ArticleMolecules (Basel, Switzerland)2011
Fluorescence resonance energy transfer assay for high-throughput screening of ADAMTS1 inhibitors.
Article in Molecules (Basel, Switzerland), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 14 citations in OpenAlex.
- Comprehensive overview of different medicinal parts fromFrontiers in pharmacology · 2024Review
- Mulberry Diels-Alder-type adducts: isolation, structure, bioactivity, and synthesis.Natural products and bioprospecting · 2022Review
- Milestones in the development and implementation of FRET-based sensors of intracellular signals: A biological perspective of the history of FRET.Cellular signalling · 2020Review
- Cartilage Protection and Analgesic Activity of a Botanical Composition Comprised ofEvidence-based complementary and alternative medicine : eCAM · 2017Article
- Analgesic and anti-Inflammatory effect of UP3005, a botanical composition Containing two standardized extracts of Uncaria gambir and Morus alba.Pharmacognosy research · 2015Article
- Article
- Förster resonance energy transfer microscopy and spectroscopy for localizing protein-protein interactions in living cells.Cytometry. Part A : the journal of the International Society for Analytical Cytology · 2013Review
- UP1306, a Botanical Composition with Analgesic and Anti-inflammatory Effect.Pharmacognosy researchArticle
- UP1304, a Botanical Composition Containing Two Standardized Extracts of Curcuma longa and Morus alba, Mitigates Pain and Inflammation in Adjuvant-induced Arthritic Rats.Pharmacognosy researchArticle
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A disintegrin and metalloprotease with thrombospondin type I motifs-1 (ADAMTS1) plays a crucial role in inflammatory joint diseases and its inhibitors are potential candidates for anti-arthritis drugs. For the purposes of drug discovery, we reported the development and validation of fluorescence resonance energy transfer (FRET) assay for high-throughput screening (HTS) of the ADAMTS1 inhibitors. A FRET substrate was designed for a quantitative assay of ADAMTS1 activity and enzyme kinetics studies. The assay was developed into a 50-µL, 384-well assay format for high throughput screening of ADAMTS1 inhibitors with an overall Z' factor of 0.89. ADAMTS1 inhibitors were screened against a diverse library of 40,960 total compounds with the established HTS system. Four structurally related hits, naturally occurring compounds, kuwanon P, kuwanon X, albafuran C and mulberrofuran J, extracted from the Chinese herb Morus alba L., were identified for further investigation. The results suggest that this FRET assay is an excellent tool, not only for measurement of ADAMTS1 activity but also for discovery of novel ADAMTS1 inhibitors with HTS.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.