Synthetic Sphingolipids with 1,2-Pyridazine Appendages Improve Antiproliferative Activity in Human Cancer Cell Lines

Autor: Brendan T. Finicle, Cuauhtemoc Ramirez, Stephen Hanessian, Vito Vece, Sylvestre P J T Bachollet, Nadine Ben Romdhane, Elizabeth Selwan, Amogha Dahal, Alison N. McCracken, Aimee L. Edinger

Publikováno v: ACS Med Chem Lett

[Image: see text] A synthetic sphingolipid related to a ring-constrained hydroxymethyl pyrrolidine analog of FTY720 that was known to starve cancer cells to death was chemically modified to include a series of alkoxy-tethered 3,6-substituted 1,2-pyri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b883ae1745f3fd992109a7830cb9ab9
https://doi.org/10.1021/acsmedchemlett.9b00553

Branched chain amino acid metabolism and cancer: the importance of keeping things in context

Autor: Aimee L. Edinger, Elizabeth Selwan

Publikováno v: Translational Cancer Research. 6:S578-S584

Because non-homeostatic proliferation increases anabolic demand, tumor cells reprogram metabolism in ways that support growth. Although tumor cells retain some metabolic flexibility, the constitutive activation of oncogenes and mutation or loss of tu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c32a2975334b27c7c7711c3dbf64b1d
https://doi.org/10.21037/tcr.2017.05.05

Targeting cancer metabolism by simultaneously disrupting parallel nutrient access pathways

Autor: Bruce J. Tromberg, Seong M. Kim, Robert Edwards, Stephen Hanessian, Ryan J. McMonigle, Garret Guenther, Aimee L. Edinger, Tricia T. Nguyen, Eric O. Potma, Brendan T. Finicle, Yanling Zhang, Bin Chen, Tiffany M. Nguyen, Jue Hou, Atsuo T. Sasaki, Archna Ravi, Satoshi Kofuji, Mari Kono, Lois S. Weisman, Alison N. McCracken, Saurabh G. Roy, Manuel U. Ramirez, Timothy Wiher, Elizabeth Selwan

Publikováno v: Kim, Seong M; Roy, Saurabh G; Chen, Bin; Nguyen, Tiffany M; McMonigle, Ryan J; McCracken, Alison N; et al.(2016). Targeting cancer metabolism by simultaneously disrupting parallel nutrient access pathways. Journal of Clinical Investigation, 126(11), 4088-4102. doi: 10.1172/jci87148. UC Irvine: Institute for Clinical and Translational Science. Retrieved from: http://www.escholarship.org/uc/item/6zh0q267

Oncogenic mutations drive anabolic metabolism, creating a dependency on nutrient influx through transporters, receptors, and macropinocytosis. While sphingolipids suppress tumor growth by downregulating nutrient transporters, macropinocytosis and aut

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3dd0ed68029bf8a65f6d0ff97e053648
https://doi.org/10.1172/jci87148

Phosphorylation of a constrained azacyclic FTY720 analog enhances anti-leukemic activity without inducing S1P receptor activation

Autor: Elizabeth Selwan, Andrea Huwiler, Daniel Fallegger, Andrew Keebaugh, Bin Chen, Gang Liu, Ryan J. McMonigle, C Brandt, Rebecca Fransson, Lorenzo Sernissi, Seong M. Kim, Aimee L. Edinger, Jérémie Tessier, Michael T. Kleinman, S Clare, Alison N. McCracken, Stephen Hanessian, Markus Müschen, Nicolas Moitessier, Michael S. Perryman, Saurabh G. Roy, S A Barr, A J Snider

Publikováno v: Leukemia, vol 31, iss 3
McCracken, AN; McMonigle, RJ; Tessier, J; Fransson, R; Perryman, MS; Chen, B; et al.(2017). Phosphorylation of a constrained azacyclic FTY720 analog enhances anti-leukemic activity without inducing S1P receptor activation. LEUKEMIA, 31(3), 669-677. doi: 10.1038/leu.2016.244. UC Irvine: Retrieved from: http://www.escholarship.org/uc/item/1sd6s65b
Leukemia

The frequency of poor outcomes in relapsed leukemia patients underscores the need for novel therapeutic approaches. The Food and Drug Administration-approved immunosuppressant FTY720 limits leukemia progression by activating protein phosphatase 2A an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5f3bd1bd3b61ad4b5f162b81fa5d518
https://escholarship.org/uc/item/1sd6s65b

Azacyclic FTY720 Analogues That Limit Nutrient Transporter Expression but Lack S1P Receptor Activity and Negative Chronotropic Effects Offer a Novel and Effective Strategy to Kill Cancer Cells in Vivo

Autor: Andrew Keebaugh, Elizabeth Selwan, Stephen Hanessian, Daniel Fallegger, Saurabh G. Roy, Ryan J. McMonigle, Rebecca Fransson, Alison N. McCracken, Aimee L. Edinger, Michael T. Kleinman, Andrea Huwiler, Bin Chen

Publikováno v: ACS chemical biology. 11(2)

FTY720 sequesters lymphocytes in secondary lymphoid organs through effects on sphingosine-1-phosphate (S1P) receptors. However, at higher doses than are required for immunosuppression, FTY720 also functions as an anti-cancer agent in multiple animal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b4a69d52afde1a1455d136c9d9621df
https://pubmed.ncbi.nlm.nih.gov/26653336