Iimveliso

I-activatable thrombin-activatable fibrinolysis inhibitor (TAFIa) yi-zinc-containing carboxypeptidase kwaye inqanda kakhulu i-fibrinolysis.I-TAFIa inhibitors ke kulindeleke ukuba isebenze njenge-profibrinolytic agents.Kutshanje sixele ukuyilwa kunye nokuhlanganiswa kwe-selenium-equlethe inhibitors ye-TAFIa kunye nomsebenzi wabo wokuthintela.Apha sichaza izakhiwo zekristal ze-selenium enamandla-, isulfure-, kunye ne-phosphinic acid-containing inhibitors ebophelelwe kwi-porcine pancreatic carboxypeptidase B (ppCPB).I-ppCPB yi-homologue ye-TAFIa kwaye ithatha indawo ye-TAFIa yohlalutyo lwecrystallographic.Izakhiwo ze-Crystal ze-ppCPB ezixutywe kunye ne-selenium compound 1a, i-analogue 2 yesulfure, kunye ne-phosphinic acid derivative EF6265 zinqunywe kwi-1.70, 2.15, kunye ne-1.90 Å isisombululo, ngokulandelanayo.I-inhibitor nganye ibophelela kwindawo esebenzayo ye-ppCPB ngendlela efanayo naleyo ibonwe kwii-inhibitors ezixelwe ngaphambili.Ngaloo ndlela, kwii-complexes, i-selenium, isulfure, kunye ne-phosphinic acid oksijini ilungelelanisa i-zinc kwi-ppCPB.Oku kukuqala kokuqwalaselwa kunye nengxelo ye-selenium yokulungelelanisa kwi-zinc kwi-CPB.