Biopolym. Cell. 1999; 15(1):23-27.
Structure and Function of Biopolymers
Search for the most common properties of extracellular receptors agonists and antagonists in the in vitro transcription as the model
1Prokopenko V. V., 1Kholodovych V. V., 1Luik A. I.
  1. Institute of Bioorganic Chemistry and Petrochemistry, NAS of Ukraine
    1, Murmans'ka Str., Kyiv, Ukraine, 02094


To search the most common properties of exiraeellular receptors agonists and antagonists the study of their action on the bade riophage T7 RNA-polymerase in vitro transcription was undertaken. Propranolol (β-adrenoceptors antagonist), prazusin (α 1adrenoceptors antagonist), yohimbine, (α2-adrenoceptors antagonist), airopine (muscarinic antagonist), isoproterenol (β-adreno-ceptors agonist), phenylephrine (aradrenoceptors agonist), clonidine (α2-adrenoceptors agonist), carbochol (muscarinic agonist) and synthetical tripeptide fMLP (polymorphonuclear leucocytes chemotaxrs receptors agonist) were studied. It was shown that agonists at the concentration of 10–5 –10–4 M either do not affect transcription or elevate its activity as much as 8–21 %. Antagonists at the same concentrations inhibit the polymerase reaction making it 15–45 % less active. The structural differences of the agonists and antagonists are discussed.


[1] Luik AI, Kukhar' VP, Savranskii LI, Skryma RN, Mukhin VV. Universal cellular systems of external signal perception, transduction and realization as a basis for drug classification and analysis of the structure-activity relations Dokl Akad Nauk SSSR. 1988;301(3):765-8.
[2] Luik AI, Mogilevich SE. The principles of drug classification Eksp Klin Farmakol. 1992;55(1):64-7.
[3] Chemical processes bioregulatory. Ed. VP Kukhar, AI Luik. Kiev: Naukova Dumka, 1992. 368p.
[4] Luik AI. Hierachical classification of physiologically active substances. Theoretical and Experimental Chemistry. 1998, 34(4), pp 177-190 1998. 34, N 4:199—212.
[5] Poda G. I., Dimogolo A. S., Tanchuk V. YU., Tetko I. V., Koshel' M. I., Luyk A. I. Investigation "structure - activity" physiologically active substances, united by a common orientation effects on cell signaling. Khim.-farm. zhurn. 1996. 30(6): 29—35.
[6] Prokopenko RA, Mogilevich SE, Luik AI, Naydyenova IY, Batrak GN, Hawryluk BR, Degtiar VY. Effects of haloperidol and chlorpromazine on smooth muscle contractility, platelet aggregation and neuronal calcium current. Gen Physiol Biophys. 1995;14(4):349-57.
[7] Luik A. I., Naboka Yu. N., Mogilevich S. E. et al. The influence of pH alteration and pharmacological modulators of adenylate cyclase system on human serum albumin conformation. J. Biomol. Struct and Dvn. 1998. 16, N 1: 21—26.
[8] Luik AI, Kukhar VP, Radchenko IV, Ilyasheva LM, Naidenova IYu, Poda GI, Kondrashova LN, Tetko IV. Stereotypical component of mechanism of xenobiotic action. Doklady Akad Nauk Ukr SSR. Ser B. 1990;(8):67-70.
[9] Green JP. Polypharmic antagonists — a class of their own. Trends Pharmacol Sci. 1987; 8(10): 377–379.
[10] LaBella FS. Molecular basis for binding promiscuity of antagonist drugs. Biochem Pharmacol. 1991;42 Suppl:S1-8.
[11] Davanloo P, Rosenberg AH, Dunn JJ, Studier FW. Cloning and expression of the gene for bacteriophage T7 RNA polymerase. Proc Natl Acad Sci USA. 1984;81(7):2035-9.
[12] Krieg PA, Melton DA. In vitro RNA synthesis with SP6 RNA polymerase. Methods Enzymol. 1987;155:397-415.
[13] Tetko I. v., Tanchuk V., Yu. Luik A. I. Application of an evolutionary algorithm to the structure-activity relationship. Proc. of 3rd Ann. Conf. on Evol. Program. Eds A. Sebald, L. Fogel). New York: World Sci., 1994: 109—119.
[14] Tetko IV, Livingstone DJ, Luik AI. Neural network studies. 1. Comparison of overfitting and overtraining. J. Chem. Inf. Comput. Sci., 1995, 35 (5), pp 826–833