Strategies to target the Hedgehog signaling pathway for cancer therapy

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

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

Synthesis and pharmacological evaluation of trifluoromethyl containing 4-(2-pyrimidinylamino)benzamides as Hedgehog signaling pathway inhibitors

(2016) Minhang Xin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and evaluation of novel benzylphthalazine derivatives as hedgehog signaling pathway inhibitors

(2016) Xiaolong Bao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hedgehog Signal Transduction: Key Players, Oncogenic Drivers, and Cancer Therapy

(2016) Ekaterina Pak et al.   DEVELOPMENTAL CELL

Discovery of novel 4-(2-pyrimidinylamino)benzamide derivatives as highly potent and orally available hedgehog signaling pathway inhibitors

(2016) Minhang Xin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thoughts on investigational hedgehog pathway inhibitors for the treatment of cancer

(2016) Tarkan Jäger et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

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

Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic

(2016) Jennifer R. Pace et al.   JOURNAL OF MEDICINAL CHEMISTRY

A phase I trial of the Hedgehog inhibitor, sonidegib (LDE225), in combination with etoposide and cisplatin for the initial treatment of extensive stage small cell lung cancer

(2016) M. Catherine Pietanza et al.   LUNG CANCER

Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview

(2016) Peter M. Fischer   MEDICINAL RESEARCH REVIEWS

Quinolone-1-(2H)-ones as hedgehog signalling pathway inhibitors

(2016) Trieu N. Trinh et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Effects of Combined Treatment With Arsenic Trioxide and Itraconazole in Patients With Refractory Metastatic Basal Cell Carcinoma

(2016) Mina S. Ally et al.   JAMA Dermatology

Hedgehog inhibitors from Artocarpus communis and Hyptis suaveolens

(2015) Midori A. Arai et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and evaluation of hedgehog signaling inhibitor with novel core system

(2015) Tomohiro Ohashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis, and evaluation of hybrid vitamin D3 side chain analogues as hedgehog pathway inhibitors

(2015) Upasana Banerjee et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Hedgehog inhibitors from Withania somnifera

(2015) Tatsuro Yoneyama et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

Management of Cutaneous and Extracutaneous Side Effects of Smoothened Inhibitor Therapy for Advanced Basal Cell Carcinoma

(2015) S. V. Mohan et al.   CLINICAL CANCER RESEARCH

Sonidegib: First Global Approval

(2015) Celeste B. Burness   DRUGS

Vitamin D3 analogues that contain modified A- and seco-B-rings as hedgehog pathway inhibitors

(2015) Albert M. DeBerardinis et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and structure–activity-relationship of tetrahydrothiazolopyridine derivatives as potent smoothened antagonists

(2015) Haikuo Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Hedgehog inhibitors: a patent review (2013 – present)

(2015) Minhang Xin   EXPERT OPINION ON THERAPEUTIC PATENTS

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

A phase II, multicenter, open-label, 3-cohort trial evaluating the efficacy and safety of vismodegib in operable basal cell carcinoma

(2015) Howard Sofen et al.   JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Phase II evaluation of IPI-926, an oral Hedgehog inhibitor, in patients with myelofibrosis

(2015) Koji Sasaki et al.   LEUKEMIA & LYMPHOMA

Targeting Notch, Hedgehog and Wnt pathways in cancer stem cells: clinical update

(2015) Naoko Takebe et al.   Nature Reviews Clinical Oncology

Squamous Change in Basal-Cell Carcinoma with Drug Resistance

(2015) Katherine J. Ransohoff et al.   NEW ENGLAND JOURNAL OF MEDICINE

Novel Small Molecule Inhibitors of Cancer Stem Cell Signaling Pathways

(2015) Danysh Abetov et al.   Stem Cell Reviews and Reports

Novel Small Molecule Inhibitors of Cancer Stem Cell Signaling Pathways

(2015) Danysh Abetov et al.   Stem Cell Reviews and Reports

Non-Canonical Hh Signaling in Cancer—Current Understanding and Future Directions

(2015) Dongsheng Gu et al.   Cancers

4-(Pyrimidin-2-ylamino)benzamide Derivatives：Design, Synthesis, and Hedgehog Signaling Pathway Inhibition Study

(2015) Liandi Zhang et al.   CHINESE JOURNAL OF ORGANIC CHEMISTRY

Physalin H fromSolanum nigrumas an Hh signaling inhibitor blocks GLI1–DNA-complex formation

(2014) Midori A Arai et al.   Beilstein Journal of Organic Chemistry

Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors

(2014) Minhang Xin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Five-membered heteroaromatic ring fused-pyrimidine derivatives: Design, synthesis, and hedgehog signaling pathway inhibition study

(2014) Liandi Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Scaffold hopping approach to a new series of smoothened antagonists

(2014) Wenfeng Lu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

A Phase I Study of PF-04449913, an Oral Hedgehog Inhibitor, in Patients with Advanced Solid Tumors

