Institution
Novum
About: Novum is a based out in . It is known for research contribution in the topics: Estrogen receptor & Receptor. The organization has 659 authors who have published 578 publications receiving 27932 citations.
Topics: Estrogen receptor, Receptor, Thyroid hormone receptor, Ligand (biochemistry), Liver X receptor
Papers published on a yearly basis
Papers
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TL;DR: It is described that silencing of AKT1 in spindle-shaped biphasic MPM cells promotes the shift toward an epithelioid phenotype and evidence that ERβ expression is induced and exerts an anti-tumor effect through selective agonist activation is provided.
Abstract: // Arcangela G. Manente 1, * , Giulia Pinton 1, * , Sara Zonca 1 , Michele Cilli 2 , Maurizio Rinaldi 1 , Antonio Daga 2 , Stefan Nilsson 3, 4 , Laura Moro 1 1 Department of Pharmaceutical Sciences, University of Piemonte Orientale “A. Avogadro”, 28100, Novara, Italy 2 IRCCS San Martino-IST, 16132, Genova, Italy 3 Karo Bio AB, Novum, S-141 57, Huddinge, Sweden 4 Department of Biosciences and Nutrition, Karolinska Institutet, Novum, S-141 57, Huddinge, Sweden * These authors have contributed equally to this work Correspondence to: Laura Moro, e-mail: moro@pharm.unipmn.it Keywords: biphasic pleural mesothelioma, lactate, estrogen receptor beta, targeted therapy Received: March 16, 2015 Accepted: June 26, 2015 Published: July 09, 2015 ABSTRACT Biphasic malignant pleural mesothelioma (MPM) is the second most common histotype of MPM. It is histologically characterized by the concomitant presence of epithelioid and sarcomatoid features, the latter associated with worse prognosis. In this report we describe that silencing of AKT1 in spindle-shaped biphasic MPM cells promotes the shift toward an epithelioid phenotype. Furthermore, AKT1 silencing resulted in decreased expression of the lactate/H+ symporter MCT4 and its chaperone CD147/Basigin, and in the induction of estrogen receptor β (ERβ) expression. We provide evidence that ERβ expression is induced by increased intracellular lactate concentration. Spheroid culturing and tumor growth of ERβ negative biphasic MPM in nude mice resulted in the induction of ERβ expression and response to the selective agonist KB9520. In both models, the treatment with the ERβ agonist results in reduced cell proliferation, decreased expression of MCT4 and CD147/Basigin and increased acetylation and inactivation of AKT1. Collectively, in response to metabolic changes, ERβ expression is induced and exerts an anti-tumor effect through selective agonist activation. The possibility to reverse the more aggressive biphasic mesothelioma histotype by targeting ERβ with a selective agonist could represent a new effective treatment strategy.
14 citations
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TL;DR: A series of 4-(3-biaryl)quinolines with sulfone substituents on the terminal aryl ring (8) was prepared as potential LXR agonists and shown to reduce atherosclerotic lesion progression.
13 citations
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TL;DR: In this article, the oxindole gave 3,3,5,7-tetranitrooxindole (1c), which readily underwent ring-opening and decarboxylation to 4,6-dinitro-2-(dimtromclhyl)aniline (4b ), which in turn could be cyclized to 3,5-7-triniuoindazole (5).
13 citations
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TL;DR: It is shown that a short fragment from the LXRalpha gene promoter spanning the region from -144 to +43 relative to the mRNA initiation site can drive transcription of a reporter gene.
13 citations
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TL;DR: High affinity thyromimetics containing a novel phenyl-naphthylene core are reported, and have sub-nanomolar binding affinities for the TRbeta receptor and low to modest selectivity for TRbeta.
13 citations
Authors
Showing all 659 results
Name | H-index | Papers | Citations |
---|---|---|---|
Rajesh Kumar | 149 | 4439 | 140830 |
Jan-Åke Gustafsson | 147 | 1058 | 98804 |
Kari Hemminki | 100 | 1274 | 55290 |
Juha Kere | 97 | 642 | 38403 |
Hans Jörnvall | 94 | 642 | 33330 |
Jonatan R. Ruiz | 84 | 621 | 30112 |
Lennart Nilsson | 82 | 861 | 34898 |
Francisco B. Ortega | 79 | 503 | 26069 |
Lennart Hammarström | 75 | 407 | 23285 |
Jan Hillert | 74 | 420 | 25296 |
Bo Angelin | 71 | 301 | 17633 |
Lorenz Poellinger | 65 | 132 | 16244 |
Elvar Theodorsson | 61 | 425 | 13695 |
Gustav Dallner | 58 | 252 | 14147 |
Peter E. Lobie | 57 | 214 | 9278 |