Overcoming the emerging drug resistance of smoothened: an overview of small-molecule SMO antagonists with antiresistance activity

Strategies to target the Hedgehog signaling pathway for cancer therapy

(2018) Minhang Xin et al.   MEDICINAL RESEARCH REVIEWS

Design, synthesis, and biological evaluation of structurally modified isoindolinone and quinazolinone derivatives as hedgehog pathway inhibitors

(2017) Deepak Bhattarai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer

(2017) Floriana Morgillo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription

(2017) Gang Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Palladium-Catalyzed Synthesis, and Biological Investigation of 2-Substituted 3-Aroylquinolin-4(1H)-ones as Inhibitors of the Hedgehog Signaling Pathway

(2017) Romina Alfonsi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand

(2017) Xianjun Zhang et al.   Nature Communications

Cellular Cholesterol Directly Activates Smoothened in Hedgehog Signaling

(2016) Pengxiang Huang et al.   CELL

Hedgehog Pathway Inhibition

(2016) Aleksandar Sekulic et al.   CELL

Hedgehog signaling pathway: a novel model and molecular mechanisms of signal transduction

(2016) Tatiana Gorojankina   CELLULAR AND MOLECULAR LIFE SCIENCES

Molecular docking study of natural alkaloids as multi-targeted hedgehog pathway inhibitors in cancer stem cell therapy

(2016) Mayank et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

Evaluation of WO2014207069 A1: Multitarget Hedgehog pathway inhibitors and uses thereof

(2016) Fabrizio Manetti et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Posaconazole, a Second-Generation Triazole Antifungal Drug, Inhibits the Hedgehog Signaling Pathway and Progression of Basal Cell Carcinoma

(2016) B. Chen et al.   MOLECULAR CANCER THERAPEUTICS

Structural basis of Smoothened regulation by its extracellular domains

(2016) Eamon F. X. Byrne et al.   NATURE

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

(2016) Navdar Sever et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sonidegib: A Review in Locally Advanced Basal Cell Carcinoma

(2016) Celeste B. Burness et al.   Targeted Oncology

DYRK1B as therapeutic target in Hedgehog/GLI-dependent cancer cells with Smoothened inhibitor resistance

(2016) Wolfgang Gruber et al.   Oncotarget

Novel small molecules targeting ciliary transport of Smoothened and oncogenic Hedgehog pathway activation

(2016) Bomi Jung et al.   Scientific Reports

Targeting the Sonic Hedgehog Signaling Pathway: Review of Smoothened and GLI Inhibitors

(2016) Tadas Rimkus et al.   Cancers

Identification of Novel Smoothened Ligands Using Structure-Based Docking

(2016) Celine Lacroix et al.   PLoS One

Smoothened Variants Explain the Majority of Drug Resistance in Basal Cell Carcinoma

(2015) Scott X. Atwood et al.   CANCER CELL

Genomic Analysis of Smoothened Inhibitor Resistance in Basal Cell Carcinoma

(2015) Hayley J. Sharpe et al.   CANCER CELL

SMO Gene Amplification and Activation of the Hedgehog Pathway as Novel Mechanisms of Resistance to Anti-Epidermal Growth Factor Receptor Drugs in Human Lung Cancer

(2015) C. M. Della Corte et al.   CLINICAL CANCER RESEARCH

An Investigator-Initiated Open-Label Trial of Sonidegib in Advanced Basal Cell Carcinoma Patients Resistant to Vismodegib

(2015) C. Danial et al.   CLINICAL CANCER RESEARCH

A comprehensive review of the role of the hedgehog pathway and vismodegib in the management of basal cell carcinoma

(2015) Gökmen Umut Erdem et al.   CURRENT MEDICAL RESEARCH AND OPINION

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

(2015) Lucile Hoch et al.   FASEB JOURNAL

Targeting GLI factors to inhibit the Hedgehog pathway

(2015) Paola Infante et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Targeting the Hedgehog signaling pathway in cancer: beyond Smoothened

