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Biochemical characterization of smoothened receptor antagonists by binding kinetics against drug-resistant mutant

Shimizu, Yuji ; Ishii, Tsuyoshi ; Ogawa, Kazumasa ; Sasaki, Satoshi ; Matsui, Hideki ; Nakayama, Masaharu

European Journal of Pharmacology, 05 October 2015, Vol.764, pp.220-227 [Peer Reviewed Journal]

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Identification of Novel Smoothened Ligands Using Structure-Based Docking

Lacroix, Celine ; Fish, Inbar ; Torosyan, Hayarpi ; Parathaman, Pranavan ; Irwin, John J ; Shoichet, Brian K ; Angers, Stephane

PloS one, 2016, Vol.11(8), pp.e0160365 [Peer Reviewed Journal]

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1 H nuclear magnetic resonance spectroscopy characterisation of metabolic phenotypes in the medulloblastoma of the SMO transgenic mice

Hekmatyar, S K ; Wilson, M ; Jerome, N ; Salek, R M ; Griffin, J L ; Peet, A ; Kauppinen, R A

British Journal of Cancer, 2010, Vol.103(8), p.1297-1304 [Peer Reviewed Journal]

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Activation of the Gi protein-RHOA axis by non-canonical Hedgehog signaling is independent of primary cilia

Ho Wei, Lan ; Arastoo, Mohammad ; Georgiou, Ioanna ; Manning, David R ; Riobo-Del Galdo, Natalia A

PloS one, 2018, Vol.13(8), pp.e0203170 [Peer Reviewed Journal]

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Phase I Study of LY2940680, a Smo Antagonist, in Patients with Advanced Cancer Including Treatment-Naïve and Previously Treated Basal Cell Carcinoma

Bendell, Johanna ; Andre, Valerie ; Ho, Alan ; Kudchadkar, Ragini ; Migden, Michael ; Infante, Jeffrey ; Tiu, Ramon V ; Pitou, Celine ; Tucker, Trevor ; Brail, Les ; Von Hoff, Daniel

Clinical cancer research : an official journal of the American Association for Cancer Research, 01 May 2018, Vol.24(9), pp.2082-2091 [Peer Reviewed Journal]

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Smoothened is a poor prognosis factor and a potential therapeutic target in glioma

Tu, Yiming ; Niu, Mingshan ; Xie, Peng ; Yue, Chenglong ; Liu, Ning ; Qi, Zhenglei ; Gao, Shangfeng ; Liu, Hongmei ; Shi, Qiong ; Yu, Rutong ; Liu, Xuejiao

Scientific reports, 14 February 2017, Vol.7, pp.42630 [Peer Reviewed Journal]

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MicroRNA-1271 inhibits proliferation and promotes apoptosis of multiple myeloma cells through inhibiting smoothened-mediated Hedgehog signaling pathway

Xu, Zhengwei ; Huang, Chen ; Hao, Dingjun

Oncology reports, February 2017, Vol.37(2), pp.1261-1269 [Peer Reviewed Journal]

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

Jung, Bomi ; Messias, Ana C ; Schorpp, Kenji ; Geerlof, Arie ; Schneider, Günter ; Saur, Dieter ; Hadian, Kamyar ; Sattler, Michael ; Wanker, Erich E ; Hasenöder, Stefan ; Lickert, Heiko

Scientific reports, 02 March 2016, Vol.6, pp.22540 [Peer Reviewed Journal]

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Inhibition of smoothened decreases proliferation of synoviocytes in rheumatoid arthritis

Zhu, Shang-Ling ; Huang, Jian-Lin ; Peng, Wei-Xiang ; Wu, Dan-Chun ; Luo, Min-Qi ; Li, Qiu-Xia ; Li, Zhao-Xia ; Feng, Xiao-Xue ; Liu, Fang ; Wang, Ming-Xia ; Chen, Wei-Qian ; Olsen, Nancy ; Zheng, Song Guo

Cellular & molecular immunology, February 2017, Vol.14(2), pp.214-222 [Peer Reviewed Journal]

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Targeting Smoothened Sensitizes Gastric Cancer to Chemotherapy in Experimental Models

Ma, Huifa ; Tian, Yongsheng ; Yu, Xiangyang

Medical science monitor : international medical journal of experimental and clinical research, 28 March 2017, Vol.23, pp.1493-1500 [Peer Reviewed Journal]

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Characterization of Kinetic Binding Properties of Unlabeled Ligands via a Preincubation Endpoint Binding Approach

