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Chemical Compound Review:

AC1L9842 (2R)-1-[(2R)-2-amino-3- phenyl-propanoyl]-N...

Synonyms: C02828, D-Phe-Pro-Arg-CH2Cl

Kunitada, S. et al., Seifried, E. et al., Orthner, C.L., Seifried, E. et al., Odake, S. et al., et al.

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High impact information on D-Phe-Pro-Arg-CH2Cl

This reduction in binding was also shown using t-PA treated with the chloromethylketone, D-Phe-Pro-Arg-CH2Cl (PPACK) (36% +/- 13%, n = 3), and with S478A, a mutant t-PA in which the active site serine at position 478 has been substituted by alanine (43% +/- 6%, n = 3) [1].
Comparison of specific antibody, D-Phe-Pro-Arg-CH2Cl and aprotinin for prevention of in vitro effects of recombinant tissue-type plasminogen activator on haemostasis parameters [2].
The tripeptide D-Phe-Pro-Arg-CH2Cl and related tetrapeptide inhibitors inhibit thrombin more potently than factor IXa and plasma kallikrein by 2-5 orders of magnitude [3].
The S2238 activity was inhibited by D-Phe-Pro-Arg-CH2Cl, but with an estimated second-order rate constant of 3 X 10(5) mol/L-1 minute-1, approximately 1000 times less than for thrombin [4].

Gene context of D-Phe-Pro-Arg-CH2Cl

In normal plasma, collected in the presence or absence of D-Phe-Pro-Arg-CH2Cl, t-PA occurs primarily as a Mr greater than 700 KDa form containing t-PA/PAI-1 complex [5].

Analytical, diagnostic and therapeutic context of D-Phe-Pro-Arg-CH2Cl

Plasma antigen was measured using enzyme-linked immunosorbent assay (ELISA) with and without treatment of blood at collection with D-Phe-Pro-Arg-CH2Cl (P PACK); activity was quantified in acidified plasma both on fibrin plates and in a chromogenic assay [6].

References

Inhibition of clot lysis and decreased binding of tissue-type plasminogen activator as a consequence of clot retraction. Kunitada, S., FitzGerald, G.A., Fitzgerald, D.J. Blood (1992) [Pubmed]
Comparison of specific antibody, D-Phe-Pro-Arg-CH2Cl and aprotinin for prevention of in vitro effects of recombinant tissue-type plasminogen activator on haemostasis parameters. Seifried, E., Tanswell, P. Thromb. Haemost. (1987) [Pubmed]
Inhibition of thrombin by arginine-containing peptide chloromethyl ketones and bis chloromethyl ketone-albumin conjugates. Odake, S., Kam, C.M., Powers, J.C. J. Enzym. Inhib. (1995) [Pubmed]
Characterization of proteases in AHF concentrates: effect on factor VIII:von Willebrand protein as assessed by high-pressure gel permeation chromatography. Orthner, C.L. J. Lab. Clin. Med. (1984) [Pubmed]
Molecular forms of plasminogen activator inhibitor-1 (PAI-1) and tissue-type plasminogen activator (t-PA) in human plasma. Alessi, M.C., Juhan-Vague, I., Declerck, P.J., Collen, D. Thromb. Res. (1991) [Pubmed]
Pharmacokinetics of antigen and activity of recombinant tissue-type plasminogen activator after infusion in healthy volunteers. Seifried, E., Tanswell, P., Rijken, D.C., Barrett-Bergshoeff, M.M., Su, C.A., Kluft, C. Arzneimittel-Forschung. (1988) [Pubmed]

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