L-lysinethiol: a subnanomolar inhibitor of aminopeptidase B.
L-Lysinethiol was found to be an extremely potent inhibitor of aminopeptidase B (AP-B) with a Ki = 9.1 X 10(-10) M. L-leucinethiol was also a potent inhibitor of AP-B (kj = 1.3 X 10(-7) M), while the D-isomer was much less effective (Ki = 9.8 X 10(-5) M). A thiol-zinc interaction at the active site is postulated for AP-B.
D000596:Amino Acids / Q000494:pharmacology; D000626:Aminopeptidases / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D000818:Animals; D003600:Cytosol / Q000201:enzymology; D007668:Kidney / Q000201:enzymology; D007931:Leucyl Aminopeptidase / Q000302:isolation & purification; D008239:Lysine / Q000031:analogs & derivatives* / Q000494:pharmacology; D008861:Microsomes / Q000201:enzymology; D013438:Sulfhydryl Compounds / Q000494:pharmacology*; D013552:Swine
D000596:Amino Acids; D013438:Sulfhydryl Compounds; C053175:lysinethiol; D000626:Aminopeptidases; D007931:Leucyl Aminopeptidase; C019721:aminopeptidase B; D008239:Lysine