[Common properties of pharmacological agonists and antagonists of surface membrane receptors]. / Obshchie svoistva farmakologicheskikh agonistov i antagonistov vneshnemembrannykh receptorov.

Using experimental transcription model in vitro, and method of electron-topological calculations the elements of pharmacological and structural community have been found in the groups of physiologically active compounds (PAC), blocking and activating external cellular receptors. This finding confirms the necessity of subdivision special groups of bio-substrates blockators and activators for hierarchical classification, of PAC.

[New donor-acceptor pairs for fluorogenic substrates with intramolecular fluorescence energy transfer for thrombin and trypsin]. / Novye donorno-aktseptornye pary dlia fluorogennykh substratov s vnutrimolekuliarnym perenosom énergii fluorestsetsii dlia trombina i tripsina.

New substrates for thrombin and trypsin are described: a fluorogenic substrate Abz-Pro-Arg-Gly-Nph (I), whose action is based on intramolecular fluorescence energy transfer, and H-D-Trp-Pro-Arg-pNA (II), which can be used both as a chromogenic substrate and as a substrate with the intramolecular fluorescence energy transfer. In substrate (I), a 4-nitrophenylhydrazide group was first used as an acceptor of excitation energy of the 2-aminobenzoyl group. The substrate is poorly hydrolyzed by thrombin (kcat/K(m) = 1.4 x 10(3) M-1 s-1) and is efficiently cleaved by trypsin (kcat/K(m) = 3.15 x 10(6) M-1 s-1). The hydrolysis of (II) can be monitored both spectrophotometrically, by absorbance at 405 nm, and from the increase in fluorescence at 340 nm. In the efficiency of hydrolysis with thrombin (kcat/K(m) = 3.0 x 10(6) M-1 s-1), compound (II) is comparable with the known chromogenic substrates for this enzyme. The proposed donor-acceptor pairs are promising in designing substrates with the intramolecular fluorescence energy transfer for a variety of proteolytic enzymes.

[Use of the computer simulation method of complementary amino acids base on a genetic code algorithm for the search for new peptide compounds belonging to tuftsin-like activity]. / Ispol'zovanie metoda komp'iuternogo modelirovaniia komplementarnosti aminokilsot na osnovanii algoritma geneticheskogo koda dlia poiska novykh peptidnykh soedinenii, obladaiushchikh taftsinopodobnoi aktivnost'iu.

Methods of k-neighbours and neural networks were used for prediction of pharmacological effects of new compounds wits tuftsin-like activities. The tested compounds were constructed by the complementarity rule of genetic code algorithm. Five of seven substitutions with stereocomplement amino acids in the tuftsin sequence lead to new active compounds. Thus, the use of amino acid complementary code can be a helpful tool for the construction of a new immunomodulating peptide.