Purmorphamine activates the Hedgehog pathway by targeting Smoothened.

PubWeight™: 3.49‹?› | Rank: Top 1%

🔗 View Article (PMID 16408088)

Published in Nat Chem Biol on November 20, 2005

Authors

Surajit Sinha1, James K Chen

Author Affiliations

1: Department of Molecular Pharmacology, Stanford University School of Medicine, Stanford, California 94305, USA.

Articles citing this

(truncated to the top 100)

Directed differentiation of ventral spinal progenitors and motor neurons from human embryonic stem cells by small molecules. Stem Cells (2008) 2.54

A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol (2009) 2.21

Lateral transport of Smoothened from the plasma membrane to the membrane of the cilium. J Cell Biol (2009) 2.10

Accelerated high-yield generation of limb-innervating motor neurons from human stem cells. J Neurosci (2013) 2.08

Selective translocation of intracellular Smoothened to the primary cilium in response to Hedgehog pathway modulation. Proc Natl Acad Sci U S A (2009) 2.04

Human oligodendrocytes from embryonic stem cells: conserved SHH signaling networks and divergent FGF effects. Development (2009) 1.90

Minimization of exogenous signals in ES cell culture induces rostral hypothalamic differentiation. Proc Natl Acad Sci U S A (2008) 1.87

Activation of heterotrimeric G proteins by Smoothened. Proc Natl Acad Sci U S A (2006) 1.84

The Hedgehog signalling pathway regulates autophagy. Nat Commun (2012) 1.80

Disruption at the PTCHD1 Locus on Xp22.11 in Autism spectrum disorder and intellectual disability. Sci Transl Med (2010) 1.75

Oxysterols are allosteric activators of the oncoprotein Smoothened. Nat Chem Biol (2012) 1.72

Periodic stripe formation by a Turing mechanism operating at growth zones in the mammalian palate. Nat Genet (2012) 1.60

Investigating synapse formation and function using human pluripotent stem cell-derived neurons. Proc Natl Acad Sci U S A (2011) 1.52

Review of Signaling Pathways Governing MSC Osteogenic and Adipogenic Differentiation. Scientifica (Cairo) (2013) 1.51

Notch activity modulates the responsiveness of neural progenitors to sonic hedgehog signaling. Dev Cell (2015) 1.50

Smoothened adopts multiple active and inactive conformations capable of trafficking to the primary cilium. PLoS One (2009) 1.42

Intra-endodermal interactions are required for pancreatic beta cell induction. Dev Cell (2008) 1.41

Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg (2017) 1.40

The extracellular domain of Smoothened regulates ciliary localization and is required for high-level Hh signaling. Curr Biol (2009) 1.39

Evc2 is a positive modulator of Hedgehog signalling that interacts with Evc at the cilia membrane and is also found in the nucleus. BMC Biol (2011) 1.21

Hedgehog and Bmp polarize hematopoietic stem cell emergence in the zebrafish dorsal aorta. Dev Cell (2009) 1.20

Oxysterol binding to the extracellular domain of Smoothened in Hedgehog signaling. Nat Chem Biol (2013) 1.18

Glucocorticoid-related molecular signaling pathways regulating hippocampal neurogenesis. Neuropsychopharmacology (2012) 1.16

Atf4 regulates chondrocyte proliferation and differentiation during endochondral ossification by activating Ihh transcription. Development (2009) 1.15

Hedgehog-Gli signaling pathway inhibitors as anticancer agents. J Med Chem (2009) 1.14

A novel murine allele of Intraflagellar Transport Protein 172 causes a syndrome including VACTERL-like features with hydrocephalus. Hum Mol Genet (2011) 1.13

Targeting cancer stem cells: a new therapy to cure cancer patients. Am J Cancer Res (2012) 1.11

Hedgehog signaling induces arterial endothelial cell formation by repressing venous cell fate. Dev Biol (2010) 1.07

Proteomic assessment of a cell model of spinal muscular atrophy. BMC Neurosci (2011) 1.05

The hedgehog processing pathway is required for NSCLC growth and survival. Oncogene (2012) 1.05

Hedgehog-stimulated chemotaxis is mediated by smoothened located outside the primary cilium. Sci Signal (2012) 1.04

Cooperative activity of noggin and gremlin 1 in axial skeleton development. Development (2011) 1.03

Direct conversion of human fibroblasts to induced serotonergic neurons. Mol Psychiatry (2015) 1.01

