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The R‐diastereomer of phosphorothioate analogs of cGMP, Rp‐cGMPS, is one of few known inhibitors of cGMP‐dependent protein kinase I (PKG I); however, its mechanism of inhibition is currently not fully understood. Here, we determined the crystal structure of the PKG Iβ cyclic nucleotide‐binding domain (PKG Iβ CNB‐B), considered a ‘gatekeeper’ for cGMP activation, bound to Rp‐cGMPS at 1.3 Å. Our structural...
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