Results 261 to 270 of about 2,656,785 (305)
AOP 460: Antagonism of Smoothened receptor leading to orofacial clefting.
ALTEXSonic hedgehog (SHH) is a major intercellular signaling pathway involved in the orchestration of embryogenesis, including orofacial morphogenesis. The SHH pathway is sensitive to disruption, including both genetic predisposition and chemical-induced ...
Jacob I. Reynolds, Brian P. Johnson
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Structural optimization on a virtual screening hit of smoothened receptor.
European Journal of Medicinal Chemistry, 2019The Hedgehog (Hh) pathway plays a critical role during embryonic development by controlling cell patterning, growth and migration. In adults, the function of Hh pathway is curtailed to tissue repair and maintenance.
Shiwei Song +13 more
semanticscholar +3 more sources
Evaluating Smoothened as a G-protein-coupled receptor for Hedgehog signalling
Trends in Cell Biology, 2010The Hedgehog signalling pathway controls numerous developmental processes. In response to Hedgehog, Smoothened (Smo), a seven-pass transmembrane protein, orchestrates pathway signalling and controls transcription factor activation. In the absence of Hedgehog, the receptor Patched indirectly inhibits Smo in a catalytic manner. Many questions surrounding
Ayers, Katie L, Thérond, Pascal P
openaire +5 more sources
The structure-based traceless specific fluorescence labeling of the smoothened receptor.
Organic & Biomolecular Chemistry, 2019The smoothened receptor (SMO) mediates the hedgehog (Hh) signaling pathway and plays a vital role in embryonic development and tumorigenesis. The visualization of SMO has the potential to provide new insights into its enigmatic mechanisms and associated ...
Dongxiang Xue +12 more
semanticscholar +3 more sources
Journal of Medicinal Chemistry, 2019
We unveiled an underside binding site on smoothened receptor (SMO) by a co-localization strategy using two struc-turally-complementary photoaffinity probes, derived from a known ligand Allo-1.
F. Zhou +13 more
semanticscholar +3 more sources
We unveiled an underside binding site on smoothened receptor (SMO) by a co-localization strategy using two struc-turally-complementary photoaffinity probes, derived from a known ligand Allo-1.
F. Zhou +13 more
semanticscholar +3 more sources
Proteins: Structure, Function, and Bioinformatics, 2020
Smoothened (SMO) antagonist Vismodegib effectively inhibits the Hedgehog pathway in proliferating cancer cells. In early stage of treatment, Vismodegib exhibited promising outcomes to regress the tumors cells, but ultimately relapsed due to the drug ...
N. Sinha, S. Chowdhury, R. Sarkar
semanticscholar +1 more source
Smoothened (SMO) antagonist Vismodegib effectively inhibits the Hedgehog pathway in proliferating cancer cells. In early stage of treatment, Vismodegib exhibited promising outcomes to regress the tumors cells, but ultimately relapsed due to the drug ...
N. Sinha, S. Chowdhury, R. Sarkar
semanticscholar +1 more source
European Journal of Pharmacology, 2015
Hedgehog (Hh) signaling critical for development, differentiation, and cell growth is involved in several cancers, including medulloblastoma and basal cell carcinoma. Although antagonism of the smoothened receptor (SMO), which mediates Hh signaling, is an attractive therapeutic target, a drug-resistant mutation in SMO (SMO-D473H) was identified in a ...
Y. Shimizu +5 more
semanticscholar +3 more sources
Hedgehog (Hh) signaling critical for development, differentiation, and cell growth is involved in several cancers, including medulloblastoma and basal cell carcinoma. Although antagonism of the smoothened receptor (SMO), which mediates Hh signaling, is an attractive therapeutic target, a drug-resistant mutation in SMO (SMO-D473H) was identified in a ...
Y. Shimizu +5 more
semanticscholar +3 more sources
Evidence for Allosteric Interactions of Antagonist Binding to the Smoothened Receptor
The Journal of Pharmacology and Experimental Therapeutics, 2009The 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 +17 more
semanticscholar +3 more sources
Computer-aided design of arylphthalazines as potential smoothened receptor antagonists
Doklady Chemistry, 2012The 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.
E. Radchenko +5 more
semanticscholar +3 more sources