Literature DB >> 28445593

NR5A2 discovering compounds that block tumor growth in PDAC.

Robert Fletterick1.   

Abstract

Pancreatic cancers depend on driver molecules, oncogene proteins such as RAS. NR5A2 protein is a transcription factor and either activates or inhibits transcription through actions at hundreds of enhancers. It has unusual properties with effects appearing in multiple signaling networks. NR5A2 is a pluripotency reprogramming factor in the class nuclear receptor. Its controlling hormone is PIP3. Experiments suggest NR5A2 activation drives PDAC and inhibitors blunt cancer cell proliferation.
© 2017 Wiley Periodicals, Inc.

Entities:  

Keywords:  LRH-1; stem cell; structure-based inhibitor design; β-catenin

Mesh:

Substances:

Year:  2017        PMID: 28445593      PMCID: PMC5519325          DOI: 10.1002/jso.24639

Source DB:  PubMed          Journal:  J Surg Oncol        ISSN: 0022-4790            Impact factor:   3.454


  12 in total

1.  Synergy between LRH-1 and beta-catenin induces G1 cyclin-mediated cell proliferation.

Authors:  Oronza A Botrugno; Elisabeth Fayard; Jean-Sébastien Annicotte; Céline Haby; Thomas Brennan; Olivia Wendling; Toshiya Tanaka; Tatsuhiko Kodama; Winston Thomas; Johan Auwerx; Kristina Schoonjans
Journal:  Mol Cell       Date:  2004-08-27       Impact factor: 17.970

2.  Nuclear receptor liver receptor homologue 1 (LRH-1) regulates pancreatic cancer cell growth and proliferation.

Authors:  Cindy Benod; Maia V Vinogradova; Natalia Jouravel; Grace E Kim; Robert J Fletterick; Elena P Sablin
Journal:  Proc Natl Acad Sci U S A       Date:  2011-09-26       Impact factor: 11.205

3.  Structural basis of coactivation of liver receptor homolog-1 by β-catenin.

Authors:  Fumiaki Yumoto; Phuong Nguyen; Elena P Sablin; John D Baxter; Paul Webb; Robert J Fletterick
Journal:  Proc Natl Acad Sci U S A       Date:  2011-12-20       Impact factor: 11.205

4.  Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1.

Authors:  Richard J Whitby; Sally Dixon; Patrick R Maloney; Philippe Delerive; Bryan J Goodwin; Derek J Parks; Timothy M Willson
Journal:  J Med Chem       Date:  2006-11-16       Impact factor: 7.446

Review 5.  Molecular basis for the regulation of the nuclear receptor LRH-1.

Authors:  Sokrates Stein; Kristina Schoonjans
Journal:  Curr Opin Cell Biol       Date:  2014-11-15       Impact factor: 8.382

6.  Structure of Liver Receptor Homolog-1 (NR5A2) with PIP3 hormone bound in the ligand binding pocket.

Authors:  Elena P Sablin; Raymond D Blind; Rubatharshini Uthayaruban; Hsiu-Ju Chiu; Ashley M Deacon; Debanu Das; Holly A Ingraham; Robert J Fletterick
Journal:  J Struct Biol       Date:  2015-09-28       Impact factor: 2.867

7.  Nr5a2 maintains acinar cell differentiation and constrains oncogenic Kras-mediated pancreatic neoplastic initiation.

Authors:  Guido von Figura; John P Morris; Christopher V E Wright; Matthias Hebrok
Journal:  Gut       Date:  2013-05-03       Impact factor: 23.059

8.  A genome-wide association study identifies pancreatic cancer susceptibility loci on chromosomes 13q22.1, 1q32.1 and 5p15.33.

