Polypharmacology – a challenge for current drug design approaches

• Autorzy: Podlewska Sabina , Kurczab Rafał

Identyfikatory

DOI

10.5604/01.3001.0013.5185

• Języki publikacji: EN

Abstrakty

EN

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-HT_2A, 5-HT_2C (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.

Słowa kluczowe

EN

G protein-coupled receptor; polypharmacology; serotonin receptor; dopamine receptor; antipsychotic profile; ligand

PL

receptor sprzężony z białkiem G; polifarmakologia; receptor serotoninowy; receptor dopaminowy; profil przeciwpsychotyczny; ligand

• Wydawca: Państwowa Wyższa Szkoła Zawodowa w Tarnowie
• Czasopismo: Science, Technology and Innovation
• Rocznik: 2019
• Tom: Vol. 6, no. 3
• Strony: 19--23
• Opis fizyczny: Bibliogr. 21 poz., rys., tab.

Twórcy

autor

Podlewska Sabina

• Maj Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31–343 Kraków, Poland
• Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30–688 Kraków, Poland

autor

Kurczab Rafał

• Maj Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31–343 Kraków, Poland

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