(2015) Annelies Gonnissen et al.   Oncotarget

Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists

(2014) Tian-Ming Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Genome Sequencing of SHH Medulloblastoma Predicts Genotype-Related Response to Smoothened Inhibition

(2014) Marcel Kool et al.   CANCER CELL

Gli1/DNA interaction is a druggable target for Hedgehog-dependent tumors

(2014) P. Infante et al.   EMBO JOURNAL

Recent advances in the design of Hedgehog pathway inhibitors for the treatment of malignancies

(2014) Upasana Banerjee et al.   Expert Opinion on Drug Discovery

New Pyrrole Derivatives with Potent Tubulin Polymerization Inhibiting Activity As Anticancer Agents Including Hedgehog-Dependent Cancer

(2014) Giuseppe La Regina et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acquired resistance to the Hedgehog pathway inhibitor vismodegib due to smoothened mutations in treatment of locally advanced basal cell carcinoma

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

Smoothened (SMO) receptor mutations dictate resistance to vismodegib in basal cell carcinoma

(2014) Sabrina Pricl et al.   Molecular Oncology

Identification of recurrent SMO and BRAF mutations in ameloblastomas

(2014) Robert T Sweeney et al.   NATURE GENETICS

Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition

(2014) Yujie Tang et al.   NATURE MEDICINE

Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs

(2014) Chong Wang et al.   Nature Communications

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

PTEN Loss Mitigates the Response of Medulloblastoma to Hedgehog Pathway Inhibition

(2013) C. Metcalfe et al.   CANCER RESEARCH

Discovery of NVP-LEQ506, a Second-Generation Inhibitor of Smoothened

(2013) Stefan Peukert et al.   ChemMedChem

Rationally Designed Multitarget Anti-HIV Agents

(2013) P. Zhan et al.   CURRENT MEDICINAL CHEMISTRY

Hedgehog Pathway Modulation by Multiple Lipid Binding Sites on the Smoothened Effector of Signal Response

(2013) Benjamin R. Myers et al.   DEVELOPMENTAL CELL

Inhibition mechanism exploration of investigational drug TAK-441 as inhibitor against Vismodegib-resistant Smoothened mutant

(2013) Tsuyoshi Ishii et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Structure of the human smoothened receptor bound to an antitumour agent

(2013) Chong Wang et al.   NATURE

Oxysterol binding to the extracellular domain of Smoothened in Hedgehog signaling

(2013) Daniel Nedelcu et al.   Nature Chemical Biology

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

Selective Identification of Hedgehog Pathway Antagonists By Direct Analysis of Smoothened Ciliary Translocation

(2012) Yu Wang et al.   ACS Chemical Biology

Initial Assessment of Tumor Regrowth After Vismodegib in Advanced Basal Cell Carcinoma

(2012) Anne Lynn S. Chang et al.   ARCHIVES OF DERMATOLOGY

Discovery of pyrrolo[3,2-c]quinoline-4-one derivatives as novel hedgehog signaling inhibitors

(2012) Tomohiro Ohashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of the investigational drug TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: Modification of the core skeleton for improved solubility

(2012) Tomohiro Ohashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling

(2012) Jiangbo Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Glucocorticoid Compounds Modify Smoothened Localization and Hedgehog Pathway Activity

(2012) Yu Wang et al.   CHEMISTRY & BIOLOGY

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

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

Hedgehog pathway inhibitor saridegib (IPI-926) increases lifespan in a mouse medulloblastoma model

(2012) M. J. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Hedgehog Signal Transduction Network

(2012) D. J. Robbins et al.   Science Signaling

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

(2011) Haiyan Tao et al.   CHEMISTRY & BIOLOGY

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

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

(2010) F. Manetti et al.   MOLECULAR PHARMACOLOGY

Arsenic antagonizes the Hedgehog pathway by preventing ciliary accumulation and reducing stability of the Gli2 transcriptional effector

(2010) J. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity

(2009) Karen Miller-Moslin et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Hedgehog: functions and mechanisms

(2008) M. Varjosalo et al.   GENES & DEVELOPMENT