1982
DOI: 10.1016/0022-2836(82)90393-x
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Crystallographic study of the binding of a trifluoroacetyl dipeptide anilide inhibitor with elastase

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Cited by 61 publications
(34 citation statements)
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“…1 between the inhibitor and the catalytic residues Ser-195 and His-57 of HNE, one can infer that the MSACK binding configuration observed is close to the productive one and has been preserved in the course of the inhibition reaction. Earlier crystallographic studies with inhibitor and cleavage product complexes in PPE (33)(34)(35)(36) showed a variety of unusual binding configurations-presumably a reflection of the shallow depth of the S, specificity pocket-and suggested that elastase might be atypical among the serine proteases. Our results strongly support the view that the elastases are "conventional" chymotrypsin-like serine proteases in their mode of productive binding as well as in the configuration of their catalytic groups.…”
Section: Resultsmentioning
confidence: 99%
“…1 between the inhibitor and the catalytic residues Ser-195 and His-57 of HNE, one can infer that the MSACK binding configuration observed is close to the productive one and has been preserved in the course of the inhibition reaction. Earlier crystallographic studies with inhibitor and cleavage product complexes in PPE (33)(34)(35)(36) showed a variety of unusual binding configurations-presumably a reflection of the shallow depth of the S, specificity pocket-and suggested that elastase might be atypical among the serine proteases. Our results strongly support the view that the elastases are "conventional" chymotrypsin-like serine proteases in their mode of productive binding as well as in the configuration of their catalytic groups.…”
Section: Resultsmentioning
confidence: 99%
“…The coordinates for the crystallographic structure of the PEl-TFAI inhibitor complex [21] were obtained from the Protein Data Bank. Subsequently, the coordinates of TFAI were inserted into the models of BSIII and HPE.…”
Section: Three-dimensional Modeland and Active-site Mappingmentioning
confidence: 99%
“…trifluoroacetylated amino-acid derivatives and peptides is of special interest, since they are potent inhibitors of proteolytic enzymes, the protecting group forcing the inhibitor to bind in a special mode to the active site of the enzyme (Hughes, Sieker, Bieth & Dimicoli, 1982).…”
mentioning
confidence: 99%
“…The rotational disorder, characteristic of the trifluoroacetamido group (Barone, Bavoso, Benedetti, Di Blasio, Grimaldi, Lelj, Pavone, Pedone, Bonora, Toniolo, Lingham & Hardy, 1984;Kalyanaraman, Kispert & Atwood, 1978), unless rigidly bound in the active site of an enzyme (Hughes et al, 1982), is found also in FsAc-Aib-OH.…”
mentioning
confidence: 99%