Efficient generation of NKX6-1+ pancreatic progenitors from multiple human pluripotent stem cell lines. Stem Cell Reports (2015) 1.01

High yields of oligodendrocyte lineage cells from human embryonic stem cells at physiological oxygen tensions for evaluation of translational biology. Stem Cell Reports (2013) 0.99

Polydactyly in mice lacking HDAC9/HDRP. Exp Biol Med (Maywood) (2008) 0.99

Glucocorticoid compounds modify smoothened localization and hedgehog pathway activity. Chem Biol (2012) 0.98

Syntheses of aminoalcohol-derived macrocycles leading to a small-molecule binder to and inhibitor of Sonic Hedgehog. Bioorg Med Chem Lett (2009) 0.97

Drugging the cancer stem cell compartment: lessons learned from the hedgehog and Wnt signal transduction pathways. Annu Rev Pharmacol Toxicol (2011) 0.97

Identification of select glucocorticoids as Smoothened agonists: potential utility for regenerative medicine. Proc Natl Acad Sci U S A (2010) 0.97

Myeloma plasma cells alter the bone marrow microenvironment by stimulating the proliferation of mesenchymal stromal cells. Haematologica (2013) 0.97

Regeneration and repair of the exocrine pancreas. Annu Rev Physiol (2014) 0.94

A human Dravet syndrome model from patient induced pluripotent stem cells. Mol Brain (2013) 0.94

Selective inhibitory effect of HPMA copolymer-cyclopamine conjugate on prostate cancer stem cells. Biomaterials (2011) 0.93

Negative regulation of Hedgehog signaling by liver X receptors. Mol Endocrinol (2009) 0.93

Generation of neuropeptidergic hypothalamic neurons from human pluripotent stem cells. Development (2015) 0.93

Assessment of the stromal contribution to Sonic Hedgehog-dependent pancreatic adenocarcinoma. Mol Oncol (2013) 0.92

Developmental expression of Smoc1 and Smoc2 suggests potential roles in fetal gonad and reproductive tract differentiation. Dev Dyn (2009) 0.91

Gli1 maintains cell survival by up-regulating IGFBP6 and Bcl-2 through promoter regions in parallel manner in pancreatic cancer cells. J Carcinog (2009) 0.91

Differential BMP signaling controls formation and differentiation of multipotent preplacodal ectoderm progenitors from human embryonic stem cells. Dev Biol (2013) 0.91

The role of small molecules in musculoskeletal regeneration. Regen Med (2012) 0.90

Pituitary adenylyl cyclase activating polypeptide inhibits gli1 gene expression and proliferation in primary medulloblastoma derived tumorsphere cultures. BMC Cancer (2010) 0.90

Sonic hedgehog regulates presynaptic terminal size, ultrastructure and function in hippocampal neurons. J Cell Sci (2012) 0.89

Canonical and non-canonical Hedgehog signalling and the control of metabolism. Semin Cell Dev Biol (2014) 0.89

A Smoothened receptor agonist is neuroprotective and promotes regeneration after ischemic brain injury. Cell Death Dis (2014) 0.89

Controlling destiny through chemistry: small-molecule regulators of cell fate. ACS Chem Biol (2010) 0.88

Expression of early developmental markers predicts the efficiency of embryonic stem cell differentiation into midbrain dopaminergic neurons. Stem Cells Dev (2012) 0.88

Hedgehog signaling via a calcitonin receptor-like receptor can induce arterial differentiation independently of VEGF signaling in zebrafish. Blood (2012) 0.88

Ptch1 and Gli regulate Shh signalling dynamics via multiple mechanisms. Nat Commun (2015) 0.87

Efficient differentiation of mouse embryonic stem cells into motor neurons. J Vis Exp (2012) 0.87

Transgenic enrichment of mouse embryonic stem cell-derived progenitor motor neurons. Stem Cell Res (2011) 0.86

A novel KRAB domain-containing zinc finger transcription factor ZNF431 directly represses Patched1 transcription. J Biol Chem (2010) 0.85

Potential for pharmacological manipulation of human embryonic stem cells. Br J Pharmacol (2013) 0.85

Cellular Cholesterol Directly Activates Smoothened in Hedgehog Signaling. Cell (2016) 0.85

Generation and characterization of spiking and nonspiking oligodendroglial progenitor cells from embryonic stem cells. Stem Cells (2013) 0.85

Stem cells from umbilical cord Wharton's jelly from preterm birth have neuroglial differentiation potential. Reprod Sci (2013) 0.84