(2014) A. J. Wagner et al.   CLINICAL CANCER RESEARCH

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

Discontinued in 2013: oncology drugs

(2014) Robert Williams   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Vismodegib for the treatment of basal cell carcinoma: results and implications of the ERIVANCE BCC trial

(2014) Clio Dessinioti et al.   Future Oncology

Arsenic trioxide inhibits tumor cell growth in malignant rhabdoid tumorsin vitroandin vivoby targeting overexpressed Gli1

(2014) Kornelius Kerl et al.   INTERNATIONAL JOURNAL OF CANCER

Structure–Activity Relationships for Vitamin D3-Based Aromatic A-Ring Analogues as Hedgehog Pathway Inhibitors

(2014) Albert M. DeBerardinis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and biological study of 6,7-dihydro-5H-pyrano[2,3-d]pyrimidine derivatives as novel hedgehog signaling pathway inhibitors

(2014) Minhang Xin et al.   MEDICINAL CHEMISTRY RESEARCH

Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition

(2014) Yujie Tang et al.   NATURE MEDICINE

Canonical and non-canonical Hedgehog signalling and the control of metabolism

(2014) Raffaele Teperino et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Advances in kinase targeting: current clinical use and clinical trials

(2014) Mathias Rask-Andersen et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Interaction of vitamin D with membrane-based signaling pathways

(2014) María Jesús Larriba et al.   Frontiers in Physiology

Analogues of the Inhoffen–Lythgoe diol with anti-proliferative activity

(2013) Albert M. DeBerardinis et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors

(2013) Minhang Xin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway

(2013) Minhang Xin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

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

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

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

(2013) Matthew Kyle Hadden   EXPERT OPINION ON THERAPEUTIC PATENTS

Mutations in Hedgehog pathway genes in fetal rhabdomyomas

(2013) Simone Hettmer et al.   JOURNAL OF PATHOLOGY

Discovery of Small-Molecule Modulators of the Sonic Hedgehog Pathway

(2013) Giannina I. Schaefer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Hh signaling inhibitors from Vitex negundo; naturally occurring inhibitors of the GLI1–DNA complex

(2013) Midori A. Arai et al.   Molecular BioSystems

Structure of the human smoothened receptor bound to an antitumour agent

(2013) Chong Wang et al.   NATURE

Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling

(2013) Elissaveta Petrova et al.   Nature Chemical Biology

Unraveling the therapeutic potential of the Hedgehog pathway in cancer

(2013) Dereck Amakye et al.   NATURE MEDICINE

Distinct cellular origin and genetic requirement of Hedgehog-Gli in postnatal rhabdomyosarcoma genesis

(2013) M Rajurkar et al.   ONCOGENE

Targeting Gli transcription activation by small molecule suppresses tumor growth

(2013) G Bosco-Clément et al.   ONCOGENE

Hedgehog signalling pathway inhibitors as cancer suppressing agents

(2013) Trieu N. Trinh et al.   MedChemComm

Identification of Vitamin D3-Based Hedgehog Pathway Inhibitors That Incorporate an Aromatic A-Ring Isostere

(2013) Albert M. DeBerardinis et al.   ACS Medicinal Chemistry Letters

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

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO

(2012) Bin Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Canonical and noncanonical Hedgehog pathway in the pathogenesis of multiple myeloma

(2012) S. Blotta et al.   BLOOD

Abstract 2819: Identification and characterization of a novel smoothened antagonist for the treatment of cancer with deregulated hedgehog signaling

(2012) Mark H. Bender et al.   CANCER RESEARCH

Glucocorticoid Compounds Modify Smoothened Localization and Hedgehog Pathway Activity

(2012) Yu Wang et al.   CHEMISTRY & BIOLOGY

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

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

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

Medulloblastoma exome sequencing uncovers subtype-specific somatic mutations

(2012) Trevor J. Pugh et al.   NATURE

Dissecting the genomic complexity underlying medulloblastoma

(2012) David T. W. Jones et al.   NATURE

Hedgehog hopes lifted by approval... and stung by failure

(2012) Malorye Allison   NATURE BIOTECHNOLOGY

Vismodegib

(2012) Andrzej Dlugosz et al.   NATURE REVIEWS DRUG DISCOVERY

Development of a Scalable Route to the SMO Receptor Antagonist SEN794

(2012) Matteo Betti et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies

(2012) Chris Dockendorff et al.   ACS Medicinal Chemistry Letters

Synthesis and biological evaluation of desmethylveramiline, a micromolar Hedgehog inhibitor

(2011) Guillaume Guerlet et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 1

(2011) Savina Malancona et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2

(2011) Olaf Kinzel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit

(2011) Matthew L. Brown et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Vitamin D3 Inhibits Hedgehog Signaling and Proliferation in Murine Basal Cell Carcinomas

(2011) J. Y. Tang et al.   Cancer Prevention Research

Hedgehog-Producing Cancer Cells Respond to and Require Autocrine Hedgehog Activity

(2011) S. Singh et al.   CANCER RESEARCH

Hedgehog signaling pathway as a therapeutic target in various types of cancer

(2011) Hideya Onishi et al.   CANCER SCIENCE

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

(2011) Haiyan Tao et al.   CHEMISTRY & BIOLOGY

In vitro and in vivo characterization of a novel hedgehog signaling antagonist in human glioblastoma cell lines

