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The reaction of a series of azapeptides with porcine pancreatic (PP) elastase and human leukocyte (HL) elastase has been studied and a series of new inhibitors and active site titrants were found for both PP elastase and HL elastase. Azapeptide p-nitrophenyl esters acylate both HL and PP elastase to form stable acylenzymes, which can be used for crystallographic studies. We have investigated the effect of a P1, P2, or P3 aza-amino acid residue on the reactivity of azapeptides with elastase. We have also studied the effect of changing the nature of the P1' leaving group and other portions of azapeptide structure. N-Acetyl-L-alanyl-L-alanyl-alpha-azaalanine p-nitrophenyl ester, N-acetyl-L-alanyl-L-alanyl-alpha-azanorleucine p-nitrophenyl ester, and N-acetyl-L-alanyl-L-alanyl-alpha-azanorvaline p-nitrophenyl ester are suitable titrants for either PP or HL elastase.
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
April 1998,
Journal of medicinal chemistry,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
April 1984,
The Journal of biological chemistry,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
September 1973,
European journal of biochemistry,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
January 1977,
Advances in experimental medicine and biology,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
October 1976,
Biochemical and biophysical research communications,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
May 1982,
The Journal of biological chemistry,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
September 1997,
Journal of medicinal chemistry,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
November 1977,
Biochimica et biophysica acta,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
March 1975,
Journal of molecular biology,
J C Powers, and
R Boone, and
D L Carroll, and
B F Gupton, and
C M Kam, and
N Nishino, and
M Sakamoto, and
P M Tuhy
February 1985,
Journal of medicinal chemistry,
