Elucidation of Mechanism for Ligand Efficacy at Leukotriene
B4 Receptor 2 (BLT2)
Posted on 2020-07-17 - 19:07
G protein-coupled
receptors (GPCRs) have always been important
drug targets in the pharmaceutical industry. One major question for
the current GPCR drug discovery is how drugs have distinct efficacies
at the same GPCR target. Related to this question, we studied how
different ligands can have disparate efficacies at Leukotriene B4 receptor (BLT2). By using molecular modeling studies, we
predicted that Tyr2716.51 located at TM6 of BLT2 performs
as a key trigger for its activation and verified the prediction by
site-directed mutagenesis, chemotactic motility studies, which included
a chemical derivative of agonist CAY10583. We further identified Asn2756.55 located at TM6 as a weak activation trigger in BLT2 and
performed double mutation studies to confirm our computational results.
Our results provide strong evidence for the exact mechanism of ligand
efficacy at BLT2.
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Kim, Minsup; Wei, Jun-Dong; Harmalkar, Dipesh S.; Goo, Ja-il; Lee, Kyeong; Choi, Yongseok; et al. (2020). Elucidation of Mechanism for Ligand Efficacy at Leukotriene
B4 Receptor 2 (BLT2). ACS Publications. Collection. https://doi.org/10.1021/acsmedchemlett.0c00065
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AUTHORS (8)
MK
Minsup Kim
JW
Jun-Dong Wei
DH
Dipesh S. Harmalkar
JG
Ja-il Goo
KL
Kyeong Lee
YC
Yongseok Choi
JK
Jae-Hong Kim
AC
Art E. Cho