Targeting of Smoothened for therapeutic gain.

[1]  Anton Barty,et al.  Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography , 2014, Nature Communications.

[2]  M. K. Hadden Hedgehog Pathway Agonism: Therapeutic Potential and Small‐Molecule Development , 2014, ChemMedChem.

[3]  Jie J. Zheng,et al.  Structural insights into the role of the Smoothened cysteine-rich domain in Hedgehog signalling , 2013, Nature Communications.

[4]  F. Charron,et al.  Signaling mechanisms of non-conventional axon guidance cues: the Shh, BMP and Wnt morphogens , 2013, Current Opinion in Neurobiology.

[5]  Zainab Jagani,et al.  Unraveling the therapeutic potential of the Hedgehog pathway in cancer , 2013, Nature Medicine.

[6]  P. Ingham,et al.  Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling , 2013, eLife.

[7]  Jose M. Duarte,et al.  An analysis of oligomerization interfaces in transmembrane proteins , 2013, BMC Structural Biology.

[8]  D. Linden,et al.  Hedgehog Agonist Therapy Corrects Structural and Cognitive Deficits in a Down Syndrome Mouse Model , 2013, Science Translational Medicine.

[9]  Benjamin R. Myers,et al.  Hedgehog pathway modulation by multiple lipid binding sites on the smoothened effector of signal response. , 2013, Developmental cell.

[10]  Alberto C. S. Costa,et al.  Prospects for Improving Brain Function in Individuals with Down Syndrome , 2013, CNS Drugs.

[11]  L. Devi,et al.  Identification of a μ-δ opioid receptor heteromer-biased agonist with antinociceptive activity , 2013, Proceedings of the National Academy of Sciences.

[12]  J. Briscoe,et al.  The mechanisms of Hedgehog signalling and its roles in development and disease , 2013, Nature Reviews Molecular Cell Biology.

[13]  Yangqing Xu,et al.  Oxysterol binding to the extracellular domain of Smoothened in Hedgehog signaling , 2013, Nature chemical biology.

[14]  Bryan L. Roth,et al.  Structure of the human smoothened receptor bound to an antitumour agent , 2013, Nature.

[15]  T. Gorojankina,et al.  Discovery, Molecular and Pharmacological Characterization of GSA-10, a Novel Small-Molecule Positive Modulator of Smoothened , 2013, Molecular Pharmacology.

[16]  C. Rudin,et al.  Phase I Study of the Hedgehog Pathway Inhibitor IPI-926 in Adult Patients with Solid Tumors , 2013, Clinical Cancer Research.

[17]  Zhaocai Zhou,et al.  Smoothened Oligomerization/Higher Order Clustering in Lipid Rafts Is Essential for High Hedgehog Activity Transduction* , 2013, The Journal of Biological Chemistry.

[18]  Didier Rognan,et al.  Encoding Protein-Ligand Interaction Patterns in Fingerprints and Graphs , 2013, J. Chem. Inf. Model..

[19]  A. Gulino,et al.  Control of stem cells and cancer stem cells by Hedgehog signaling: pharmacologic clues from pathway dissection. , 2013, Biochemical pharmacology.

[20]  Arthur Christopoulos,et al.  Signalling bias in new drug discovery: detection, quantification and therapeutic impact , 2012, Nature Reviews Drug Discovery.

[21]  N. Riobo,et al.  Smoothened Is a Fully Competent Activator of the Heterotrimeric G Protein Gi , 2013, Molecular Pharmacology.

[22]  M. K. Hadden Hedgehog pathway inhibitors: a patent review (2009 – present) , 2013, Expert opinion on therapeutic patents.

[23]  C. Zimmer,et al.  Sonic Hedgehog Signaling Is a Positive Oligodendrocyte Regulator during Demyelination , 2013, The Journal of Neuroscience.

[24]  L. Rangell,et al.  The Ciliary G-Protein-Coupled Receptor Gpr161 Negatively Regulates the Sonic Hedgehog Pathway via cAMP Signaling , 2013, Cell.

