In:
Angewandte Chemie, Wiley, Vol. 131, No. 43 ( 2019-10-21), p. 15567-15574
Abstract:
Photopharmacology relies on ligands that change their pharmacodynamics upon photoisomerization. Many of these ligands are azobenzenes that are thermodynamically more stable in their elongated trans ‐configuration. Often, they are biologically active in this form and lose activity upon irradiation and photoisomerization to their cis ‐isomer. Recently, cyclic azobenzenes, so‐called diazocines, have emerged, which are thermodynamically more stable in their bent cis ‐form. Incorporation of these switches into a variety of photopharmaceuticals could convert dark‐active ligands into dark‐inactive ligands, which is preferred in most biological applications. This “pharmacological sign‐inversion” is demonstrated for a photochromic blocker of voltage‐gated potassium channels, termed CAL, and a photochromic opener of G protein‐coupled inwardly rectifying potassium (GIRK) channels, termed CLOGO.
Type of Medium:
Online Resource
ISSN:
0044-8249
,
1521-3757
DOI:
10.1002/ange.v131.43
DOI:
10.1002/ange.201905790
Language:
English
Publisher:
Wiley
Publication Date:
2019
detail.hit.zdb_id:
505868-5
detail.hit.zdb_id:
506609-8
detail.hit.zdb_id:
514305-6
detail.hit.zdb_id:
505872-7
detail.hit.zdb_id:
1479266-7
detail.hit.zdb_id:
505867-3
detail.hit.zdb_id:
506259-7
Bookmarklink