(2011) Pietro Ferruzzi et al.   INTERNATIONAL JOURNAL OF CANCER

Itraconazole Side Chain Analogues: Structure–Activity Relationship Studies for Inhibition of Endothelial Cell Proliferation, Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Glycosylation, and Hedgehog Signaling

(2011) Wei Shi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting the Hedgehog Pathway: The development of Cyclopamine and the Development of Anti-Cancer Drugs Targeting the Hedgehog Pathway

(2011) A. Gould et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Effective Targeting of Hedgehog Signaling in a Medulloblastoma Model with PF-5274857, a Potent and Selective Smoothened Antagonist That Penetrates the Blood-Brain Barrier

(2011) A. Rohner et al.   MOLECULAR CANCER THERAPEUTICS

The cancer stem cell: premises, promises and challenges

(2011) Hans Clevers   NATURE MEDICINE

A Novel Synthetic Smoothened Antagonist Transiently Inhibits Pancreatic Adenocarcinoma Xenografts in a Mouse Model

(2011) Martin F. Strand et al.   PLoS One

Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened

(2011) Michael J. Munchhof et al.   ACS Medicinal Chemistry Letters

Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway

(2010) Neeraj Mahindroo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

Smoothened antagonists for hair inhibition

(2010) Jie Jack Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway

(2010) Georgette M. Castanedo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A structure-activity relationship study of small-molecule inhibitors of GLI1-mediated transcription

(2010) Marcelo Actis et al.   BIOPOLYMERS

Assessing the efficacy of the Hedgehog pathway inhibitor vitamin D3 in a murine xenograft model for pancreatic cancer

(2010) Lois W. Brüggemann et al.   CANCER BIOLOGY & THERAPY

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

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

(2010) Stefan Peukert et al.   ChemMedChem

Targeting Hedgehog -- a Cancer Stem Cell Pathway

(2010) A. A. Merchant et al.   CLINICAL CANCER RESEARCH

Study of a cyclopamine glucuronide prodrug for the selective chemotherapy of glioblastoma

(2010) Florian Hamon et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Arsenic trioxide inhibits human cancer cell growth and tumor development in mice by blocking Hedgehog/GLI pathway

(2010) Elspeth M. Beauchamp et al.   JOURNAL OF CLINICAL INVESTIGATION

A Bisindole Alkaloid with Hedgehog Signal Inhibitory Activity from the MyxomycetePerichaena chrysosperma

(2010) Akinori Shintani et al.   JOURNAL OF NATURAL PRODUCTS

Terpenoids and a Flavonoid Glycoside fromAcacia pennataLeaves as Hedgehog/GLI-Mediated Transcriptional Inhibitors

(2010) Yusnita Rifai et al.   JOURNAL OF NATURAL PRODUCTS

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

(2010) F. Manetti et al.   MOLECULAR PHARMACOLOGY

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

Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of Sonic Hedgehog

(2009) Lee F. Peng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway

(2009) Gabriella Dessole et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GDC-0449—A potent inhibitor of the hedgehog pathway

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

Converse Conformational Control of Smoothened Activity by Structurally Related Small Molecules

(2009) Hongbo Yang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure−Activity Relationships and Cancer-Cell Selective Toxicity of Novel Inhibitors of Glioma-Associated Oncogene Homologue 1 (Gli1) Mediated Transcription

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

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

A small molecule that binds Hedgehog and blocks its signaling in human cells

(2009) Benjamin Z Stanton et al.   Nature Chemical Biology

Design and Synthesis of Inhibitors of Hedgehog Signaling Based on the Alkaloid Cyclopamine

(2009) Jeffrey D. Winkler et al.   ORGANIC LETTERS

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

Mechanisms of Hedgehog pathway activation in cancer and implications for therapy

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

Hedgehog/GLI-mediated transcriptional inhibitors from Zizyphus cambodiana

(2008) Midori A. Arai et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and anticancer activity studies of cyclopamine derivatives

(2008) Jianjun Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification and structure–activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway

(2008) Stefan Peukert et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Naturally Occurring Small-Molecule Inhibitors of Hedgehog/GLI-Mediated Transcription

(2008) Takahiro Hosoya et al.   CHEMBIOCHEM

Hedgehog: functions and mechanisms

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

Semisynthetic Cyclopamine Analogues as Potent and Orally Bioavailable Hedgehog Pathway Antagonists

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

Potent Inhibitors of the Hedgehog Signaling Pathway

(2008) Shirley A. Brunton et al.   JOURNAL OF MEDICINAL CHEMISTRY

An orally bioavailable small-molecule inhibitor of Hedgehog signaling inhibits tumor initiation and metastasis in pancreatic cancer

(2008) G. Feldmann et al.   MOLECULAR CANCER THERAPEUTICS

A paracrine requirement for hedgehog signalling in cancer

(2008) Robert L. Yauch et al.   NATURE