Shimizu, Yuji ; Ogawa, Kazumasa ; Nakayama, Masaharu

Journal of Biomolecular Screening, August 2016, Vol.21(7), pp.729-737 [Peer Reviewed Journal]

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

Tu, Jing ; Li, Jiao Jiao ; Song, Li Ting ; Zhai, Hong Lin ; Wang, Juan ; Zhang, Xiao Yun

Pharmacological Research, March 2018, Vol.129, pp.491-499 [Peer Reviewed Journal]

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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

Bai, Qifeng ; Shen, Yulin ; Jin, Nengzhi ; Liu, Huanxiang ; Yao, Xiaojun

BBA - General Subjects, July 2014, Vol.1840(7), pp.2128-2138 [Peer Reviewed Journal]

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

Zhang, Xianjun ; Zhao, Fei ; Wu, Yiran ; Yang, Jun ; Han, Gye Won ; Zhao, Suwen ; Ishchenko, Andrii ; Ye, Lintao ; Lin, Xi ; Ding, Kang ; Dharmarajan, Venkatasubramanian ; Griffin, Patrick R ; Gati, Cornelius ; Nelson, Garrett ; Hunter, Mark S ; Hanson, Michael A ; Cherezov, Vadim ; Stevens, Raymond C ; Tan, Wenfu ; Tao, Houchao ; Xu, Fei

Nature communications, 17 May 2017, Vol.8, pp.15383 [Peer Reviewed Journal]

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Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays

Lu, Wenfeng ; Zhang, Dihua ; Ma, Haikuo ; Tian, Sheng ; Zheng, Jiyue ; Wang, Qin ; Luo, Lusong ; Zhang, Xiaohu

European Journal of Medicinal Chemistry, 15 July 2018, Vol.155, pp.34-48 [Peer Reviewed Journal]

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16
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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

Liu, Gang ; Xue, Ding ; Yang, Jun ; Wang, Juan ; Liu, Xiaohua ; Huang, Wenjing ; Li, Jie ; Long, Ya-Qiu ; Tan, Wenfu ; Zhang, Ao

Journal of medicinal chemistry, 22 December 2016, Vol.59(24), pp.11050-11068 [Peer Reviewed Journal]

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17
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Arl13b Promotes Gastric Tumorigenesis by Regulating Smo Trafficking and Activation of the Hedgehog Signaling Pathway

Shao, Jia ; Xu, Linlin ; Chen, Limin ; Lu, Quqin ; Xie, Xinsheng ; Shi, Wei ; Xiong, Huanting ; Shi, Chao ; Huang, Xuan ; Mei, Jinhong ; Rao, Hai ; Lu, Hua ; Lu, Nonghua ; Luo, Shiwen

Cancer research, 01 August 2017, Vol.77(15), pp.4000-4013 [Peer Reviewed Journal]

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18
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Gastric cancer and Hedgehog signaling pathway: emerging new paradigms

Akyala, Adamu Ishaku ; Peppelenbosch, Maikel P

Genes & cancer, January 2018, Vol.9(1-2), pp.1-10 [Peer Reviewed Journal]

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Pancreatic islet-autonomous insulin and smoothened-mediated signalling modulate identity changes of glucagon α-cells

Cigliola, Valentina ; Ghila, Luiza ; Thorel, Fabrizio ; Van Gurp, Léon ; Baronnier, Delphine ; Oropeza, Daniel ; Gupta, Simone ; Miyatsuka, Takeshi ; Kaneto, Hideaki ; Magnuson, Mark A ; Osipovich, Anna B ; Sander, Maike ; Wright, Christopher E V ; Thomas, Melissa K ; Furuyama, Kenichiro ; Chera, Simona ; Herrera, Pedro L

Nature cell biology, November 2018, Vol.20(11), pp.1267-1277 [Peer Reviewed Journal]

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20
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Generation of a SMO homozygous knockout human embryonic stem cell line WAe001-A-16 by CRISPR/Cas9 editing

Wu, Feima ; Gao, Ge ; Pan, Tingcai ; Yang, Zhen ; Xu, Guosheng ; Abbas, Nasir ; Liu, Yanli ; Chen, Yan ; Tan, Shenglin ; You, Kai ; Ke, Xinrong ; Zhuang, Yuanqi ; Lin, Xianhua ; Yang, Fan ; Li, Yin-Xiong

Stem cell research, March 2018, Vol.27, pp.5-9 [Peer Reviewed Journal]

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21
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Segmental basal cell naevus syndrome caused by an activating mutation in smoothened

