Benzamidine, trypsin inhibition

G Naray-Szabo (1984) Quantum chemical calculation of the enzyme ligand interaction energy for trypsin inhibition by benzamidines, J Am Chem Soc 106( 16 ) 4584—4589... 

Indicator variables (/) are often used to highlight a structural feature present in some of the molecules in a data set that confers unusual activity or lack of it to these particular members. Their use could be beneficial in cases where the data set is heterogeneous and includes large numbers of members with unusual features that may or may not impact a biological response. QSAR for the inhibition of trypsin by X-benzamidines used indicator variables to denote the presence of unusual features such as positional isomers and vinyl/ carbonyl-containing substituents (170). A recent study on the inhibition of lipoxygenase catalyzed production of leukotriene B4 and 5-hydroxyeicosatetraenoic from arachidonic... 

Substituted (i.e. C (NH)NH2, halogen, N02 etc.) benzylphenyl ethers, a,(ji)-dioxyalkanes and a,a, a"-tris(phenoxy) mesitylene benzamidines have been synthesized and analyzed for their inhibition of boar acrosin, a trypsin-like protease in spermatozoa. 2 of the compounds are more... 

Markwart F, Landmann H, Walsmann P. Comparative studies on the inhibition of trypsin, plasmin, and thrombin by derivatives of benzylamine and benzamidine. Eur J Biochem 1968 6 502-506. 

Popular stabilizers in the solubUization buffer are 10 to 20% (w/v) glycerine, 1 mM DTT, and 0.1 to 1 mM EDTA. The protease inhibitors PMSF, bacitracine, trypsin inhibitor, leu-peptin, benzamide, and benzamidine are also a blessing, in that binding activities in solution are more sensitive against protease than in the membrane (see Table 5.1). PMSF irreversibly inhibits serin proteases via covalent derivatization of the active center. A one-time application is thus sufficient, especially because PMSF falls apart in watery solution (half-life of a few hours). 

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