikováno v: Protein Science. 23:1332-1340
PI3Kα remains an attractive target for the development of anticancer targeted therapy. A number of p110α crystal structures in complex with the nSH2-iSH2 fragment of p85 regulatory subunit have been reported, including a few small molecule co-cryst
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a8d5819bf6de0c62fc37217b99c556d5
https://doi.org/10.1002/pro.2517
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6
Discovery of a Novel Series of Inhibitors of Lymphoid Tyrosine Phosphatase with Activity in Human T Cells
Autor: Sheng Li, Zhong Yin Zhang, Andrew C. Chan, Matthew D. Falk, Nunzio Bottini, Rossella Messina, Stephanie M. Stanford, Divya Krishnamurthy, Xiao Yu, Yantao He, Russell Dahl, Roza Kazemi, Virgil L. Woods, Bikash Debnath, Nouri Neamati, Amy M. Barrios, Tong Liu
Publikováno v: Journal of Medicinal Chemistry. 54:1640-1654
The lymphoid tyrosine phosphatase LYP, encoded by the PTPN22 gene, is a critical regulator of signaling in T cells and recently emerged as a candidate target for therapy of autoimmune diseases. Here, by library screening, we identified a series of no
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad928fc7c63aa08b1e512b8a8e73110a
https://doi.org/10.1021/jm101202j
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7
Enzyme kinetics and distinct modulation of the protein kinase N family of kinases by lipid activators and small molecule inhibitors
Autor: Stephan Grant, Ben Bolaños, Alexei Brooun, Sergei Timofeevski, Anke Klippel, Keziban Unsal-Kacmaz, Matthew D. Falk, Wei Liu
Publikováno v: Bioscience Reports
Bioscience Reports, Vol 34, Iss 2, p e00097 (2014)
The PKN (protein kinase N) family of Ser/Thr protein kinases regulates a diverse set of cellular functions, such as cell migration and cytoskeletal organization. Inhibition of tumour PKN activity has been explored as an oncology therapeutic approach,
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9296fbb67d23c619416a2b8cfbef2774
https://doi.org/10.1042/bsr20140010
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