Khamaysi, Z ; Bochner, R ; Indelman, M ; Magal, L ; Avitan-Hersh, E ; Sarig, O ; Sprecher, E ; Bergman, R

The British journal of dermatology, July 2016, Vol.175(1), pp.178-81 [Peer Reviewed Journal]

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22
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KIF13B establishes a CAV1-enriched microdomain at the ciliary transition zone to promote Sonic hedgehog signalling

Schou, Kenneth B ; Mogensen, Johanne B ; Morthorst, Stine K ; Nielsen, Brian S ; Aleliunaite, Aiste ; Serra-Marques, Andrea ; Fürstenberg, Nicoline ; Saunier, Sophie ; Bizet, Albane A ; Veland, Iben R ; Akhmanova, Anna ; Christensen, Søren T ; Pedersen, Lotte B

Nature communications, 30 January 2017, Vol.8, pp.14177 [Peer Reviewed Journal]

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23
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Hypomorphic Smo mutant with inefficient ciliary enrichment disrupts the highest level of vertebrate Hedgehog response

Gigante, Eduardo D ; Long, Alyssa Bushey ; Ben-Ami, Johanna ; Caspary, Tamara

Developmental biology, 15 May 2018, Vol.437(2), pp.152-162 [Peer Reviewed Journal]

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24
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Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model

Lauressergues, Emilie ; Heusler, Peter ; Lestienne, Fabrice ; Troulier, David ; Rauly‐Lestienne, Isabelle ; Tourette, Amélie ; Ailhaud, Marie‐Christine ; Cathala, Claudie ; Tardif, Stéphanie ; Denais‐Laliève, Delphine ; Calmettes, Marie‐Thérèse ; Degryse, Anne‐Dominique ; Dumoulin, Antoine ; De Vries, Luc ; Cussac, Didier

Pharmacology Research & Perspectives, April 2016, Vol.4(2), pp.n/a-n/a [Peer Reviewed Journal]

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25
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Smoothened signaling in the mouse osteoblastoid lineage is required for efficient B lymphopoiesis

Lu, Wenyan ; Dordai, Dominic ; Huso, David ; Desiderio, Stephen

Blood, 18 January 2018, Vol.131(3), pp.323-327 [Peer Reviewed Journal]

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26
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Overcoming the resistance mechanisms of Smoothened inhibitors

Dong, Xiaochun ; Wang, Chenglin ; Chen, Zhongjian ; Zhao, Weili

Drug discovery today, March 2018, Vol.23(3), pp.704-710 [Peer Reviewed Journal]

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27
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Cell Cycle-Related Kinase (CCRK) regulates ciliogenesis and Hedgehog signaling in mice

Snouffer, Ashley ; Brown, Desmond ; Lee, Hankyu ; Walsh, Jonathon ; Lupu, Floria ; Norman, Ryan ; Lechtreck, Karl ; Ko, Hyuk Wan ; Eggenschwiler, Jonathan

PLoS genetics, August 2017, Vol.13(8), pp.e1006912 [Peer Reviewed Journal]

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28
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LncRNA-MEG3 inhibits activation of hepatic stellate cells through SMO protein and miR-212

Yu, Fujun ; Geng, Wujun ; Dong, Peihong ; Huang, Zhiming ; Zheng, Jianjian

Cell death & disease, 03 October 2018, Vol.9(10), pp.1014 [Peer Reviewed Journal]

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29
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Selective vulnerability of the primitive meningeal layer to prenatal Smo activation for skull base meningothelial meningioma formation

Boetto, Julien ; Apra, Caroline ; Bielle, Franck ; Peyre, Matthieu ; Kalamarides, Michel

Oncogene, September 2018, Vol.37(36), pp.4955-4963 [Peer Reviewed Journal]

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30
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A Recurrent Mosaic Mutation in SMO, Encoding the Hedgehog Signal Transducer Smoothened, Is the Major Cause of Curry-Jones Syndrome

Twigg, Stephen R F ; Hufnagel, Robert B ; Miller, Kerry A ; Zhou, Yan ; Mcgowan, Simon J ; Taylor, John ; Craft, Jude ; Taylor, Jenny C ; Santoro, Stephanie L ; Huang, Taosheng ; Hopkin, Robert J ; Brady, Angela F ; Clayton-Smith, Jill ; Clericuzio, Carol L ; Grange, Dorothy K ; Groesser, Leopold ; Hafner, Christian ; Horn, Denise ; Temple, I Karen ; Dobyns, William B ; Curry, Cynthia J ; Jones, Marilyn C ; Wilkie, Andrew O M

