- Tytuł:
- Polypharmacology – a challenge for current drug design approaches
- Autorzy:
-
Podlewska, Sabina
Kurczab, Rafał - Powiązania:
- https://bibliotekanauki.pl/articles/93192.pdf
- Data publikacji:
- 2019
- Wydawca:
- Państwowa Wyższa Szkoła Zawodowa w Tarnowie
- Tematy:
-
G protein-coupled receptor
polypharmacology
serotonin receptor
dopamine receptor
antipsychotic profile
ligand
receptor sprzężony z białkiem G
polifarmakologia
receptor serotoninowy
receptor dopaminowy
profil przeciwpsychotyczny - Opis:
- Drug design process faces many challenges, and the most important ones are connected with side effects. Finding compounds that possess affinity towards target of interest is relatively simple; however, an approach one disease-one target is now making space for the search of polypharmacological ligands, where activity towards several proteins is considered at one time. Such proteins are not always the target ones, but very often such panels include also anti-targets, interaction with which is not desired, due to the side effects that may occur upon such contact. In the study, we examined ligands of four G protein-coupled receptors, forming antipsychotic profile: dopamine receptor D2, serotonin receptors 5-HT2A, 5-HT2C (anti-target), and 5-HT6. Number of ligands belonging to particular activity groups, as well as the selected compound structures are examined in detail. Also compound similarity between sets of different activity groups is analysed, giving a picture of difficulty of constructing molecular modeling methodologies that can help in the search of compounds with desired activity profile.
- Źródło:
-
Science, Technology and Innovation; 2019, 6, 3; 19-23
2544-9125 - Pojawia się w:
- Science, Technology and Innovation
- Dostawca treści:
- Biblioteka Nauki
Artykuł