SANT-1
SANT-1 structure
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Common Name | SANT-1 | ||
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| CAS Number | 304909-07-7 | Molecular Weight | 373.49 | |
| Density | 1.13g/cm3 | Boiling Point | 547.4ºC at 760mmHg | |
| Molecular Formula | C23H27N5 | Melting Point | 104-106ºC | |
| MSDS | Chinese USA | Flash Point | 284.8ºC | |
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Smoothened adopts multiple active and inactive conformations capable of trafficking to the primary cilium.
PLoS ONE 4(4) , e5182, (2009) Activation of Hedgehog (Hh) signaling requires the transmembrane protein Smoothened (Smo), a member of the G-protein coupled receptor superfamily. In mammals, Smo translocates to the primary cilium upon binding of Hh ligands to their receptor, Patched (Ptch1)... |
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MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes.
Arthritis Rheumatology 67(2) , 423-34, (2015) Hedgehog (HH) signaling has recently been associated with cartilage degradation in osteoarthritis (OA). Because interleukin-1β (IL-1β) has been implicated as a principal instigator of OA, we sought to determine whether IL-1β induces the expression of sonic HH... |
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MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor.
FASEB J. 29 , 1817-29, (2015) The Smoothened (Smo) receptor, a member of class F G protein-coupled receptors, is the main transducer of the Hedgehog (Hh) signaling pathway implicated in a wide range of developmental and adult processes. Smo is the target of anticancer drugs that bind to a... |
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Ciliary IFT80 balances canonical versus non-canonical hedgehog signalling for osteoblast differentiation.
Nat. Commun. 7 , 11024, (2016) Intraflagellar transport proteins (IFT) are required for hedgehog (Hh) signalling transduction that is essential for bone development, however, how IFT proteins regulate Hh signalling in osteoblasts (OBs) remains unclear. Here we show that deletion of ciliary... |
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Histone deacetylase 6 represents a novel drug target in the oncogenic Hedgehog signaling pathway.
Mol. Cancer Ther. 14 , 727-39, (2015) Uncontrolled Hedgehog (Hh) signaling is the cause of several malignancies, including the pediatric cancer medulloblastoma, a neuroectodermal tumor affecting the cerebellum. Despite the development of potent Hh pathway antagonists, medulloblastoma drug resista... |
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Hedgehog associated to microparticles inhibits adipocyte differentiation via a non-canonical pathway.
Sci. Rep. 6 , 23479, (2016) Hedgehog (Hh) is a critical regulator of adipogenesis. Extracellular vesicles are natural Hh carriers, as illustrated by activated/apoptotic lymphocytes specifically shedding microparticles (MP) bearing the morphogen (MP(Hh+)). We show that MP(Hh+) inhibit ad... |
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Guggulsterone sensitizes glioblastoma cells to Sonic hedgehog inhibitor SANT-1 induced apoptosis in a Ras/NFκB dependent manner.
Cancer Lett. 336(2) , 347-58, (2013) Since Shh pathway effector, Gli1, is overexpressed in gliomas, we investigated the effect of novel Shh inhibitor SANT-1 on glioma cell viability. Though SANT-1 failed to induce apoptosis, it reduced proliferation of glioma stem-like cells. Apart from canonica... |
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Sonic hedgehog signaling pathway is activated in ALK-positive anaplastic large cell lymphoma.
Cancer Res. 69(6) , 2550-8, (2009) Deregulation of the sonic hedgehog (SHH) signaling pathway has been implicated in several cancers but has not been explored in T-cell lymphomas. Here, we report that the SHH/GLI1 signaling pathway is activated in anaplastic lymphoma kinase (ALK)-positive anap... |
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Inhibition of GLI, but not Smoothened, induces apoptosis in chronic lymphocytic leukemia cells.
Oncogene Jul 5 , (2010) The Hedgehog (Hh) pathway regulates cell proliferation and survival and contributes to tumorigenesis. We investigated the expression and function of this pathway in B-cell chronic lymphocytic leukemia (CLL) cells and in healthy B lymphocytes. Profiling of cog... |
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Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling.
Elife 2 , e01340, (2013) The Hedgehog (Hh) signal is transduced across the membrane by the heptahelical protein Smoothened (Smo), a developmental regulator, oncoprotein and drug target in oncology. We present the 2.3 Å crystal structure of the extracellular cysteine rich domain (CRD)... |