Multiple modes of cholesterol translocation in the human Smoothened receptor [PDF]
eLifeSmoothened (SMO), a member of the G-protein-coupled receptor superfamily, mediates Hedgehog signaling and is linked to cancer and birth defects. SMO responds to accessible cholesterol in the ciliary membrane, translocating it via a longitudinal tunnel to
Prateek D Bansal +3 more
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Cyclopamine modulates smoothened receptor activity in a binding position dependent manner [PDF]
Communications BiologyCyclopamine, a natural alkaloid, can act as an agonist when it binds to the Cysteine-Rich Domain (CRD) of Smoothened receptor and as an antagonist when it binds to the Transmembrane Domain (TMD).
Kihong Kim +2 more
doaj +5 more sources
Deciphering the Allosteric Effect of Antagonist Vismodegib on Smoothened Receptor Deactivation Using Metadynamics Simulation [PDF]
Frontiers in Chemistry, 2019 The smoothened receptor (Smo) plays a key role in Hedgehog (Hh) signaling pathway and it has been regarded as an efficacious therapeutic target for basal cell carcinoma (BCC) and medulloblastoma (MB).
Xiaoli An +6 more
doaj +6 more sources
Pharmacological targeting of smoothened receptor cysteine-rich domain by Budesonide promotes in vitro myelination [PDF]
Frontiers in Molecular NeuroscienceBackgroundThe myelin sheath ensures efficient nerve impulse transmission along the axons. Remyelination is a spontaneous process that restores axonal insulation, promoting neuroprotection and recovery after myelin damage.
Antonella Damiana Recchia +12 more
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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.
Bansal PD, Dutta S, Shukla D.
europepmc +4 more sources
Structure‐Activity Relationship Studies of Hydantoin‐Cored Ligands for Smoothened Receptor [PDF]
ChemistryOpen, 2021 An underside binding site was recently identified in the transmembrane domain of smoothened receptor (SMO). Herein, we report efforts in the exploration of new insights into the interactions between the ligand and SMO. The hydantoin core in the middle of
Dr. Yang Liu +11 more
doaj +5 more sources
Crystal structure of a multi-domain human smoothened receptor in complex with a super stabilizing ligand [PDF]
Nature Communications, 2017 Smoothened receptors (SMO) play a key role in the Hedgehog signalling pathway. Here the authors present the structure of a multi-domain human SMO with a rationally designed stabilizing ligand bound in the transmembrane domain of the receptor, and propose
Xianjun Zhang +20 more
doaj +3 more sources
Contribution of Smoothened Receptor Signaling in GABAergic Neurotransmission and Chloride Homeostasis in the Developing Rodent Brain [PDF]
Frontiers in Physiology, 2021 In the early stages of the central nervous system growth and development, γ-aminobutyric acid (GABA) plays an instructive trophic role for key events including neurogenesis, migration, synaptogenesis, and network formation.
Mira Hamze +11 more
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Smoothened receptor signaling regulates the developmental shift of GABA polarity in rat somatosensory cortex. [PDF]
J Cell Sci, 2020 Sonic hedgehog (Shh) and its patched–smoothened receptor complex control a variety of functions in the developing central nervous system, such as neural cell proliferation and differentiation.
Delmotte Q +6 more
europepmc +6 more sources
Neuroprotective Effects of a Smoothened Receptor Agonist against Early Brain Injury after Experimental Subarachnoid Hemorrhage in Rats. [PDF]
Front Cell Neurosci, 2016 The sonic hedgehog (Shh) signaling pathway plays a fundamental role in the central nervous system (CNS) development, but its effects on neural cell survival and brain repair after subarachnoid hemorrhage (SAH) has not been well-investigated.
Hu Q +11 more
europepmc +2 more sources