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- Chen, Kai; Stafford, Alan R.; Wu, Chengliang; Yeh, Calvin H.; Kim, Paul Y.; Fredenburgh, James C.; Weitz, Jeffrey I.
- Biochemistry 2017 v.56 no.24 pp. 3119-3128
- active sites; anticoagulants; endothelial cells; fibrin; fibrinogen; glycoproteins; ligands; oligonucleotides; thrombin
- ... Thrombin activity, inhibition, and localization are regulated by two exosites that flank the active site. Substrates, cofactors, and inhibitors bind to exosite 1 to promote active site access, whereas exosite 2 interactions hold thrombin on cells, platelets, and proteins. The exosites also serve allosteric roles, whereby ligand binding alters thrombin activity. Previously, we showed that ligands t ...
- Pan, Li-Li; Song, Lin Frank; Miao, Yipu; Yang, Yue; Merz, Kenneth M.
- Biochemistry 2017 v.56 no.24 pp. 2995-3007
- active sites; catalytic activity; energy; fungi; models; molecular dynamics; mutants; topology
- ... FtmPT1 is a fungal indole prenyltransferase that affords Tryprostatin B from Brevianamide F and dimethylallyl pyrophosphate; however, when a single residue in the active site is mutated (Gly115Thr), a novel five-membered ring compound is obtained as the major product with Tryprostatin B as the minor product. Herein, we describe detailed studies of the catalysis of the Gly115Thr mutant of FtmPT1 wi ...