Results 1 to 10 of about 12,161 (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

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   +4 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   +4 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

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.
europepmc   +3 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

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 ...
Wang C, Wu H, Katritch V, Han GW, Huang XP, Liu W, Siu FY, Roth BL, Cherezov V, Stevens RC.   +9 more
europepmc   +4 more sources

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, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC.   +13 more
europepmc   +4 more sources

The Development of a High-Content Screening Binding Assay for the Smoothened Receptor [PDF]

Journal of Biomolecular Screening, 2012
In this study, the development of an image-based high-content screening (HCS) binding assay for the seven-transmembrane (7TM) receptor Smoothened (Smo) is described. Using BacMam-based gene delivery of Smo, BODIPY-cyclopamine as a fluorescent probe, and a confocal imaging system, a robust 384-well assay that could be used for high-throughput compound ...
Keith Hornberger, William Zuercher, Robert S Ames   +2 more
exaly   +3 more sources