Small molecule modulation of Smoothened activity

By James Chen, Jussi Taipale, K. Young, T. Maiti, P. Beachy. Proceedings of the National Academy of Sciences of the United States of America, 2002

1,013 citations recorded by the source corpus.

Subfields: Genetics, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/04efb5044cabe130bff5bc3d73338f823e7ed248

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Citations in the corpus

Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened. (2002, background): “Similar changes in SmoA1 localization were observed with an Hh pathway agonist that also acts directly on Smo (SAG; Chen et al. 2002; FrankKamenetsky et al. 2002; Fig.”
Pattern formation in the vertebrate neural tube: a sonic hedgehog morphogen-regulated transcriptional network (2008, background): “Use of small-molecule antagonists and Smo agonists in neural cells indicate that a graded activation of Smo recapitulates the graded cellular response to a Shh concentration gradient (Chen et al., 2002a; Chen et al., 2002b; Dessaud et al., 2007; Frank- Kamenetsky et al., 2002).”
Cyclopamine‐Mediated Hedgehog Pathway Inhibition Depletes Stem‐Like Cancer Cells in Glioblastoma (2007, methodology): “As a positive control, we used conditioned medium isolated from Shh-N-producing HEK 293 cells [ 40 ].”
Hedgehog Signaling in Development and Cancer (2008, neutral): “Indeed, a number of natural and synthetic small molecules can inhibit or activate the Hh pathway at the level of Smo (Chen et al., 2002).”
Small-molecule antagonists of the oncogenic Tcf/β-catenin protein complex (2004, background): “To evaluate specificity of the active chemicals, tions are also vulnerable to small-molecule interference (Berg et al., 2002; Chen et al., 2002) and define allosteric interactionswe determined their effect on the presence of E-cadherin and APC in -catenin immunoprecipitates from HCT116 and HT29…”
Targeting the Hedgehog pathway in cancer (2006, background): “The clear connection between activation of Hh signalling in basal cells of the skin and the formation of BCC lesions led to a series of studies designed to identify small-molecule Hh antagonist”
Communicating with Hedgehogs (2005, background): “Various cyclopamine mimics (and other small molecules) bind to the transmembrane helices of SMO and either activate or inhibit signallin”
Tissue repair and stem cell renewal in carcinogenesis (2004, result): “Consistent with this possibility, recent studies using cyclopamine, a specific Hh pathway antagonis”
Hedgehog signalling within airway epithelial progenitors and in small-cell lung cancer (2003, background): “through interaction with the Hh signalling protein smoothene”
Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours (2003, methodology): “Hh-responsive reporter assays Hh-responsive firefly luciferase and control SV40 Renilla luciferase reporter assays were performed on subconfluent triplicate cultures as described previousl”