[25]  C. Rudin,et al.  Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonists. , 2013, Cancer cell.

[26]  Liping Xu,et al.  Heterobivalent ligands target cell-surface receptor combinations in vivo , 2012, Proceedings of the National Academy of Sciences.

[27]  R. N. Takahashi,et al.  Anti-inflammatory lipoxin A4 is an endogenous allosteric enhancer of CB1 cannabinoid receptor , 2012, Proceedings of the National Academy of Sciences.

[28]  A. Chang,et al.  Initial assessment of tumor regrowth after vismodegib in advanced Basal cell carcinoma. , 2012, Archives of dermatology.

[29]  K. Seifert,et al.  Potent small molecule Hedgehog agonists induce VEGF expression in vitro. , 2012, Bioorganic & medicinal chemistry.

[30]  R. Rohatgi,et al.  A Smoothened-Evc2 complex transduces the Hedgehog signal at primary cilia. , 2012, Developmental cell.

[31]  A. Chang,et al.  Hedgehog pathway inhibition and the race against tumor evolution , 2012, The Journal of cell biology.

[32]  M. Febbraio,et al.  Hedgehog Partial Agonism Drives Warburg-like Metabolism in Muscle and Brown Fat , 2012, Cell.

[33]  A. McMahon,et al.  Glucocorticoid compounds modify smoothened localization and hedgehog pathway activity. , 2012, Chemistry & biology.

[34]  J. Zwerina,et al.  Hedgehog signaling controls fibroblast activation and tissue fibrosis in systemic sclerosis. , 2012, Arthritis and rheumatism.

[35]  Luis E. Gonzalez-Reyes,et al.  Sonic Hedgehog Maintains Cellular and Neurochemical Homeostasis in the Adult Nigrostriatal Circuit , 2012, Neuron.

[36]  K. Garcia,et al.  Structural Basis of Wnt Recognition by Frizzled , 2012, Science.

[37]  A. Mauviel,et al.  Crosstalk between TGF‐β and hedgehog signaling in cancer , 2012, FEBS letters.

[38]  W. Matsui,et al.  Molecular Pathways Molecular Pathways : The Hedgehog Signaling Pathway in Cancer , 2012 .

[39]  Kris Chang,et al.  Inhibiting the hedgehog pathway in patients with the basal-cell nevus syndrome. , 2012, The New England journal of medicine.

[40]  Aleksandar Sekulic,et al.  Efficacy and safety of vismodegib in advanced basal-cell carcinoma. , 2012, The New England journal of medicine.

[41]  J. Olson,et al.  Hedgehog pathway inhibitor saridegib (IPI-926) increases lifespan in a mouse medulloblastoma model , 2012, Proceedings of the National Academy of Sciences.

[42]  W. Matsui,et al.  Hedgehog pathway as a drug target: Smoothened inhibitors in development , 2012, OncoTargets and therapy.

[43]  Oliver Distler,et al.  Basic and translational research , 2011 .

[44]  M. Ruat,et al.  Hedgehog trafficking, cilia and brain functions. , 2012, Differentiation; research in biological diversity.

[45]  P. Schlesinger,et al.  Oxysterols are allosteric activators of the oncoprotein Smoothened , 2011, Nature chemical biology.

[46]  M. Mahoney,et al.  Noncanonical Hedgehog signaling. , 2012, Vitamins and hormones.

[47]  J. Distler,et al.  Morphogen Pathways in Systemic Sclerosis , 2012, Current Rheumatology Reports.

[48]  M. Galko,et al.  Hedgehog Signaling Regulates Nociceptive Sensitization , 2011, Current Biology.

[49]  A. McMahon,et al.  Boc and Gas1 each form distinct Shh receptor complexes with Ptch1 and are required for Shh-mediated cell proliferation. , 2011, Developmental cell.

[50]  A. McMahon,et al.  Overlapping roles and collective requirement for the coreceptors GAS1, CDO, and BOC in SHH pathway function. , 2011, Developmental cell.

