State of the art of Smo antagonists for cancer therapy: advances in the target receptor and new ligand structures

Hedgehog pathway and smoothened inhibitors in cancer therapies

(2018) Kirti K. Chahal et al.   ANTI-CANCER DRUGS

Oncogenic Signaling Pathways in The Cancer Genome Atlas

(2018) Francisco Sanchez-Vega et al.   CELL

Structural Basis of Smoothened Activation in Hedgehog Signaling

(2018) Pengxiang Huang et al.   CELL

GPCRs: Emerging anti-cancer drug targets

(2018) Ainhoa Nieto Gutierrez et al.   CELLULAR SIGNALLING

Overcoming the resistance mechanisms of Smoothened inhibitors

(2018) Xiaochun Dong et al.   DRUG DISCOVERY TODAY

Vismodegib: A Review in Advanced Basal Cell Carcinoma

(2018) James E. Frampton et al.   DRUGS

Strategies to target the Hedgehog signaling pathway for cancer therapy

(2018) Minhang Xin et al.   MEDICINAL RESEARCH REVIEWS

Molecular modeling study on resistance of WT/D473H SMO to antagonists LDE-225 and LEQ-506

(2018) Jing Tu et al.   PHARMACOLOGICAL RESEARCH

A novel hedgehog inhibitor for the treatment of hematological malignancies

(2018) Peng Lin et al.   ANTI-CANCER DRUGS

Role of GLI Transcription Factors in Pathogenesis and Their Potential as New Therapeutic Targets

(2018) Maja Sabol et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Trends in GPCR drug discovery: new agents, targets and indications

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

The role of canonical and non-canonical Hedgehog signaling in tumor progression in a mouse model of small cell lung cancer

(2017) A Szczepny et al.   ONCOGENE

Hijacking the Hedgehog Pathway in Cancer Therapy

(2016) Mikko O. Laukkanen et al.   Anti-Cancer Agents in Medicinal Chemistry

Cellular Cholesterol Directly Activates Smoothened in Hedgehog Signaling

(2016) Pengxiang Huang et al.   CELL

The Emerging Hallmarks of Cancer Metabolism

(2016) Natalya N. Pavlova et al.   Cell Metabolism

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

Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists

(2016) Gang Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Suppressor of Fused Chaperones Gli Proteins To Generate Transcriptional Responses to Sonic Hedgehog Signaling

(2016) Ziyu Zhang et al.   MOLECULAR AND CELLULAR BIOLOGY

Structural basis of Smoothened regulation by its extracellular domains

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

Identification of Novel Smoothened Ligands Using Structure-Based Docking

(2016) Celine Lacroix et al.   PLoS One

The Hedgehog pathway: role in cell differentiation, polarity and proliferation

(2015) Yanfei Jia et al.   ARCHIVES OF TOXICOLOGY

Vismodegib Resistance in Basal Cell Carcinoma: Not a Smooth Fit

(2015) Todd W. Ridky et al.   CANCER CELL

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

AT-101 inhibits hedgehog pathway activity and cancer growth

(2015) Juan Wang et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

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

Sonidegib: First Global Approval

(2015) Celeste B. Burness   DRUGS

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

ZINC 15 – Ligand Discovery for Everyone

(2015) Teague Sterling et al.   Journal of Chemical Information and Modeling

Rolling the Genetic Dice: Neutral and Deleterious Smoothened Mutations in Drug-Resistant Basal Cell Carcinoma

(2015) Scott X. Atwood et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Vismodegib in patients with advanced basal cell carcinoma (STEVIE): a pre-planned interim analysis of an international, open-label trial

(2015) Nicole Basset-Seguin et al.   LANCET ONCOLOGY

Regulation of the oncoprotein Smoothened by small molecules

(2015) Hayley J Sharpe et al.   Nature Chemical Biology

GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1–2 September 2014

(2015) Alexander Heifetz et al.   NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY

Evasion of anti-growth signaling: A key step in tumorigenesis and potential target for treatment and prophylaxis by natural compounds

(2015) A.R.M. Ruhul Amin et al.   SEMINARS IN CANCER BIOLOGY

Targeting GLI factors to inhibit the Hedgehog pathway

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

FOXC1 Activates Smoothened-Independent Hedgehog Signaling in Basal-like Breast Cancer

(2015) Bingchen Han et al.   Cell Reports

Signal Transduction in Cancer

(2015) R. Sever et al.   Cold Spring Harbor Perspectives in Medicine

Molecular modeling study on the dynamical structural features of human smoothened receptor and binding mechanism of antagonist LY2940680 by metadynamics simulation and free energy calculation

(2014) Qifeng Bai et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Immune Escape Mechanisms as a Guide for Cancer Immunotherapy

(2014) G. L. Beatty et al.   CLINICAL CANCER RESEARCH

Smoothened inhibitors in the treatment of advanced basal cell carcinomas

(2014) Rainer Kunstfeld   CURRENT OPINION IN ONCOLOGY

Roles for Hedgehog signaling in adult organ homeostasis and repair

(2014) R. Petrova et al.   DEVELOPMENT

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

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

Hedgehog signaling pathway: A novel target for cancer therapy: Vismodegib, a promising therapeutic option in treatment of basal cell carcinomas

