Activation mechanism of the human Smoothened receptor. [PDF]
Biophys J, 2023 Smoothened (SMO) is a membrane protein of the Class F subfamily of G-Protein Coupled Receptors (GPCRs) and maintains homeostasis of cellular differentiation. SMO undergoes conformational change during activation, transmitting the signal across the membrane, making it amenable to bind to its intracellular signaling partner.
Bansal PD, Dutta S, Shukla D.
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Cholesterol activates the G-protein coupled receptor Smoothened to promote Hedgehog signaling
eLife, 2016 Cholesterol is necessary for the function of many G-protein coupled receptors (GPCRs). We find that cholesterol is not just necessary but also sufficient to activate signaling by the Hedgehog (Hh) pathway, a prominent cell-cell communication system in ...
Giovanni Luchetti +8 more
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Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs. [PDF]
Nat Commun, 2014 The Smoothened receptor (SMO) mediates signal transduction in the hedgehog pathway, which is implicated in normal development and carcinogenesis. SMO antagonists can suppress the growth of some tumors; however, mutations at SMO have been found to abolish their anti-tumor effects, a phenomenon known as chemoresistance.
Wang C +13 more
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A structurally guided dissection-then-evolution strategy for ligand optimization of smoothened receptor. [PDF]
Medchemcomm, 2017 We present herein a novel dissection-then-evolution strategy for ligand optimization.
Ye L +12 more
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Identification of Novel Smoothened Ligands Using Structure-Based Docking. [PDF]
PLoS ONE, 2016 The seven transmembrane protein Smoothened is required for Hedgehog signaling during embryonic development and adult tissue homeostasis. Inappropriate activation of the Hedgehog signalling pathway leads to cancers such as basal cell carcinoma and ...
Celine Lacroix +6 more
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The hedgehog receptor patched is involved in cholesterol transport. [PDF]
PLoS ONE, 2011 Sonic hedgehog (Shh) signaling plays a crucial role in growth and patterning during embryonic development, and also in stem cell maintenance and tissue regeneration in adults. Aberrant Shh pathway activation is involved in the development of many tumors,
Michel Bidet +10 more
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Solubilization, purification, and ligand binding characterization of G protein-coupled receptor SMO in native membrane bilayer using styrene maleic acid copolymer [PDF]
PeerJ, 2022 Smoothened (SMO) protein is a member of the G protein-coupled receptor (GPCR) family that is involved in the Hedgehog (Hh) signaling pathway. It is a putative target for treating various cancers, including medulloblastoma and basal cell carcinoma (BCC ...
Lina Zhu +10 more
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Residue 6.43 defines receptor function in class F GPCRs
Nature Communications, 2021 The class Frizzled of G protein-coupled receptors (GPCRs) consist of ten Frizzled (FZD1-10) subtypes and Smoothened (SMO). Here the Schulte laboratory demonstrates that FZDs differ substantially from SMO in receptor activation-associated conformational ...
Ainoleena Turku +4 more
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Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement [PDF]
Journal of Medicinal Chemistry, 2021 Class F G protein-coupled receptors are characterized by a large extracellular domain (ECD) in addition to the common transmembrane domain (TMD) with seven α-helixes. For smoothened receptor (SMO), structural studies revealed dissected ECD and TMD, and their integrated assemblies. However, distinct assemblies were reported under different circumstances.
Fei Zhao +16 more
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Role of the Drosophila non-visual ß-arrestin kurtz in hedgehog signalling. [PDF]
PLoS Genetics, 2011 The non-visual ß-arrestins are cytosolic proteins highly conserved across species that participate in a variety of signalling events, including plasma membrane receptor degradation, recycling, and signalling, and that can also act as scaffolding for ...
Cristina Molnar +5 more
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