Literature DB >> 24703627

Targeting of Smoothened for therapeutic gain.

Martial Ruat1, Lucile Hoch2, Hélène Faure2, Didier Rognan3.   

Abstract

The Smoothened (Smo) receptor is a key transducer of the Hedgehog (Hh) signaling pathway, which plays a critical role in tissue maintenance and repair. Recent studies have highlighted the therapeutic value of Smo antagonists for treating Hh-linked cancers. Research on Smo agonists indicates that these molecules are important not only for delineating canonical versus noncanonical Hh signaling but also for understanding the role of Smo in physiological and pathological conditions. This review provides an update on the potential therapeutic importance of Smo modulators, and unravels the increasing complexity of its pharmacology with regard to clinical implications.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Hedgehog; bias agonism; cancer; neurodegenerative disease; stem cell

Mesh：

Substances：

Year:  2014        PMID： 24703627     DOI： 10.1016/j.tips.2014.03.002

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN： 0165-6147            Impact factor:   14.819


  41 in total

Review 1.  Synthetic Small Molecule Inhibitors of Hh Signaling As Anti-Cancer Chemotherapeutics.

Authors:  C A Maschinot; J R Pace; M K Hadden
Journal:  Curr Med Chem       Date:  2015       Impact factor: 4.530

2.  Endogenous B-ring oxysterols inhibit the Hedgehog component Smoothened in a manner distinct from cyclopamine or side-chain oxysterols.

Authors:  Navdar Sever; Randall K Mann; Libin Xu; William J Snell; Carmen I Hernandez-Lara; Ned A Porter; Philip A Beachy
Journal:  Proc Natl Acad Sci U S A       Date:  2016-05-09       Impact factor: 11.205

3.  α-catenin. A tumor suppressor beyond adherens junctions.

Authors:  Yutong Sun; Jinsong Zhang; Li Ma
Journal:  Cell Cycle       Date:  2014       Impact factor: 4.534

4.  MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor.

Authors:  Lucile Hoch; Helene Faure; Hermine Roudaut; Angele Schoenfelder; Andre Mann; Nicolas Girard; Laure Bihannic; Olivier Ayrault; Elena Petricci; Maurizio Taddei; Didier Rognan; Martial Ruat
Journal:  FASEB J       Date:  2015-01-30       Impact factor: 5.191

5.  Inversion of Sonic hedgehog action on its canonical pathway by electrical activity.

Authors:  Yesser H Belgacem; Laura N Borodinsky
Journal:  Proc Natl Acad Sci U S A       Date:  2015-03-17       Impact factor: 11.205

Review 6.  Regulation of the oncoprotein Smoothened by small molecules.

Authors:  Hayley J Sharpe; Weiru Wang; Rami N Hannoush; Frederic J de Sauvage
Journal:  Nat Chem Biol       Date:  2015-04       Impact factor: 15.040

7.  Association between donor and recipient smoothened gene polymorphisms and the risk of hepatocellular carcinoma recurrence following orthotopic liver transplantation in a Han Chinese population.

Authors:  Pusen Wang; Weiyong Song; Hao Li; Cunguang Wang; Baojie Shi; Wenzhi Guo; Lin Zhong
Journal:  Tumour Biol       Date:  2015-05-06

8.  Rapid, direct activity assays for Smoothened reveal Hedgehog pathway regulation by membrane cholesterol and extracellular sodium.

Authors:  Benjamin R Myers; Lila Neahring; Yunxiao Zhang; Kelsey J Roberts; Philip A Beachy
Journal:  Proc Natl Acad Sci U S A       Date:  2017-12-11       Impact factor: 11.205

9.  Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice.

Authors:  Eric W Fish; Scott E Parnell; Kathleen K Sulik; Lorinda K Baker; Laura B Murdaugh; David Lamson; Kevin P Williams
Journal:  Birth Defects Res       Date:  2017-01-20       Impact factor: 2.344

10.  Disruption of the ciliary GTPase Arl13b suppresses Sonic hedgehog overactivation and inhibits medulloblastoma formation.

Authors:  Sarah N Bay; Alyssa B Long; Tamara Caspary
Journal:  Proc Natl Acad Sci U S A       Date:  2018-01-29       Impact factor: 11.205
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