Genetically modified cyclic-nucleotide controlled ion channels

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes genetically modified cyclic nucleotide-gated (CNG) ion channels, specifically engineered to have enhanced sensitivity and selectivity for cyclic adenosine monophosphate (cAMP) over cyclic guanosine monophosphate (cGMP). The key modification involves substituting certain amino acids (such as threonine at position 537 replaced by methionine or valine) in the alpha3 subunit of the CNG channels. The result is a CNG channel that can more accurately detect and respond to changes in intracellular cAMP levels. These modified channels, and cell lines expressing them, can serve as highly sensitive sensors in drug discovery, pharmacological studies, and for real-time measurement of cellular signal transduction pathways involving cAMP.

Use CasesContent extracted from patent full text and abstract with AI.

• High-throughput pharmaceutical drug screening to identify compounds that affect cAMP pathways (such as GPCR agonists/antagonists, adenylate cyclase and phosphodiesterase modulators).
• Functional analysis of G protein-coupled receptors (GPCRs), adenylate cyclases, and phosphodiesterases by measuring intracellular cAMP changes in real time.
• Quantitative characterization of pharmacologically relevant proteins and signaling cascades in both research and pharmaceutical industries.
• Development of sensitive cellular systems or assays to measure intracellular Ca2+ or cAMP levels for diagnostic or research purposes.
• Potential use in basic research to study signal transduction mechanisms involving cyclic nucleotides.

BenefitsContent extracted from patent full text and abstract with AI.

• Much higher sensitivity and selectivity for cAMP compared to wild-type channels, allowing detection of small fluctuations in cAMP even in the presence of cGMP.
• Reduced interference from cGMP, ensuring more accurate and reliable cAMP measurements.
• Enables real-time monitoring of intracellular cAMP changes, which is critical for kinetic studies and rapid screening.
• Facilitates high throughput and even ultra-high throughput screening, enabling testing of tens of thousands of compounds per day.
• Improves the quantitativeness and reproducibility of assay systems for drug discovery and protein characterization.
• Applicable to various cell types and adaptable to many eukaryotic expression systems, increasing assay flexibility.

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Patent Abstract

A genetically modified cyclic-nucleotide controlled ion channels where the subunits thereof are altered in such a manner that they have a higher sensitivity for cAMP in relation to cGMP in comparison with the Wildtype according to Seq ID No. 1 and 2.