Chemical technologies for probing embryonic development. Chem Soc Rev (2008) 0.84

Indian Hedgehog signalling triggers Nkx3.2 protein degradation during chondrocyte maturation. Biochem J (2012) 0.83

Hedgehog signaling activates a positive feedback mechanism involving insulin-like growth factors to induce osteoblast differentiation. Proc Natl Acad Sci U S A (2015) 0.83

An in vivo chemical genetic screen identifies phosphodiesterase 4 as a pharmacological target for hedgehog signaling inhibition. Cell Rep (2015) 0.82

Hedgehog activity controls opening of the primary mouth. Dev Biol (2014) 0.82

The potential of induced pluripotent stem cells as a translational model for neurotoxicological risk. Neurotoxicology (2012) 0.82

Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies. ACS Med Chem Lett (2012) 0.81

Tumor shrinkage by cyclopamine tartrate through inhibiting hedgehog signaling. Chin J Cancer (2011) 0.81

Regulation of the bone-restricted IFITM-like (Bril) gene transcription by Sp and Gli family members and CpG methylation. J Biol Chem (2013) 0.81

MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB J (2015) 0.80

Antagonistic interactions of hedgehog, Bmp and retinoic acid signals control zebrafish endocrine pancreas development. Development (2011) 0.80

Controlling the Regional Identity of hPSC-Derived Neurons to Uncover Neuronal Subtype Specificity of Neurological Disease Phenotypes. Stem Cell Reports (2015) 0.79

Yeast-based assay identifies novel Shh/Gli target genes in vertebrate development. BMC Genomics (2012) 0.79

Aberrant activation of hedgehog signaling promotes cell proliferation via the transcriptional activation of forkhead Box M1 in colorectal cancer cells. J Exp Clin Cancer Res (2017) 0.78

Discovery of small-molecule modulators of the Sonic Hedgehog pathway. J Am Chem Soc (2013) 0.78

Sonic Hedgehog-activated engineered blood vessels enhance bone tissue formation. Proc Natl Acad Sci U S A (2012) 0.78

Gi proteins mediate activation of the canonical hedgehog pathway in the myocardium. Am J Physiol Heart Circ Physiol (2014) 0.78

Drugging Hedgehog: signaling the pathway to translation. BMC Biol (2013) 0.78

Manipulating gene expression and signaling activity in cultured mouse limb bud cells. Dev Dyn (2014) 0.77

SOX18 Is a Novel Target Gene of Hedgehog Signaling in Cervical Carcinoma Cell Lines. PLoS One (2015) 0.77

The formation of endoderm-derived taste sensory organs requires a Pax9-dependent expansion of embryonic taste bud progenitor cells. PLoS Genet (2014) 0.77

Functional differentiation of midbrain neurons from human cord blood-derived induced pluripotent stem cells. Stem Cell Res Ther (2014) 0.77

Regulation of hedgehog signaling by Myc-interacting zinc finger protein 1, Miz1. PLoS One (2013) 0.77

Ubr3, a Novel Modulator of Hh Signaling Affects the Degradation of Costal-2 and Kif7 through Poly-ubiquitination. PLoS Genet (2016) 0.76

Induction of Human iPSC-Derived Cardiomyocyte Proliferation Revealed by Combinatorial Screening in High Density Microbioreactor Arrays. Sci Rep (2016) 0.75

C-O bond Formation in a Microfluidic Reactor: High Yield SNAr Substitution of Heteroaryl Chlorides. Tetrahedron Lett (2016) 0.75

Nek2A/SuFu feedback loop regulates Gli-mediated Hedgehog signaling pathway. Int J Oncol (2016) 0.75

Gelatin device for the delivery of growth factors involved in endochondral ossification. PLoS One (2017) 0.75

Agonizing hedgehog. Nat Chem Biol (2006) 0.75

Promotion of Cancer Cell Proliferation by Cleaved and Secreted Luminal Domains of ER Stress Transducer BBF2H7. PLoS One (2015) 0.75

A novel function of the human oncogene Stil: Regulation of PC12 cell toxic susceptibility through the Shh pathway. Sci Rep (2015) 0.75

Targeting human respiratory syncytial virus transcription anti-termination factor M2-1 to inhibit in vivo viral replication. Sci Rep (2016) 0.75

Development-on-chip: in vitro neural tube patterning with a microfluidic device. Development (2016) 0.75

