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Investigation of thrombin activity with par 1-based fluorogenic peptides
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نویسنده
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vieira s.m. ,dos reis f.g. ,geraldo r. ,da silva dutra d.l. ,juliano l. ,juliano m.a. ,mignaco j.a. ,zingali r.b.
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منبع
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protein and peptide letters - 2013 - دوره : 20 - شماره : 10 - صفحه:1129 -1135
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چکیده
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Thrombin,a highly specific protease of blood coagulation,has two exosites that modulate its specificity. we designed two sets of synthetic substrate fret peptides with 25- or 11- amino acids (aa) each,based on the par 1 sequence,to characterize the effect of exosite 1 engagement on substrate catalysis and preference. the 25-aa set encompassed a sequence binding to exosite 1,and structural modeling showed that binding to thrombin did not differ significantly from that of par 1 peptide. modification at the p3'position of the 25 or 11-aa peptides resulted in small effect on kinetic parameters. ionic strength higher than physiologic depressed thrombin action on the 25-aa peptides. addition of ligands of the exosite 1 negatively modulated the catalysis of 25-aa substrates. in conclusion,we succeeded to mimic and study in real time,using these synthetic peptides,the influence of ligand binding to exosite 1 on thrombin activity. © 2013 bentham science publishers.
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کلیدواژه
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Enzyme activity; Exosite 1; Fluorogenic peptides; PAR 1 and thrombin
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آدرس
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instituto de bioquímica médica,ufrj,ccs,sala h2-008,avenida carlos chagas filho,373, Brazil, instituto de bioquímica médica,ufrj,ccs,sala h2-008,avenida carlos chagas filho,373, Brazil, instituto de bioquímica médica,ufrj,ccs,sala h2-008,avenida carlos chagas filho,373, Brazil, departamento de biofísica,escola paulista de medicina, Brazil, departamento de biofísica,escola paulista de medicina, Brazil, instituto de bioquímica médica,ufrj,ccs,sala h2-008,avenida carlos chagas filho,373, Brazil, instituto de bioquímica médica,ufrj,ccs,sala h2-008,avenida carlos chagas filho,373,rio de janeiro - rj,brazil,instituto nacional de biologia estrutural e bioimagem, Brazil
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Authors
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