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

Open-Label, Exploratory Phase II Trial of Oral Itraconazole for the Treatment of Basal Cell Carcinoma

(2014) Daniel J. Kim et al.   JOURNAL OF CLINICAL ONCOLOGY

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(2014) Tjinta Brinkhuizen et al.   JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Targeting of Smoothened for therapeutic gain

(2014) Martial Ruat et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography

(2014) Uwe Weierstall et al.   Nature Communications

Itraconazole and Arsenic Trioxide Inhibit Hedgehog Pathway Activation and Tumor Growth Associated with Acquired Resistance to Smoothened Antagonists

(2013) James Kim et al.   CANCER CELL

Hedgehog Pathway Agonism: Therapeutic Potential and Small-Molecule Development

(2013) M. Kyle Hadden   ChemMedChem

Hedgehog pathway inhibitors: a patent review (2009 – present)

(2013) Matthew Kyle Hadden   EXPERT OPINION ON THERAPEUTIC PATENTS

Structure of the human smoothened receptor bound to an antitumour agent

(2013) Chong Wang et al.   NATURE

Unraveling the therapeutic potential of the Hedgehog pathway in cancer

(2013) Dereck Amakye et al.   NATURE MEDICINE

The mechanisms of Hedgehog signalling and its roles in development and disease

(2013) James Briscoe et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Structural insights into the role of the Smoothened cysteine-rich domain in Hedgehog signalling

(2013) Rajashree Rana et al.   Nature Communications

Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling

(2013) Sigrid Nachtergaele et al.   eLife

Hedgehog Partial Agonism Drives Warburg-like Metabolism in Muscle and Brown Fat

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Molecular Pathways: The Hedgehog Signaling Pathway in Cancer

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Acylthiourea, Acylurea, and Acylguanidine Derivatives with Potent Hedgehog Inhibiting Activity

(2012) Antonio Solinas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hedgehog pathway as a drug target: Smoothened inhibitors in development

(2012) Tara Lin et al.   OncoTargets and Therapy

Small Molecule Antagonists in Distinct Binding Modes Inhibit Drug-Resistant Mutant of Smoothened

(2011) Haiyan Tao et al.   CHEMISTRY & BIOLOGY

Phase I Trial of Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) in Patients with Refractory, Locally Advanced or Metastatic Solid Tumors

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Hedgehog trafficking, cilia and brain functions

(2011) Martial Ruat et al.   DIFFERENTIATION

Itraconazole, a Commonly Used Antifungal that Inhibits Hedgehog Pathway Activity and Cancer Growth

(2010) James Kim et al.   CANCER CELL

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance

(2010) Gerrit J. P. Dijkgraaf et al.   CANCER RESEARCH

Identification and Mechanism of Action of the Acylguanidine MRT-83, a Novel Potent Smoothened Antagonist

(2010) H. Roudaut et al.   MOLECULAR PHARMACOLOGY

Virtual Screening-Based Discovery and Mechanistic Characterization of the Acylthiourea MRT-10 Family as Smoothened Antagonists

(2010) F. Manetti et al.   MOLECULAR PHARMACOLOGY

Interfering with Resistance to Smoothened Antagonists by Inhibition of the PI3K Pathway in Medulloblastoma

(2010) S. Buonamici et al.   Science Translational Medicine

Towards an integrated view of Wnt signaling in development

(2009) R. van Amerongen et al.   DEVELOPMENT

Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer

(2009) Baozhi Chen et al.   Nature Chemical Biology

Dual and opposing roles of primary cilia in medulloblastoma development

(2009) Young-Goo Han et al.   NATURE MEDICINE

Treatment of Medulloblastoma with Hedgehog Pathway Inhibitor GDC-0449

(2009) Charles M. Rudin et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of the Hedgehog Pathway in Advanced Basal-Cell Carcinoma

(2009) Daniel D. Von Hoff et al.   NEW ENGLAND JOURNAL OF MEDICINE

Small-molecule inhibitors reveal multiple strategies for Hedgehog pathway blockade

(2009) J. M. Hyman et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Hedgehog signal transduction by Smoothened: Pharmacologic evidence for a 2-step activation process

(2009) R. Rohatgi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Smoothened Mutation Confers Resistance to a Hedgehog Pathway Inhibitor in Medulloblastoma

(2009) R. L. Yauch et al.   SCIENCE

Mechanisms of Hedgehog pathway activation in cancer and implications for therapy

(2009) Suzie J. Scales et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Post-transcriptional down-regulation of Atoh1/Math1 by bone morphogenic proteins suppresses medulloblastoma development

(2008) H. Zhao et al.   GENES & DEVELOPMENT