Neuroprotective Effects of a Smoothened Receptor Agonist against Early Brain Injury after Experimental Subarachnoid Hemorrhage in Rats. Front Cell Neurosci (2017) 0.75

Articles by these authors

Medulloblastoma growth inhibition by hedgehog pathway blockade. Science (2002) 6.53

Small-molecule inhibitors reveal multiple strategies for Hedgehog pathway blockade. Proc Natl Acad Sci U S A (2009) 2.41

A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol (2009) 2.21

Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2. Science (2004) 2.19

Small-molecule inhibitors of the AAA+ ATPase motor cytoplasmic dynein. Nature (2012) 2.16

The BAH domain of ORC1 links H4K20me2 to DNA replication licensing and Meier-Gorlin syndrome. Nature (2012) 2.07

Light-controlled gene silencing in zebrafish embryos. Nat Chem Biol (2007) 2.02

Small-molecule regulation of zebrafish gene expression. Nat Chem Biol (2007) 2.00

A crucial requirement for Hedgehog signaling in small cell lung cancer. Nat Med (2011) 1.97

Smoothened signal transduction is promoted by G protein-coupled receptor kinase 2. Mol Cell Biol (2006) 1.38

A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. Sci Transl Med (2011) 1.35

Centrosome repositioning in T cells is biphasic and driven by microtubule end-on capture-shrinkage. J Cell Biol (2013) 1.26

Versatile synthesis and rational design of caged morpholinos. J Am Chem Soc (2009) 1.23

The decoupling of Smoothened from Galphai proteins has little effect on Gli3 protein processing and Hedgehog-regulated chick neural tube patterning. Dev Biol (2008) 1.13

Diacylglycerol promotes centrosome polarization in T cells via reciprocal localization of dynein and myosin II. Proc Natl Acad Sci U S A (2013) 1.12

Neuropilins are positive regulators of Hedgehog signal transduction. Genes Dev (2011) 1.07

Spatiotemporal resolution of the Ntla transcriptome in axial mesoderm development. Nat Chem Biol (2012) 1.01

Cyclic caged morpholinos: conformationally gated probes of embryonic gene function. Angew Chem Int Ed Engl (2012) 0.93

Post-transcriptional mechanisms contribute to Etv2 repression during vascular development. Dev Biol (2013) 0.92

Converse conformational control of smoothened activity by structurally related small molecules. J Biol Chem (2009) 0.90

Controlling destiny through chemistry: small-molecule regulators of cell fate. ACS Chem Biol (2010) 0.88

Sequential gene silencing using wavelength-selective caged morpholino oligonucleotides. Angew Chem Int Ed Engl (2014) 0.88

General method for regulating protein stability with light. ACS Chem Biol (2013) 0.88

The imidazopyridine derivative JK184 reveals dual roles for microtubules in Hedgehog signaling. Angew Chem Int Ed Engl (2009) 0.86

Germ cell migration in zebrafish is cyclopamine-sensitive but Smoothened-independent. Dev Biol (2009) 0.86

Roles of Hedgehog pathway components and retinoic acid signalling in specifying zebrafish ventral spinal cord neurons. Development (2011) 0.84

Fish 'n clicks. Nat Chem Biol (2008) 0.84

Synthetic strategies for studying embryonic development. Chem Biol (2010) 0.84

Oligonucleotide-based tools for studying zebrafish development. Zebrafish (2010) 0.84

Chemical technologies for probing embryonic development. Chem Soc Rev (2008) 0.84

Gene regulation technologies in zebrafish. Mol Biosyst (2008) 0.82

Lineage labeling of zebrafish cells with laser uncagable fluorescein dextran. J Vis Exp (2011) 0.80

Chemical 'Jekyll and Hyde's: small-molecule inhibitors of developmental signaling pathways. Chem Soc Rev (2011) 0.80

Hedgehog and retinoic acid signaling cooperate to promote motoneurogenesis in zebrafish. Development (2011) 0.79

Spatiotemporal control of embryonic gene expression using caged morpholinos. Methods Cell Biol (2011) 0.79

Functional inhibition of UQCRB suppresses angiogenesis in zebrafish. Biochem Biophys Res Commun (2013) 0.77

Cytoplasmic Dynein Antagonists with Improved Potency and Isoform Selectivity. ACS Chem Biol (2015) 0.77

Nitroreductase-activatable morpholino oligonucleotides for in vivo gene silencing. ACS Chem Biol (2014) 0.75

Emerging technologies in molecular imaging: new windows into biology. Curr Opin Chem Biol (2013) 0.75