Design av Peptid mimetics foer den Rodopsinbundna Konformationen ave Transducins C-Terminala Segment Gta (340-350)(Suggestion on Novel Peptidomimetics for the Rhodopsin-bound Conformation of Transducin's C-terminal Segment Gta(340-350)).

摘要

In the chemical structure of a ligand is known, molecular modelling can be used to design structurally simplified lead compounds with receptor activity. By using (theoretical) conformational search, knowledge of a simplified structure's ability to mimic the active conformation of a ligand can be gained. Molecular modelling techniques can be used to reduce the time demanding step of designing new compounds (Antidotes, drugs and other active substances) by reducing the number of lead compounds that needs to be synthesized and tested with respect to activity. In this report, a number of peptide mimetics for the G-protein Transducin's C-terminal segments Gt(alpha)(340-350) is presented. These have been selected using molecular modelling techniques with the aim to mimic Transducin's conformation when bound to the receptor Rhodospin. The purpose with these lead compounds was to see if the conformation of Gt(alpha)(340-350), proposed by transferred-NOE (TRNOE), was correct. With shown activity towards Rhodopsin, these compounds might be able to inhibit the GTP-GDP exchange and by that the light cascade.