Discovery of Anthranilic Acid Derivatives as Antagonists of the Pro-Inflammatory Orphan G Protein-Coupled Receptor GPR17

The G protein-coupled receptor 17 (GPR17) is an orphan receptor involved in inflammatory diseases. GPR17 antagonists have been proposed for the treatment of multiple sclerosis due to their potential to induce remyelination. Potent, selective antagonists are required to enable target validation. In t...

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Bibliographic Details
Main Author:	Nader M. Boshta (20027701) (author)
Other Authors:	Michael Lewash (20027704) (author), Meryem Köse (1822522) (author), Vigneshwaran Namasivayam (1799728) (author), Soumya Sarkar (1404682) (author), Jan H. Voss (9411140) (author), Andy J. Liedtke (1284045) (author), Anna Junker (1950910) (author), Maoqun Tian (1675567) (author), Anne Stößel (1947553) (author), Mahmoud Rashed (9308243) (author), Ahmed Mahal (5753633) (author), Nicole Merten (2259895) (author), Cécile Pegurier (20027707) (author), Jörg Hockemeyer (6588773) (author), Evi Kostenis (176797) (author), Christa E. Müller (1550497) (author)
Published:	2024
Subjects:	Biophysics Biochemistry Cell Biology Molecular Biology Pharmacology Immunology Cancer Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified radioligand binding assays orphan receptor involved multiple sclerosis due future drug development enable target validation coupled receptor 17 compounds ’ potencies anthranilic acid scaffold anthranilic acid derivatives coupled receptor gpr17 2 nm ). gpr17 antagonists based 91 nm gpr17 antagonists selective antagonists selected antagonists present study novel class lipophilic pocket inflammatory diseases induce remyelination g protein calcium mobilization additionally studied
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Discovery of Anthranilic Acid Derivatives as Antagonists of the Pro-Inflammatory Orphan G Protein-Coupled Receptor GPR17

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