Interakcija različitih fragmenata treće citoplazmatične petlje dopaminskog d2l receptora čoveka sa a-podjedinicom gi1 proteina - moguća terapeutska primena
Interaction of different third intracellular loop fragments of human dopamine d2l receptor with a-subunit of gi1 protein - prospective therapeutic application
2002
Authors:
Ignjatović, ĐurđicaŠukalović, Vladimir B.
Tasić, Bosiljka
Kostić-Rajačić, Slađana V.
Šoškić, Vukić
Document Type:
Article (Published version)
,
@ 2015 Društvo medicinskih biohemičara Srbije i Crne Gore
Metadata
Show full item recordAbstract:
In order to find the essential structural motif of the D2L dopamine receptor necessary for the interaction with a-subunit of Gi1 protein, four fragments of the third cytoplasmic loop (CPL3) of this receptor were cloned, expressed in E. coli and purified. After that, fusion proteins with glutathione-S-transferase (GST) were prepared and the interactions quantified by a colorimetric assay for GST activity determination. The presence of D2L-CPL3 fragment-Gia1 complexes was detected by SDS-polyacrylamide gel electrophoresis (PAGE). Kd values for the interaction of the three fragments with Gia1 were similar and in nmol/L range of concentrations, while the peptide representing the insert in the long form of the dopamine D2 receptor expressed about 10-fold lower binding affinity. These results could serve to design new therapeutic agents that might act at the level of receptor/G protein interaction rather than at the level of ligand-receptor binding.
Keywords:
dopaminski D2L receptor; Dopamine D2L receptor; third intracellular loop; treća intracelularna petlja; synthetic peptide; sintetski peptid; receptor/G protein coupling; sprega receptor/G proteinSource:
Yugoslav Medical Biochemistry, 2002, 21, 1, 9-14
DOI: 10.2298/JMH0201009I
ISSN: 0354-3447
WoS: 000174350800002
Scopus: 2-s2.0-0036118627
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