scholarly journals Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells

2016 ◽  
Vol 11 (12) ◽  
pp. 3256-3262 ◽  
Author(s):  
Ursula R. Rodgers ◽  
Thomas Lanyon-Hogg ◽  
Naoko Masumoto ◽  
Markus Ritzefeld ◽  
Rosemary Burke ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
Hedgehog Signaling ◽  
Acyltransferase Inhibitors ◽  
Hedgehog Acyltransferase ◽  
Small Molecule Probe

Rational design of water-dispersible and biocompatible nanoprobes with H2S-triggered NIR emission for cancer cell imaging

2020 ◽  
Vol 8 (28) ◽  
pp. 6013-6016
Author(s):  
Hengyan Liu ◽  
Ge Xu ◽  
Tianli Zhu ◽  
Rongchen Wang ◽  
Jiahui Tan ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cancer Cell ◽  
Small Molecule ◽  
Rational Design ◽  
Cell Imaging ◽  
Imaging Modality ◽  
Aqueous Solubility ◽  
Water Dispersible ◽  
Nir Emission ◽  
Small Molecule Probe

A nanoprobe with good aqueous solubility and biocompatibility by trapping an H2S-activatable small molecule probe in the interior of surface cross-linked micelles was fabricated for imaging of H2S-rich cancer cells in a dual-color imaging modality.

scholarly journals Microfluidic Mobility Shift Assay for Real-Time Analysis of Peptide N-Palmitoylation

2017 ◽  
Vol 22 (4) ◽  
pp. 418-424
Author(s):  
Thomas Lanyon-Hogg ◽  
Neki V. Patel ◽  
Markus Ritzefeld ◽  
Katherine J. Boxall ◽  
Rosemary Burke ◽  
...  
Keyword(s):  
Real Time ◽  
Small Molecule ◽  
Hedgehog Signaling ◽  
Mobility Shift ◽  
Real Time Analysis ◽  
Extracellular Signaling ◽  
Molecule Inhibitor ◽  
Mobility Shift Assay ◽  
Catalyzed Reactions ◽  
Hedgehog Acyltransferase

The Hedgehog pathway is a key developmental signaling pathway but is also implicated in many types of cancer. The extracellular signaling protein Sonic hedgehog (Shh) requires dual lipidation for functional signaling, whereby N-terminal palmitoylation is performed by the enzyme Hedgehog acyltransferase (Hhat). Hhat is an attractive target for small-molecule inhibition to arrest Hedgehog signaling, and methods for assaying Hhat activity are central to understanding its function. However, all existing assays to quantify lipidation of peptides suffer limitations, such as safety hazards, high costs, extensive manual handling, restriction to stopped-assay measurements, or indirect assessment of lipidation. To address these limitations, we developed a microfluidic mobility shift assay (MSA) to analyze Shh palmitoylation. MSA allowed separation of fluorescently labeled Shh amine-substrate and palmitoylated Shh amide-product peptides based on differences in charge and hydrodynamic radius, coupled with online fluorescence intensity measurements for quantification. The MSA format was employed to study Hhat-catalyzed reactions, investigate Hhat kinetics, and determine small-molecule inhibitor IC50 values. Both real-time and stopped assays were performed, with the latter achieved via addition of excess unlabeled Shh peptide. The MSA format therefore allows direct and real-time fluorescence-based measurement of acylation and represents a powerful alternative technique in the study of N-lipidation.

scholarly journals Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death

Cancer Cell ◽  
2015 ◽  
Vol 28 (2) ◽  
pp. 240-252 ◽  
Author(s):  
Lei Wang ◽  
Yang Yu ◽  
Dar-Chone Chow ◽  
Fei Yan ◽  
Chih-Chao Hsu ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Small Molecule ◽  
Steroid Receptor ◽  
Cell Stress ◽  
Steroid Receptor Coactivator

scholarly journals Characterization of the Indirubin Derivative LDD970 as a Small Molecule Aurora Kinase A Inhibitor in Human Colorectal Cancer Cells

2017 ◽  
Vol 17 (2) ◽  
pp. 110 ◽  
Author(s):  
Karyn Muzinga Ndolo ◽  
Kyeong Ryang Park ◽  
Hyo Jeong Lee ◽  
Kyoung Bin Yoon ◽  
Yong-Chul Kim ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Cancer Cells ◽  
Small Molecule ◽  
Aurora Kinase ◽  
Human Colorectal Cancer ◽  
Aurora Kinase A ◽  
Colorectal Cancer Cells ◽  
Human Colorectal Cancer Cells ◽  
Kinase A

scholarly journals Identification and characterization of small molecule inhibitors of the ubiquitin ligases Siah1/2 in melanoma and prostate cancer cells

2019 ◽  
Vol 449 ◽  
pp. 145-162 ◽  
Author(s):  
Yongmei Feng ◽  
E. Hampton Sessions ◽  
Fan Zhang ◽  
Fuqiang Ban ◽  
Veronica Placencio-Hickok ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Ubiquitin Ligases ◽  
Prostate Cancer Cells ◽  
Identification And Characterization

scholarly journals Characterization of a Novel Small Molecule Subtype Specific Estrogen-Related Receptor α Antagonist in MCF-7 Breast Cancer Cells

PLoS ONE ◽  
2009 ◽  
Vol 4 (5) ◽  
pp. e5624 ◽  
Author(s):  
Michael J. Chisamore ◽  
Michael E. Cunningham ◽  
Osvaldo Flores ◽  
Hilary A. Wilkinson ◽  
J. Don Chen
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Small Molecule ◽  
Breast Cancer Cells ◽  
Estrogen Related Receptor ◽  
Mcf 7
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