[51]  T. Curran,et al.  The Hedgehog's tale: developing strategies for targeting cancer , 2011, Nature Reviews Cancer.

[52]  N. Riobo,et al.  Heterotrimeric Gi Proteins Link Hedgehog Signaling to Activation of Rho Small GTPases to Promote Fibroblast Migration* , 2011, The Journal of Biological Chemistry.

[53]  A. Louvi,et al.  Cilia in the CNS: The Quiet Organelle Claims Center Stage , 2011, Neuron.

[54]  T. Gorojankina,et al.  Identification and Mechanism of Action of the Acylguanidine MRT-83, a Novel Potent Smoothened Antagonist , 2011, Molecular Pharmacology.

[55]  L. N. Borodinsky,et al.  Sonic hedgehog signaling is decoded by calcium spike activity in the developing spinal cord , 2011, Proceedings of the National Academy of Sciences.

[56]  S. Pons,et al.  Sonic Hedgehog-induced Proliferation Requires Specific Gα Inhibitory Proteins* , 2011, The Journal of Biological Chemistry.

[57]  F. D. de Sauvage,et al.  Clinical experience with Hedgehog pathway inhibitors. , 2010, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[58]  Jing Yuan,et al.  Interfering with Resistance to Smoothened Antagonists by Inhibition of the PI3K Pathway in Medulloblastoma , 2010, Science Translational Medicine.

[59]  A. Giannis,et al.  Modulators of the hedgehog signaling pathway. , 2010, Bioorganic & medicinal chemistry.

[60]  B. Wang,et al.  G protein-coupled receptor kinase 2 promotes high-level Hedgehog signaling by regulating the active state of Smo through kinase-dependent and kinase-independent mechanisms in Drosophila. , 2010, Genes & development.

[61]  S. Peukert,et al.  Small‐Molecule Inhibitors of the Hedgehog Signaling Pathway as Cancer Therapeutics , 2010, ChemMedChem.

[62]  X. Ren,et al.  Identification of select glucocorticoids as Smoothened agonists: Potential utility for regenerative medicine , 2010, Proceedings of the National Academy of Sciences.

[63]  M. Ruat,et al.  Sonic Hedgehog signaling in the mammalian brain , 2010, Journal of neurochemistry.

[64]  K. Anderson,et al.  The primary cilium: a signalling centre during vertebrate development , 2010, Nature Reviews Genetics.

[65]  Jun O. Liu,et al.  Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. , 2010, Cancer cell.

[66]  S. Peukert,et al.  Small‐Molecule Inhibitors of the Hedgehog Signaling Pathway as Cancer Therapeutics , 2010, ChemMedChem.

[67]  L. Yang,et al.  Activation of the hedgehog-signaling pathway in human cancer and the clinical implications , 2010, Oncogene.

[68]  Jeremy Stinson,et al.  Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449. , 2009, The New England journal of medicine.

[69]  David S. Goodsell,et al.  AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility , 2009, J. Comput. Chem..

[70]  B. Alman,et al.  Modulating hedgehog signaling can attenuate the severity of osteoarthritis , 2009, Nature Medicine.

[71]  M. Scott,et al.  Lateral transport of Smoothened from the plasma membrane to the membrane of the cilium , 2009, The Journal of cell biology.

[72]  C. Rudin,et al.  Smoothened Mutation Confers Resistance to a Hedgehog Pathway Inhibitor in Medulloblastoma , 2009, Science.

[73]  A. Álvarez-Buylla,et al.  Dual and opposing roles of primary cilia in medulloblastoma development , 2009, Nature Medicine.

[74]  L. Rubin,et al.  Potent agonists of the Hedgehog signaling pathway. , 2009, Bioorganic & medicinal chemistry letters.

[75]  D. Jenkins Hedgehog signalling: emerging evidence for non-canonical pathways. , 2009, Cellular signalling.

[76]  Joseph L. Goldstein,et al.  Structure of N-Terminal Domain of NPC1 Reveals Distinct Subdomains for Binding and Transfer of Cholesterol , 2009, Cell.

