Synthesis and kinetic evaluation of peptide α-keto-β-aldehyde-based inhibitors of trypsin-like serine proteases

Journal of Pharmacy and Pharmacology

Volumn 53, Issue 4, 2001, Pages 473-480

  Lynas, J F ^a   Martin, S L ^a   Walker, B ^a  

^a QUEEN'S UNIVERSITY BELFAST   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ALDEHYDE DERIVATIVE; LEUPEPTIN; N ALPHA BENZYLOXYCARBONYL GLY GLY ARG 7 AMINO 4 METHYLCOUMARIN; N ALPHA TERT BUTYLOXYCARBONYL VAL LEU LYS 7 AMINO 4 METHYLCOUMARIN; N ALPHA TERT BUTYLOXYCARBONYL VAL PRO ARG 7 AMINO 4 METHYLCOUMARIN; PEPTIDE DERIVATIVE; PLASMIN; SERINE PROTEINASE; SERINE PROTEINASE INHIBITOR; THROMBIN; TRYPSIN; TRYPTASE; UNCLASSIFIED DRUG;

ARTICLE; ASTHMA; BINDING KINETICS; BLOOD CLOTTING DISORDER; CARBOXY TERMINAL SEQUENCE; CATTLE; COMPARATIVE STUDY; DRUG ACTIVITY; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; ENZYME ACTIVITY; ENZYME BINDING; ENZYME INHIBITION; INHIBITION KINETICS; MEDIATOR; MICHAELIS CONSTANT; MICHAELIS MENTEN KINETICS; MOLECULAR MODEL;

EID: 0035042494     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/0022357011775767     Document Type: Article

References (21)

1. Neutrophil elastase inhibitors as treatments for emphysema and chronic bronchitis
2. The urokinase plasminogen activator system in cancer metastasis
3. α-Diketone and α-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases
4. Peptide β-homo-aspartals: Specific inhibitors of interleukin-1β converting enzyme and its homologues (caspases)
5. Peptide aldehyde inhibitors of the kallikreins: An investigation of subsite interactions with tripeptides containing structural variations at the amino terminus
6. Inhibitors of the chymotrypsin-like activity of proteasome based on di- and tri-peptidyl α-keto aldehydes (glyoxals)
7. Development of peptidyl α-keto-β-aldehydes as new inhibitors of cathepsin L - Comparisons of potency and selectivity profiles with cathepsin B
8. Inhibition studies of serine and thiol proteases by new leupeptin analogues
9. The slow-binding and slow tight-binding inhibition of enzyme-catalysed reactions
10. Diastereotopic covalent binding of the natural inhibitor leupeptin to trypsin. Detecting the two interconverting hemiacetals by solution and solid phase NMR spectroscopy
11. Synthesis and biological activity of peptide aldehyde urokinase inhibitors
12. Synthetic low molecular weight thrombin inhibitors - Molecular design and pharmacological profile
13. Determination of the rate constant of the enzyme modification by measuring the substrate reaction in the presence of the modifier
14. Antibiotics and other related microbial products
15. Thrombosis and coagulation
16. Solid-phase peptide synthesis
17. Peptide glyoxals: A novel class of inhibitor for serine and cysteine proteinases
18. Evaluation of dipeptide α-keto-β-aldehydes as new inhibitors of cathepsin S
19. The role of neutral proteases in asthma and rhinitis
20. Synthesis of chiral N-protected α-amino-β-diketones from α-diazoketones derived from natural amino acids