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A Click-Chemistry Linked 2′3′-cGAMP Analogue
Authors:Clemens Reto Dialer  Samuele Stazzoni  David Jan Drexler  Felix Moritz Müller  Simon Veth  Alexander Pichler  Dr Hidenori Okamura  Dr Gregor Witte  Prof Dr Karl-Peter Hopfner  Prof Dr Thomas Carell
Institution:1. Department of Chemistry, Ludwig-Maximilians-Universität München, Butenandtstrasse 5–13, 81377 Munich, Germany;2. Gene Center and Department of Biochemistry, Ludwig-Maximilians-Universität München, Feodor-Lynen-Strasse 25, 81377 Munich, Germany
Abstract:2′3′-cGAMP is an uncanonical cyclic dinucleotide where one A and one G base are connected via a 3′-5′ and a unique 2′-5′ linkage. The molecule is produced by the cyclase cGAS in response to cytosolic DNA binding. cGAMP activates STING and hence one of the most powerful pathways of innate immunity. cGAMP analogues with uncharged linkages that feature better cellular penetrability are currently highly desired. Here, the synthesis of a cGAMP analogue with one amide and one triazole linkage is reported. The molecule is best prepared via a first CuI-catalyzed click reaction, which establishes the triazole, while the cyclization is achieved by macrolactamization.
Keywords:cGAMP analogue  click chemistry  cyclophane  macrolactamization  STING
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