Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 11, Pages 4839-4844Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm501840b
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Anabaenopeptins isolated from cyanobacteria were identified as inhibitors of carboxypeptidase TAFIa. Cocrystal structures of these macrocyclic natural product inhibitors in a modified porcine carboxypeptidase B revealed their binding mode and provided the basis for the rational design of small molecule inhibitors with a previously unknown central urea motif. Optimization based on these design concepts allowed for a rapid evaluation of the SAR and delivered potent small molecule inhibitors of TAFIa with a promising overall profile.
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