ИСТИНА

Gastroprotection and adaptive gastroprotection medicines are welcome since by estimation about 10% of EU and US people suffer from dysfunction of gastrointestinal tract, especially caused by administration of non-steroidal anti-inflammatory drugs (NSAID). Despite the protective effect of prostaglandin E2 (PGE2) was shown in early 1980s, no consistent and widely accepted model of gastroprotection has appeared in the literature since that time. PGE2 is known to exert its activity through the four subtypes of PGE2 receptors – EP1, EP2, EP3 and EP4, which are GPCR-receptors, whose activation results in different and sometime opposite cellular response. To guide structure based drug design of gastroprotective medicines with desired activity and selectivity profile, high quality models of all subtypes of PGE2 receptors are necessary. Homology models for all four subtypes of human PGE2 receptors were constructed with different approaches to assure diversity and increase success rate.