• Publications
  • Influence
Irreversible inhibition of serine proteases by peptide derivatives of (alpha-aminoalkyl)phosphonate diphenyl esters.
TLDR
The tripeptide Boc-Val-Pro-ValP(OPh)2, which has a sequence found in a good trifluoromethyl ketone inhibitor of HLE, is the best inhibitor for HLE and porcine pancreatic elastase and the rates of inactivation of chymotrypsin were decreased 2-5-fold in the presence of the corresponding substrate. Expand
Comparision of the Cytotoxic Effects of Birch Bark Extract, Betulin and Betulinic Acid Towards Human Gastric Carcinoma and Pancreatic Carcinoma Drug-sensitive and Drug-Resistant Cell Lines
TLDR
Comparison of cytotoxic activity of crude birch bark extract and purified betulin and betulinic acid towards human gastric carcinoma and human pancreatic carcinoma cell lines shows significant differences in sensitivity between cell lines depending on the compound used, and suggests that both betulin And betulin can be considered as a promising leads in the treatment of cancer. Expand
Mechanism‐based isocoumarin inhibitors for serine proteases: Use of active site structure and substrate specificity in inhibitor design
TLDR
Isocoumarins should be useful in further investigations of the physiological function of serine proteases and may have future therapeutic utility for the treatment of emphysema and coagulation disorders. Expand
Human neutrophil elastase phosphonic inhibitors with improved potency of action.
TLDR
The most active and selective compound developed possessed a k(inact)/K(I) of 2353000 M(-1) s(-1), which is the most potent irreversible peptidyl inhibitor of human neutrophil elastase reported to date. Expand
Glucocorticosteroids inhibit degradation in bovine cartilage explants stimulated with concomitant plasminogen and interleukin-1
TLDR
The inhibition of cartilage degradation by glucocorticosteroids may be due to down-regulation of urokinase plasminogen activator (u-PA) activity, and it has been shown that u-PA may be the first enzyme in the cascade of activation of pro-matrix metalloproteinases by the fibrinolytic system. Expand
Dipeptide phosphonates as inhibitors of dipeptidyl peptidase IV.
TLDR
A series of dipeptides which contained phosphonate analogs of proline and piperidine-2-carboxylic acid (homoproline) have been synthesized and tested as inhibitors of DPP-IV and may be useful therapeutically in the prevention of the rejection of transplanted tissue. Expand
Novel amidine-containing peptidyl phosphonates as irreversible inhibitors for blood coagulation and related serine proteases.
TLDR
The novel amidine-containing peptidyl phosphonates reported here are effective anticoagulants in vitro, and they may have utility for use in vivo. Expand
Phosphonic analogues of glutamic acid as irreversible inhibitors of Staphylococcus aureus endoproteinase GluC: an efficient synthesis and inhibition of the human IgG degradation.
TLDR
The synthesis and the inhibitory properties of novel peptidyl derivatives of a phosphonic glutamic acid analogue are presented and a compound with the highest inhibitory potency showed the ability to prevent V8-mediated human IgG proteolysis in vitro. Expand
The complete control of glucose level utilizing the composition of ketogenic diet with the gluconeogenesis inhibitor, the anti-diabetic drug metformin, as a potential anti-cancer therapy.
TLDR
It is hypothesized that a new treatment for cancer diseases should be explored which includes the ketogenic diet combined with the inhibition of gluconeogenesis by the anti-diabetic drug metformin. Expand
...
1
2
3
4
5
...