(2014) Afroz Abidi   INDIAN JOURNAL OF PHARMACOLOGY

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

Hedgehog Pathway Inhibition in Chondrosarcoma Using the Smoothened Inhibitor IPI-926 Directly Inhibits Sarcoma Cell Growth

(2014) V. T. Campbell et al.   MOLECULAR CANCER THERAPEUTICS

G-protein-coupled receptors, Hedgehog signaling and primary cilia

(2014) Saikat Mukhopadhyay et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Targeting of Smoothened for therapeutic gain

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

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

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

(2013) Stefan Peukert et al.   ChemMedChem

Hedgehog Signaling Pathway and Cancer Therapeutics: Progress to Date

(2013) Joshua M. Ruch et al.   DRUGS

Molecular Similarity in Medicinal Chemistry

(2013) Gerald Maggiora et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Medicinal history of North American Veratrum

(2013) Christopher M. Chandler et al.   PHYTOCHEMISTRY REVIEWS

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

Small molecule inhibitors of the hedgehog signaling pathway for the treatment of cancer

(2012) Jeong In Yun et al.   ARCHIVES OF PHARMACAL RESEARCH

Targeting hedgehog in hematologic malignancy

(2012) D. A. Irvine et al.   BLOOD

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

(2012) Raffaele Teperino et al.   CELL

Molecular Pathways: The Hedgehog Signaling Pathway in Cancer

(2012) R. McMillan et al.   CLINICAL CANCER RESEARCH

Targeting Hedgehog signaling and understanding refractory response to treatment with Hedgehog pathway inhibitors

(2012) Karla C.S. Queiroz et al.   DRUG RESISTANCE UPDATES

Targeting the Hedgehog signaling pathway for cancer therapy

(2012) Yiwei Li et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Hedgehog pathway inhibition and the race against tumor evolution

(2012) Scott X. Atwood et al.   JOURNAL OF CELL BIOLOGY

Hedgehog-GLI Pathway in Medulloblastoma

(2012) Tenley C. Archer et al.   JOURNAL OF CLINICAL ONCOLOGY

Structural Basis of Wnt Recognition by Frizzled

(2012) C. Y. Janda et al.   SCIENCE

Hedgehog pathway as a drug target: Smoothened inhibitors in development

(2012) Tara Lin et al.   OncoTargets and Therapy

Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors

(2011) Jesus M. Ontoria et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists

(2011) Ester Muraglia et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hedgehog Fights Back: Mechanisms of Acquired Resistance against Smoothened Antagonists

(2011) C. Metcalfe et al.   CANCER RESEARCH

Exo-Cyclopamine—a stable and potent inhibitor of hedgehog-signaling

(2011) Philipp Heretsch et al.   CHEMICAL COMMUNICATIONS

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

(2011) Haiyan Tao et al.   CHEMISTRY & BIOLOGY

Mechanisms and functions of Hedgehog signalling across the metazoa

(2011) Philip W. Ingham et al.   NATURE REVIEWS GENETICS

A Perspective on Cancer Cell Metastasis

(2011) C. L. Chaffer et al.   SCIENCE

Stability study of the human G-protein coupled receptor, Smoothened

(2010) Rony Nehmé et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines

(2010) Jacob A. Kaizerman et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists

(2010) Brian S. Lucas et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

Small-Molecule Inhibitors of the Hedgehog Signaling Pathway as Cancer Therapeutics

(2010) Stefan Peukert et al.   ChemMedChem

Mechanism and evolution of cytosolic Hedgehog signal transduction

(2010) C. W. Wilson et al.   DEVELOPMENT

Conserved Binding Mode of Human β2Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography

(2010) Daniel Wacker et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist

(2010) Shifeng Pan et al.   ACS Medicinal Chemistry Letters

Review: Targeting the Hedgehog pathway in cancer

(2010) Sachin Gupta et al.   Therapeutic Advances in Medical Oncology

Synthesis and biological evaluation of SANT-2 and analogues as inhibitors of the hedgehog signaling pathway

(2009) Anita Büttner et al.   BIOORGANIC & MEDICINAL CHEMISTRY

GDC-0449—A potent inhibitor of the hedgehog pathway

(2009) Kirk D. Robarge et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a Potent and Orally Active Hedgehog Pathway Antagonist (IPI-926)

(2009) Martin R. Tremblay et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Hedgehog-Gli Signaling Pathway Inhibitors as Anticancer Agents

(2009) Neeraj Mahindroo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Trafficking, development and hedgehog

(2009) Fiona Simpson et al.   MECHANISMS OF DEVELOPMENT

Small-molecule modulators of the Sonic Hedgehog signaling pathway

(2009) Benjamin Z. Stanton et al.   Molecular BioSystems

Hedgehog signalling is essential for maintenance of cancer stem cells in myeloid leukaemia

(2009) Chen Zhao et al.   NATURE

Treatment of Medulloblastoma with Hedgehog Pathway Inhibitor GDC-0449

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

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

Semisynthetic Cyclopamine Analogues as Potent and Orally Bioavailable Hedgehog Pathway Antagonists

(2008) Martin R. Tremblay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hedgehog signaling pathway: Development of antagonists for cancer therapy

(2008) Jingwu Xie   Current Oncology Reports