Imikhiqizo

I-thrombin-activatable fibrinolysis inhibitor (TAFIa) ecushiwe iyi-carboxypeptidase equkethe i-zinc futhi ivimbela ngokuphawulekayo i-fibrinolysis.Ngakho-ke ama-TAFIa inhibitors kulindeleke ukuthi asebenze njengama-profibrinolytic agents.Sisanda kubika ukuklanywa nokuhlanganiswa kwe-selenium-containing inhibitors ye-TAFIa kanye nomsebenzi wawo wokuvinjelwa.Lapha sibika izakhiwo zekristalu ze-selenium-, i-sulphur-, ne-phosphinic acid-containing inhibitors enamandla aboshwe ku-porcine pancreatic carboxypeptidase B (ppCPB).I-ppCPB iyi-homologue ye-TAFIa futhi ithatha indawo ye-TAFIa yokuhlaziywa kwecrystallographic.Izinhlaka zekristalu ze-ppCPB ezihlanganiswe ne-selenium compound 1a, i-analogue 2 yesulfure yayo, kanye nokuphuma kwe-phosphinic acid EF6265 kunqunywe ku-1.70, 2.15, kanye ne-1.90 Å resolution, ngokulandelana.I-inhibitor ngayinye ibophezela kusayithi elisebenzayo le-ppCPB ngendlela efanayo naleyo ephawulwe kuma-inhibitor abikwe ngaphambilini.Ngakho-ke, kuma-complexes, i-selenium, isulfure, ne-phosphinic acid oksijini ixhumanisa i-zinc ku-ppCPB.Lokhu ukubonwa kokuqala kanye nombiko we-selenium exhumanisa ne-zinc ku-CPB.