Authors:  Gloria M Petersen; Laufey Amundadottir; Charles S Fuchs; Peter Kraft; Rachael Z Stolzenberg-Solomon; Kevin B Jacobs; Alan A Arslan; H Bas Bueno-de-Mesquita; Steven Gallinger; Myron Gross; Kathy Helzlsouer; Elizabeth A Holly; Eric J Jacobs; Alison P Klein; Andrea LaCroix; Donghui Li; Margaret T Mandelson; Sara H Olson; Harvey A Risch; Wei Zheng; Demetrius Albanes; William R Bamlet; Christine D Berg; Marie-Christine Boutron-Ruault; Julie E Buring; Paige M Bracci; Federico Canzian; Sandra Clipp; Michelle Cotterchio; Mariza de Andrade; Eric J Duell; J Michael Gaziano; Edward L Giovannucci; Michael Goggins; Göran Hallmans; Susan E Hankinson; Manal Hassan; Barbara Howard; David J Hunter; Amy Hutchinson; Mazda Jenab; Rudolf Kaaks; Charles Kooperberg; Vittorio Krogh; Robert C Kurtz; Shannon M Lynch; Robert R McWilliams; Julie B Mendelsohn; Dominique S Michaud; Hemang Parikh; Alpa V Patel; Petra H M Peeters; Aleksandar Rajkovic; Elio Riboli; Laudina Rodriguez; Daniela Seminara; Xiao-Ou Shu; Gilles Thomas; Anne Tjønneland; Geoffrey S Tobias; Dimitrios Trichopoulos; Stephen K Van Den Eeden; Jarmo Virtamo; Jean Wactawski-Wende; Zhaoming Wang; Brian M Wolpin; Herbert Yu; Kai Yu; Anne Zeleniuch-Jacquotte; Joseph F Fraumeni; Robert N Hoover; Patricia Hartge; Stephen J Chanock
Journal:  Nat Genet       Date:  2010-01-24       Impact factor: 38.330

9.  Canonical Wnt/β-catenin regulation of liver receptor homolog-1 mediates pluripotency gene expression.

Authors:  Ryan T Wagner; Xueping Xu; Fei Yi; Bradley J Merrill; Austin J Cooney
Journal:  Stem Cells       Date:  2010-10       Impact factor: 6.277

10.  Disulfide-Trapping Identifies a New, Effective Chemical Probe for Activating the Nuclear Receptor Human LRH-1 (NR5A2).

Authors:  Felipe de Jesus Cortez; Miyuki Suzawa; Sam Irvy; John M Bruning; Elena Sablin; Matthew P Jacobson; Robert J Fletterick; Holly A Ingraham; Pamela M England
Journal:  PLoS One       Date:  2016-07-28       Impact factor: 3.240

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  5 in total

Review 1.  Nuclear receptor subfamily 5 group A member 2 (NR5A2): role in health and diseases.

Authors:  Nikita Sandhu; Satyavati Rana; Kiran Meena
Journal:  Mol Biol Rep       Date:  2021-10-13       Impact factor: 2.316

2.  NR5A2 transcriptional activation by BRD4 promotes pancreatic cancer progression by upregulating GDF15.

Authors:  Feng Guo; Yingke Zhou; Hui Guo; Dianyun Ren; Xin Jin; Heshui Wu
Journal:  Cell Death Discov       Date:  2021-04-13

3.  Integrative analysis of KRAS wildtype metastatic pancreatic ductal adenocarcinoma reveals mutation and expression-based similarities to cholangiocarcinoma.

Authors:  James T Topham; Erica S Tsang; Joanna M Karasinska; David F Schaeffer; Daniel J Renouf; Andrew Metcalfe; Hassan Ali; Steve E Kalloger; Veronika Csizmok; Laura M Williamson; Emma Titmuss; Karina Nielsen; Gian Luca Negri; Sandra E Spencer Miko; Gun Ho Jang; Robert E Denroche; Hui-Li Wong; Grainne M O'Kane; Richard A Moore; Andrew J Mungall; Jonathan M Loree; Faiyaz Notta; Julie M Wilson; Oliver F Bathe; Patricia A Tang; Rachel Goodwin; Gregg B Morin; Jennifer J Knox; Steven Gallinger; Janessa Laskin; Marco A Marra; Steven J M Jones
Journal:  Nat Commun       Date:  2022-10-08       Impact factor: 17.694

4.  Pharmacological LRH-1/Nr5a2 inhibition limits pro-inflammatory cytokine production in macrophages and associated experimental hepatitis.

Authors:  Thomas Brunner; M Eugenia Delgado; Juliane Schwaderer; Truong San Phan; Astrid Glöckner; Johannes Delp; Marcel Leist
Journal:  Cell Death Dis       Date:  2020-02-28       Impact factor: 8.469

Review 5.  The Dual Role of miR-186 in Cancers: Oncomir Battling With Tumor Suppressor miRNA.

Authors:  Ying Xiang; Qing Tian; Li Guan; Shuai-Shuai Niu
Journal:  Front Oncol       Date:  2020-03-05       Impact factor: 6.244

  5 in total

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