Figure 4.
Fig. 4. Active site region of human tPA in complex with the
bis-benzamidine inhibitor. The proximal benzamidine occupies
the^ specificity pocket, and the distal benzamidine reaches
toward^ an electrophilic pocket formed by the side chain
carbonyl atoms of Asp97, Thr98, and Arg174. The benzyl ring of
the inhibitor is perpendicular to the side^ chain of Tyr99; the
side chain of Arg174 is displaced by the amidino group. A,
experimental density (2F[o] F[c]) of
the active site region in complex with the bis-benzamidine^
inhibitor. B, active site region of human tPA in complex with
bis-benzamidine. Arg174 from b-tPA is superimposed (thin lines).
The above figure is reprinted
by permission from the ASBMB:
J Biol Chem
(1997,
272,
21713-21719)
copyright 1997.
F[c]) of
the active site region in complex with the bis-benzamidine^
inhibitor. B, active site region of human tPA in complex with
bis-benzamidine. Arg174 from b-tPA is superimposed (thin lines).