American journal of human genetics, 02 June 2016, Vol.98(6), pp.1256-1265 [Peer Reviewed Journal]

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31
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SUMO regulates the activity of Smoothened and Costal-2 in Drosophila Hedgehog signaling

Zhang, Jie ; Liu, Yajuan ; Jiang, Kai ; Jia, Jianhang

Scientific reports, 14 February 2017, Vol.7, pp.42749 [Peer Reviewed Journal]

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32
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Effect of the sonic hedgehog receptor smoothened on the survival and function of dopaminergic neurons

Zhou, Xiaofei ; Pace, Jonathan ; Filichia, Emily ; Lv, Tao ; Davis, Brandon ; Hoffer, Barry ; Selman, Warren ; Luo, Yu

Experimental neurology, September 2016, Vol.283(Pt A), pp.235-45 [Peer Reviewed Journal]

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33
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Endogenous B-ring oxysterols inhibit the Hedgehog component Smoothened in a manner distinct from cyclopamine or side-chain oxysterols

Sever, Navdar ; Mann, Randall K ; Xu, Libin ; Snell, William J ; Hernandez-Lara, Carmen I ; Porter, Ned A ; Beachy, Philip A

Proceedings of the National Academy of Sciences of the United States of America, 24 May 2016, Vol.113(21) [Peer Reviewed Journal]

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34
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Meta-analysis of Icelandic and UK data sets identifies missense variants in SMO, IL11, COL11A1 and 13 more new loci associated with osteoarthritis

Styrkarsdottir, Unnur ; Lund, Sigrun H ; Thorleifsson, Gudmar ; Zink, Florian ; Stefansson, Olafur A ; Sigurdsson, Jon K ; Juliusson, Kristinn ; Bjarnadottir, Kristbjörg ; Sigurbjornsdottir, Sara ; Jonsson, Stefan ; Norland, Kristjan ; Stefansdottir, Lilja ; Sigurdsson, Asgeir ; Sveinbjornsson, Gardar ; Oddsson, Asmundur ; Bjornsdottir, Gyda ; Gudmundsson, Reynir L ; Halldorsson, Gisli H ; Rafnar, Thorunn ; Jonsdottir, Ingileif ; Steingrimsson, Eirikur ; Norddahl, Gudmundur L ; Masson, Gisli ; Sulem, Patrick ; Jonsson, Helgi ; Ingvarsson, Thorvaldur ; Gudbjartsson, Daniel F ; Thorsteinsdottir, Unnur ; Stefansson, Kari

Nature genetics, December 2018, Vol.50(12), pp.1681-1687 [Peer Reviewed Journal]

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35
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A Transposon Screen Identifies Loss of Primary Cilia as a Mechanism of Resistance to SMO Inhibitors

Zhao, Xuesong ; Pak, Ekaterina ; Ornell, Kimberly J ; Pazyra-Murphy, Maria F ; Mackenzie, Ethan L ; Chadwick, Emily J ; Ponomaryov, Tatyana ; Kelleher, Joseph F ; Segal, Rosalind A

Cancer discovery, December 2017, Vol.7(12), pp.1436-1449

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36
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Rapid, direct activity assays for Smoothened reveal Hedgehog pathway regulation by membrane cholesterol and extracellular sodium

Myers, Benjamin R ; Neahring, Lila ; Zhang, Yunxiao ; Roberts, Kelsey J ; Beachy, Philip A

Proceedings of the National Academy of Sciences of the United States of America, 26 December 2017, Vol.114(52), pp.E11141-E11150 [Peer Reviewed Journal]

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Genetic ablation of Smoothened in pancreatic fibroblasts increases acinar-ductal metaplasia

Liu, Xin ; Pitarresi, Jason R ; Cuitiño, Maria C ; Kladney, Raleigh D ; Woelke, Sarah A ; Sizemore, Gina M ; Nayak, Sunayana G ; Egriboz, Onur ; Schweickert, Patrick G ; Yu, Lianbo ; Trela, Stefan ; Schilling, Daniel J ; Halloran, Shannon K ; Li, Maokun ; Dutta, Shourik ; Fernandez, Soledad A ; Rosol, Thomas J ; Lesinski, Gregory B ; Shakya, Reena ; Ludwig, Thomas ; Konieczny, Stephen F ; Leone, Gustavo ; Wu, Jinghai ; Ostrowski, Michael C

Genes & development, 01 September 2016, Vol.30(17), pp.1943-55 [Peer Reviewed Journal]

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