Results 211 to 220 of about 12,161 (240)

smoothened encodes a receptor-like serpentine protein required for hedgehog signalling

Nature, 1996
Members of the Hedgehog family of secreted proteins control a number of important inductive interactions in the development of both vertebrates and Drosophila, but little is known about the ways in which their signalling activities are transduced. In Drosophila, hedgehog is one of the segment-polarity genes, mutations of which disrupt the pattern and ...
Philip William Ingham, Marcel Van den Heuvel, Ingham Philip W   +2 more
exaly   +3 more sources

Inhibition of smoothened receptor by vismodegib leads to micrognathia during embryogenesis

Differentiation, 2022
The mandible is an important part of the craniofacial skeleton. Mandibular development is complex and involves multiple signaling pathways. These signaling pathways participate in a complex regulatory mechanism to regulate mandibular growth. The function of hedgehog signaling has previously been shown to be crucial for mandibular arch development.
Yan Guo, Di Wu, QingJiang Xu, Weihui Chen   +3 more
openaire   +2 more sources

Evidence for Allosteric Interactions of Antagonist Binding to the Smoothened Receptor

The Journal of Pharmacology and Experimental Therapeutics, 2009
The Smoothened receptor (Smo) mediates hedgehog (Hh) signaling critical for development, cell growth, and migration, as well as stem cell maintenance. Aberrant Hh signaling pathway activation has been implicated in a variety of cancers, and small-molecule antagonists of Smo have entered human clinical trials for the treatment of cancer. Here, we report
Cynthia M, Rominger, Wei-Lin Tiger, Bee, Robert A, Copeland, Elizabeth A, Davenport, Aidan, Gilmartin, Richard, Gontarek, Keith R, Hornberger, Lorena A, Kallal, Zhihong, Lai, Kenneth, Lawrie, Quinn, Lu, Lynette, McMillan, Maggie, Truong, Peter J, Tummino, Brandon, Turunen, Matthew, Will, William J, Zuercher, David H, Rominger   +17 more
openaire   +2 more sources

The structure-based traceless specific fluorescence labeling of the smoothened receptor

Organic & Biomolecular Chemistry, 2019
Inspired by recent progress in structural studies of the smoothened receptor (SMO), a group of affinity probes were developed to specifically light up SMO by grafting a small fluorescent group at the specific residue K395.
Dongxiang Xue, Lintao Ye, Jun Zheng, Yiran Wu, Xianjun Zhang, Yueming Xu, Tao Li, Raymond C. Stevens, Fei Xu, Min Zhuang, Suwen Zhao, Fei Zhao, Houchao Tao   +12 more
openaire   +2 more sources

Smoothened receptor as a novel target for remyelination therapies

2021
Multiple Sclerosis (MS) is an autoimmune demyelinating disease of unknown aetiology, causing neurodegeneration in the Central Nervous System (CNS). Although the spontaneous capacity of myelin to regenerate can restore neuronal function, during MS progression, the instauration of an inflammatory microenvironment limits oligodendrocyte precursor cells ...
openaire   +1 more source

[Structure of the Smoothened receptor].

Medecine sciences : M/S, 2013
The Smoothened (Smo) receptor is a major component involved in signal transduction of the Hedgehog (Hh) morphogens both during embryogenesis and in the adult. Smo antagonists represent a promi-sing alternative for the treatment of cancers linked to abnormal Hh signalling.
Ruat, Martial, Hoch, Lucile, Faure, Hélène, Rognan, Didier   +3 more
openaire   +2 more sources

Pharmacological and structural studies on the hedgehog pathway receptor smoothened

2023
The Frizzled-class G protein-coupled receptor Smoothened (SMO) is an essential component of the Hedgehog (HH) signalling pathway, which is of paramount importance to developmental processes of bilaterians. Dysregulation of HH signalling has been implicated in multiple pathophysiological processes in adult organisms, such as cancer development.
openaire   +1 more source

Attenuation of early liver fibrosis by pharmacological inhibition of smoothened receptor signaling

Journal of Drug Targeting, 2012
Hedgehog (Hh) signaling is involved in the pathogenesis of liver fibrosis. It has been previously shown that Hh-inhibitor cyclopamine (CYA) can reduce liver fibrosis in rats. However, CYA is not stable in vivo, which limits its clinical application.
Akshay, Pratap, Saurabh, Singh, Vaibhav, Mundra, Ningning, Yang, Ravikiran, Panakanti, James D, Eason, Ram I, Mahato   +6 more
openaire   +2 more sources

Computer-aided design of arylphthalazines as potential smoothened receptor antagonists

Doklady Chemistry, 2012
The goal is to propose a model of activity-structure relations for antagonists. A comparative analysis of activity charts for molecular field topology analysis and comparative molecular similarity indices analysis demonstrates a good coherence. A virtual screening method is used for the synthesis of the new antagonists.
Radchenko, E. V., Koshelev, S. O., Tsareva, D. A., Voronkov, A. E., Palyulin, V. A., Zefirov, N. S.   +5 more
openaire   +2 more sources

Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor

Journal of Medicinal Chemistry, 2019
We unveiled an underside binding site on smoothened receptor (SMO) by a colocalization strategy using two structurally complementary photoaffinity probes derived from a known ligand Allo-1. Docking study and structural dissection identified key interactions within the site, including hydrogen bonding, π-π interactions, and hydrophobic interactions ...
Fang Zhou, Kang Ding, Yiqing Zhou, Yang Liu, Xiaoyan Liu, Fei Zhao, Yiran Wu, Xianjun Zhang, Qiwen Tan, Fei Xu, Wenfu Tan, Youli Xiao, Suwen Zhao, Houchao Tao   +13 more
openaire   +2 more sources