Improved homology modeling of the human & rat EP4 prostanoid receptors

Autor: Melissa C. Holt, Chi S. Ho, M. Inés Morano, Stephen D. Barrett, Adam J. Stein

Publikováno v: BMC Molecular and Cell Biology, Vol 20, Iss 1, Pp 1-14 (2019)

Abstract Background The EP4 prostanoid receptor is one of four GPCRs that mediate the diverse actions of prostaglandin E2 (PGE2). Novel selective EP4 receptor agonists would assist to further elucidate receptor sub-type function and promote developme

Externí odkaz: https://doaj.org/article/c90815da60ca4e659303d9709faffaad

Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors

Autor: Melissa C. Holt, Zahra Assar, Reza Beheshti Zavareh, Lin Lin, Justin Anglin, Oksana Mashadova, Daniel Haldar, Edouard Mullarky, Daniel M. Kremer, Lewis C. Cantley, Alec C. Kimmelman, Adam J. Stein, Luke L. Lairson, Costas A. Lyssiotis

Publikováno v: Biochemistry. 57:6604-6614

Pancreatic cancer cells are characterized by deregulated metabolic programs that facilitate growth and resistance to oxidative stress. Among these programs, pancreatic cancers preferentially utilize a metabolic pathway through the enzyme aspartate am

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28f0132c70b3f3925ded93a2125cdd5f
https://doi.org/10.1021/acs.biochem.8b00914

Exploiting an Asp-Glu 'switch' in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia

Autor: Morgan Back, Matthew B. Robers, Edward M. Scolnick, Adam J. Stein, Jennifer Gale, Lina Benajiba, Damodharan Lakshminarasimhan, Arthur Campbell, Thomas Machleidt, Richard Stone, Florence F. Wagner, Xi Shi, Michael T. Hemann, Jennifer Wilkinson, Amy Saur Conway, Andrew L. Kung, Edward Holson, Joshua R. Sacher, Alexandre Puissant, Yan-Ling Zhang, Daniel J. DeAngelo, Yana Pikman, Ilene Galinsky, Linda Ross, Jen Q. Pan, Olivier Hermine, Kimberly Stegmaier, Gabriela Alexe, Taner Kaya, Michel Weiwer

Publikováno v: Science Translational Medicine
Science Translational Medicine, American Association for the Advancement of Science, 2018, 10 (431), 〈10.1126/scitranslmed.aam8460〉

International audience; Glycogen synthase kinase 3 (GSK3), a key regulatory kinase in the wingless-type MMTV integration site family (WNT) pathway, is a therapeutic target of interest in many diseases. Although dual GSK3α/β inhibitors have entered

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01f26d3a8beef63982f0fc1f137af7cc
https://hal.archives-ouvertes.fr/hal-01815758

Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis

Autor: Lance Goulet, Fei Huang, Patricia Prodanovich, Dave Lonergan, Gretchen Bain, Janice Darlington, Andiliy G. Lai, Angelina M. Santini, Kristen E. Shannon, Gina L. Ma, Christopher D. King, Jilly F. Evans, Imelda Calderon, Adam J. Stein, John H. Hutchinson

Publikováno v: The Journal of pharmacology and experimental therapeutics. 360(1)

Autotaxin (ATX) is a secreted glycoprotein that converts lysophosphatidylcholine (LPC) to the bioactive phospholipid lysophosphatidic acid (LPA) and is the major enzyme generating circulating LPA. Inhibition of LPA signaling has profound antifibrotic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b07cf278a0329f302e73eee640438c30
https://pubmed.ncbi.nlm.nih.gov/27754931

Structural and biochemical basis for misfolded RNA recognition by the Ro autoantigen

Autor: Sandra L. Wolin, Karin M. Reinisch, Chunmei Fu, Adam J. Stein, Gabriele Fuchs

Publikováno v: Nature Structural & Molecular Biology. 13:1002-1009

The Ro autoantigen is ring-shaped, binds misfolded noncoding RNAs and is proposed to function in quality control. Here we determine how Ro interacts with misfolded RNAs. Binding of Ro to misfolded precursor (pre)-5S ribosomal RNA requires a single-st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::719b7bc46640c181a75bf283367cbce5
https://doi.org/10.1038/nsmb1156