Results 1 to 10 of about 12,144 (240)

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, Dr. Fang Zhou, Kang Ding, Dr. Dongxiang Xue, Zhihao Zhu, Cuixia Li, Fei Li, Dr. Yueming Xu, Prof. Fei Xu, Prof. Zhiping Le, Prof. Suwen Zhao, Prof. Houchao Tao   +11 more
doaj   +6 more sources

Multiple modes of cholesterol translocation in the human Smoothened receptor [PDF]

eLife
Smoothened (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, Maia Kinnebrew, Rajat Rohatgi, Diwakar Shukla   +3 more
doaj   +6 more sources

Cyclopamine modulates smoothened receptor activity in a binding position dependent manner [PDF]

Communications Biology
Cyclopamine, 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, Prateek D. Bansal, Diwakar Shukla   +2 more
doaj   +4 more sources

Structure of the human smoothened receptor bound to an antitumour agent [PDF]

Nature, 2013
The smoothened (SMO) receptor, a key signal transducer in the Hedgehog (Hh) signaling pathway is both responsible for the maintenance of normal embryonic development and implicated in carcinogenesis. The SMO receptor is classified as a class Frizzled (class F) G protein-coupled receptor (GPCR), although the canonical Hh signaling pathway involves the ...
Huixian Wu, Vsevolod Katritch, Gye Won Han   +2 more
exaly   +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, Qifeng Bai, Fang Bai, Danfeng Shi, Huanxiang Liu, Xiaojun Yao, Xiaojun Yao   +6 more
doaj   +2 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, Fei Zhao, Yiran Wu, Jun Yang, Gye Won Han, Suwen Zhao, Andrii Ishchenko, Lintao Ye, Xi Lin, Kang Ding, Venkatasubramanian Dharmarajan, Patrick R. Griffin, Cornelius Gati, Garrett Nelson, Mark S. Hunter, Michael A. Hanson, Vadim Cherezov, Raymond C. Stevens, Wenfu Tan, Houchao Tao, Fei Xu   +20 more
doaj   +2 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, Mira Hamze, Mira Hamze, Igor Medina, Igor Medina, Igor Medina, Quentin Delmotte, Quentin Delmotte, Quentin Delmotte, Christophe Porcher, Christophe Porcher, Christophe Porcher   +11 more
doaj   +2 more sources

Pharmacological targeting of smoothened receptor cysteine-rich domain by Budesonide promotes in vitro myelination [PDF]

Frontiers in Molecular Neuroscience
BackgroundThe 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, Alessandra Dominicis, Vincenzo Maria D'Amore, Tommaso Fabiano, Tommaso Fabiano, Aland Ibrahim Ahmed Al Jaf, Simone Peria, Francesco Basoli, Alberto Rainer, Alberto Rainer, Luciana Marinelli, Francesco Saverio Di Leva, Antonella Ragnini-Wilson   +12 more
doaj   +2 more sources

Sonic Hedgehog Activates Phospholipase A2 to Enhance Smoothened Ciliary Translocation

Cell Reports, 2017
The G protein-coupled receptor Smoothened (Smo) is the signal transducer of the Sonic Hedgehog (Shh) pathway. Smo signals through G protein-dependent and -independent routes, with G protein-independent canonical signaling to Gli effectors requiring Smo ...
Angela M. Arensdorf, Miriam E. Dillard, Jacob M. Menke, Matthew W. Frank, Charles O. Rock, Stacey K. Ogden   +5 more
doaj   +3 more sources

Hedgehog signalling controls sinoatrial node development and atrioventricular cushion formation

Open Biology, 2021
Smoothened is a key receptor of the hedgehog pathway, but the roles of Smoothened in cardiac development remain incompletely understood. In this study, we found that the conditional knockout of Smoothened from the mesoderm impaired the development of the
Chaohui Zhang, Yuxin Li, Jiaheng Cao, Beibei Yu, Kaiyue Zhang, Ke Li, Xinhui Xu, Zhikun Guo, Yinming Liang, Xiao Yang, Zhongzhou Yang, Yunfu Sun, Vesa Kaartinen, Keyue Ding, Jikui Wang   +14 more
doaj   +1 more source