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Items: 4


3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.

Baqi Y, Pillaiyar T, Abdelrahman A, Kaufmann O, Alshaibani S, Rafehi M, Ghasimi S, Akkari R, Ritter K, Simon K, Spinrath A, Kostenis E, Zhao Q, Köse M, Namasivayam V, Müller CE.

J Med Chem. 2018 Sep 27;61(18):8136-8154. doi: 10.1021/acs.jmedchem.7b01768. Epub 2018 Sep 5.


Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist.

Hennen S, Wang H, Peters L, Merten N, Simon K, Spinrath A, Blättermann S, Akkari R, Schrage R, Schröder R, Schulz D, Vermeiren C, Zimmermann K, Kehraus S, Drewke C, Pfeifer A, König GM, Mohr K, Gillard M, Müller CE, Lu QR, Gomeza J, Kostenis E.

Sci Signal. 2013 Oct 22;6(298):ra93. doi: 10.1126/scisignal.2004350.


Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling.

Hillmann P, Ko GY, Spinrath A, Raulf A, von Kügelgen I, Wolff SC, Nicholas RA, Kostenis E, Höltje HD, Müller CE.

J Med Chem. 2009 May 14;52(9):2762-75. doi: 10.1021/jm801442p.


Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes.

Christiansen E, Urban C, Merten N, Liebscher K, Karlsen KK, Hamacher A, Spinrath A, Bond AD, Drewke C, Ullrich S, Kassack MU, Kostenis E, Ulven T.

J Med Chem. 2008 Nov 27;51(22):7061-4. doi: 10.1021/jm8010178.


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