Selected Publications from 7TM Pharma

Svendsen, A, Vrecl M, Ellis, T, Heding, A, Kristensen J, Wade J, Bathgate R, De Meyts P, and Nøhr J (2008). Cooperative Binding of Insulin-Like Peptide 3 to a Dimeric Relaxin Family Peptide Receptor 2, Endocrinology, 149(3):1113–1120.

Jorgensen R, Holliday ND, Hansen JL, Vrecl M, Heding A, Schwartz TW, Elling CE (2007). Characterization of G-Protein Coupled Receptor Kinase Interaction with the NK-1 Receptor Using BRET, Molecular Pharmacology, 2007 Nov 6. Epub ahead of print.

Tran TM, Jorgensen R, Clark RB (2007). Phosphorylation of the beta(2)-Adrenergic Receptor in Plasma Membranes by Intrinsic GRK5. Biochemistry, 46(50):14438-49.

Kubale V, Abramović Z, Pogačnik A, Heding A, Šentjurc M, Vrecl M. (2007). Evidence for a role of caveolin-1 in neurokinin-1 receptor plasma membrane localization, efficient signaling and interaction with β-arrestin 2. Cell Tissue Res. Published online: Aug 23.

Jorgensen R, Kubale V, Vrecl M, Schwartz TW, Elling CE (2007). Oxyntomodulin differentially affects glucagon-like peptide-1 receptor beta-arrestin recruitment and signaling through Galpha(s). J Pharmacol Exp Ther.;322(1):148-54. Epub Mar 29.

Elster L, Elling CE and Heding A (2007). Bioluminescence Resonance Energy Transfer as a Screening Assay: Focus on Partial and Inverse Agonism. J Biomol Screen; 12; 41.

Uller L, Mathiesen JM, Alenmyr L, Korsgren M, Ulven T, Högberg T, Andersson G, Persson CG, Kostenis E. (2007). Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respir. Res. Feb 28;8:16.

Ulven T, Receveur JM, Grimstrup M, Rist O, Frimurer TM, Gerlach LO, Mathiesen JM, Kostenis E, Uller L, Högberg T. (2006). Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. J. Med. Chem. 49, 6638-41

Vrecl M, Drinovec L, Elling CE, Heding A (2006). Opsin oligomeriztion in a heterologous cell system. J. Recept. Signal Transduct. Res. 26, 505-26.

Holst B, Lang M, Brandt E, Bach A, Howard AD, Frimurer TM, Beck-Sickinger A and Schwartz TW (2006). Ghrelin receptor inverse agonists – identification of an active peptide core and its interaction epitopes on the receptor. Mol. Pharmacol.70, 936-46.

Nygaard R, Nielbo S, Schwartz TW and Poulsen FM (2006). The PP-fold Solution Structure of Human Polypeptide YY and Human PYY3-36 as Determined by NMR. Biochemistry 45, 8350-57.

Elling CE, Frimurer TM, Gerlach LO, Jørgensen R, Holst B and Schwartz TW (2006). Metal-site Engineering indicating a Global Toggle Switch activation mechanism for 7TM Receptors. J..Biol..Chem.281, 17337-46.

Ulven T, Little PB, Receveur J-M, Frimurer TM, Rist Ø, Nørregaard PK, Högberg T (2006). 6-Acylamino-2-amino-4-methylquinolines as Potent Melanin-Concentrating Hormone (MCH) Receptor 1 Antagonists. East and West libraries. Bioorg. Med. Chem. Let. 16, 1070-1075.

Mathiesen JM, Christopoulos A, Ulven T, Royer JF, Campillo M, Heinemann A, Pardo L, Kostenis E (2006). On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Mol. Pharmacol. 69, 1441-53.

Schwartz TW, Frimurer TM, Holst B, Rosenkilde MM and Elling CE (2006). Molecular Mechanism of 7TM Receptor Activation – a Global Toggle Switch Model. Annu. Rev. Pharmacol. Toxicol. 46, 481-519.

Holst B, Brandt E, Bach A, Heding A and Schwartz TW (2005). Non-peptide and Peptide Growth Hormone Secretagogues Act both as Agonists and as Positive or Negative Allosteric Modulators of Ghrelin Signaling. Mol..Endocrinol. 19, 2400-11.

Frimurer TM, Ulven T, Elling CE, Gerlach LO, Kostenis E, Högberg T (2005). A physicogenetic method to assign ligand-binding relationships between 7TM receptors. Bioorg. Med. Chem. Lett. 15, 3707-12.

Ulven T, Frimurer TM, Receveur JM, Little PB, Rist O, Nørregaard PK, Högberg T (2005). 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. J. Med. Chem.48,5684-97.

Mathiesen JM, Ulven T, Martini L, Gerlach LO, Heinemann A, Kostenis E (2005). Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. Mol. Pharmacol. 68, 393-402.

Kostenis E, Martini L, Ellis J, Waldhoer M, Heydorn A, Rosenkilde MM, Nørregaard PK, Jorgensen R, Whistler JL, Milligan G (2005). A highly conserved glycine within linker I and the extreme C terminus of G protein alpha subunits interact cooperatively in switching G protein-coupled receptor-to-effector specificity. J. Pharmacol. Exp. Ther. 313, 78-87.

Jorgensen R, Martini L, Schwartz TW, Elling CE (2005). Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype. Mol. Endocrinol. 19, 812-23.

Ulven T, Kostenis E (2005). Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J. Med. Chem. 48, 897-900.

Heydorn A, Ward RJ, Jorgensen R, Rosenkilde MM, Frimurer TM, Milligan G, Kostenis E (2004). Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction. Mol. Pharmacol.66, 250-9.

Receveur J-M; Bjurling E; Ulven T; Little PB; Nørregaard PK; Högberg T (2004). 4-Acylamino- and 4-Ureidobenzamides as Melanin-Concentrating Hormone (MCH) