An Ultrasensitive and Specific Fluorescence Split-Aptasensor for D-Vp Detection Based on Target-Induced Self-Propelled 3d-Dna Walkers Coupled with Crispr-Cas12a

Published: Jan. 1, 2025

Language: Английский

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Photoisomerization of Azobenzene‐Extended Charybdotoxin for the Optical Control of K_v1.2 Potassium Channel Activity

Angewandte Chemie International Edition, Journal Year: 2025, Volume and Issue: unknown

Published: March 9, 2025

Natural peptides from animal venoms effectively modulate ion channel activity. While photoswitches regulate small compound pharmacology, their application to natural rich in disulfide bridges and active on channels is novel due larger pharmacophores. A pilot study integrating azobenzene into charybdotoxin (ChTx), known for blocking potassium initiated. Two click-chemistry-compatible are synthesized differing length amide orientation (Az1 & Az2). Az1 grafted onto ChTx at various amino acid positions using L-azidohomoalanine mutation. monomers outperformed dimers, particularly with position 14, by exhibiting optimal photoswitching In the cis configuration, altered ChTx's pharmacophore, reducing blockage, while conversely, Az2 increased potency. This pioneers photoswitch complex peptides, leveraging structure-activity relationships. Successful integration depends precise positioning chemical grafting guided SAR insights. advancement underscores adaptability of technology intricate peptide structures, offering new avenues pharmacological modulation.

Language: Английский

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An ultrasensitive and specific fluorescence split-aptasensor for D-VP detection based on target-induced self-propelled 3D DNA walkers coupled with CRISPR-Cas12a

Talanta, Journal Year: 2025, Volume and Issue: 293, P. 128102 - 128102

Published: April 8, 2025

Language: Английский

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Photoisomerization of Azobenzene‐Extended Charybdotoxin for the Optical Control of K_v1.2 Potassium Channel Activity

Angewandte Chemie, Journal Year: 2025, Volume and Issue: unknown

Published: March 9, 2025

Abstract Natural peptides from animal venoms effectively modulate ion channel activity. While photoswitches regulate small compound pharmacology, their application to natural rich in disulfide bridges and active on channels is novel due larger pharmacophores. A pilot study integrating azobenzene into charybdotoxin (ChTx), known for blocking potassium initiated. Two click‐chemistry‐compatible are synthesized differing length amide orientation (Az 1 & Az 2 ). grafted onto ChTx at various amino acid positions using L‐azidohomoalanine mutation. monomers outperformed dimers, particularly with position 14, by exhibiting optimal photoswitching In the cis configuration, altered ChTx's pharmacophore, reducing blockage, while conversely, increased potency. This pioneers photoswitch complex peptides, leveraging structure‐activity relationships. Successful integration depends precise positioning chemical grafting guided SAR insights. advancement underscores adaptability of technology intricate peptide structures, offering new avenues pharmacological modulation.

Language: Английский

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Azologing Vasopressin Provides a Light-Dependent V1bR Probe

Synfacts, Journal Year: 2023, Volume and Issue: 20(01), P. 0088 - 0088

Published: Dec. 8, 2023

Key words vasopressin - photoswitch V1bR Baeyer–Mills reaction

Language: Английский

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