[77]  F. D. de Sauvage,et al.  Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. , 2009, Trends in pharmacological sciences.

[78]  W. Zuercher,et al.  Evidence for Allosteric Interactions of Antagonist Binding to the Smoothened Receptor , 2009, Journal of Pharmacology and Experimental Therapeutics.

[79]  F. Charron,et al.  Sonic Hedgehog Guides Axons through a Noncanonical, Src-Family-Kinase-Dependent Signaling Pathway , 2009, Neuron.

[80]  Shuo Lin,et al.  Converse Conformational Control of Smoothened Activity by Structurally Related Small Molecules* , 2009, The Journal of Biological Chemistry.

[81]  P. Chuang,et al.  Smoothened Adopts Multiple Active and Inactive Conformations Capable of Trafficking to the Primary Cilium , 2009, PloS one.

[82]  M. Scott,et al.  Hedgehog signal transduction by Smoothened: Pharmacologic evidence for a 2-step activation process , 2009, Proceedings of the National Academy of Sciences.

[83]  D. Rowitch,et al.  Hedgehog signaling has a protective effect in glucocorticoid-induced mouse neonatal brain injury through an 11betaHSD2-dependent mechanism. , 2009, The Journal of clinical investigation.

[84]  Robert Machold,et al.  Medulloblastoma can be initiated by deletion of Patched in lineage-restricted progenitors or stem cells. , 2008, Cancer cell.

[85]  R. Lefkowitz,et al.  β-Arrestin–Mediated Localization of Smoothened to the Primary Cilium , 2008, Science.

[86]  Hua Tian,et al.  A paracrine requirement for hedgehog signalling in cancer , 2008, Nature.

[87]  J. García-Verdugo,et al.  Hedgehog signaling and primary cilia are required for the formation of adult neural stem cells , 2008, Nature Neuroscience.

[88]  Yun Zhao,et al.  Hedgehog regulates smoothened activity by inducing a conformational switch , 2007, Nature.

[89]  P. Walsh Hedgehog signalling in prostate regeneration, neoplasia and metastasis. , 2005, The Journal of urology.

[90]  Yasuko Nakamura,et al.  The Upregulated Expression of Sonic Hedgehog in Motor Neurons after Rat Facial Nerve Axotomy , 2004, The Journal of Neuroscience.

[91]  P. Schultz,et al.  Purmorphamine induces osteogenesis by activation of the hedgehog signaling pathway. , 2004, Chemistry & biology.

[92]  Yutaka Shimada,et al.  Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours , 2003, Nature.

[93]  Stephen B. Baylin,et al.  Hedgehog signalling within airway epithelial progenitors and in small-cell lung cancer , 2003, Nature.

[94]  H. Wichterle,et al.  Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists , 2002, Journal of biology.

[95]  Jussi Taipale,et al.  Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened. , 2002, Genes & development.

[96]  Jussi Taipale,et al.  Small molecule modulation of Smoothened activity , 2002, Proceedings of the National Academy of Sciences of the United States of America.

[97]  T. Engber,et al.  Behavioural and immunohistochemical changes following supranigral administration of sonic hedgehog in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated common marmosets , 2002, Neuroscience.

[98]  James M. Olson,et al.  Medulloblastoma Growth Inhibition by Hedgehog Pathway Blockade , 2002, Science.

[99]  C. Shults,et al.  Intrastriatal Injection of Sonic Hedgehog Reduces Behavioral Impairment in a Rat Model of Parkinson's Disease , 2002, Experimental Neurology.

[100]  M. Scott,et al.  Effects of oncogenic mutations in Smoothened and Patched can be reversed by cyclopamine , 2000, Nature.

[101]  M. Ruat,et al.  Regional Distribution of Sonic Hedgehog, Patched, and Smoothened mRNA in the Adult Rat Brain , 1998, Journal of neurochemistry.

[102]  Q. Gu,et al.  Activating Smoothened mutations in sporadic basal-cell carcinoma , 1998, Nature.