Peptidyl inverse esters of p-methoxybenzoic acid: a novel class of potent inactivator of the serine proteases

J LYNAS, B WALKER - Biochemical Journal, 1997 - portlandpress.com
A series of novel synthetic peptides, containing a C-terminal β-amino alcohol linked to p-
methoxybenzoic acid via an ester linkage, have been prepared and tested as inhibitors …

O'-(Epoxyalkyl) tyrosines and (Epoxyalkyl) phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism

G Tous, A Bush, A Tous, F Jordan - Journal of medicinal chemistry, 1990 - ACS Publications
A series of 0-(epoxyalky l) tyrosines and a carboxy terminal (epoxyalkyl) tyrosine and-
phenylalanine were synthesized as potential serine protease inhibitors. N-Acetyl derivatives …

Carboxyl-modified amino acids and peptides as protease inhibitors

SA Thompson, PR Andrews… - Journal of medicinal …, 1986 - ACS Publications
Design Our purpose was to evaluate the inhibitory potential of functional groups
incorporated into substrate analogues by testing them ágainst proteases representing …

N-(sulfonyloxy) phthalimides and analogues are potent inactivators of serine proteases.

U Neumann, M Gütschow - Journal of Biological Chemistry, 1994 - Elsevier
A series of 2-(sulfonyloxy) and 2-(acyloxy)-1H-isoindole-1, 3 (2H)-diones and analogous 1H-
benz [de] isoquinoline-1, 3 (2H)-diones was prepared, and their potential to inactivate …

Irreversible inhibitions of serine proteases by peptidyl allylic halide derivatives

T Ohba, E Ikeda, J Wakayama, H Takei - Bioorganic & Medicinal Chemistry …, 1996 - Elsevier
IRREVERSIBLE INHIBITIONS OF SERINE PROTEASES BY PEPTIDYL ALLYLIC HALIDE
DERIVATIVES R Page 1 Pergamon Bioorganic & Medicinal Chemistry Letters, Vol. 6, No. 3, pp …

Synthesis of peptidyl ene diones: selective inactivators of the cysteine proteinases

P Darkins, BF Gilmore, SJ Hawthorne… - Chemical Biology & …, 2007 - Wiley Online Library
A series of synthetic peptides in which the C‐terminal carboxyl grouping (‐CO2H) of each
has been chemically converted into a variety of ene dione derivatives (‐CO‐CH= CH‐CO‐X; …

[引用][C] Synthetic and naturally occurring protease inhibitors containing an electrophilic carbonyl group

S Mehdi - Bioorganic Chemistry, 1993 - Elsevier
If an enzymologist were to list the attributes of an enzyme that would be most useful for the
design of a mechanism-based inhibitor, the presence of an activesite nucleophile with a well …

Mechanism-based inactivation of human leukocyte elastase via an enzyme-induced sulfonamide fragmentation process

L Wei, Z Lai, X Gan, KR Alliston, J Zhong… - Archives of biochemistry …, 2004 - Elsevier
We describe herein the design and in vitro biochemical evaluation of a novel class of
mechanism-based inhibitors of human leukocyte elastase (HLE) that inactivate the enzyme …

N-[2,2-Dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-l-phenylalanine Ethyl Ester as a Stable Ester-Type Inhibitor of Chymotrypsin-like Serine Proteases:  Structural …

K Iijima, J Katada, E Yasuda, I Uno… - Journal of medicinal …, 1999 - ACS Publications
We introduce a new potent inhibitor, N-[2, 2-dimethyl-3-(N-(4-cyanobenzoyl) amino)
nonanoyl]-l-phenylalanine ethyl ester (3), which preferentially inhibits serine proteases …

Aminoalkylphosphonofluoridate derivatives: Rapid and potentially selective inactivators of serine peptidases

LA Lamden, FA Bartlett - Biochemical and Biophysical Research …, 1983 - Elsevier
Phosphonic acid analogs of N-Cbz-alanine and N-Cbz-phenylalanine have been converted
to the ester and amide fluoridates and evaluated as inactivators of elastase (EC 3.4. 21.11) …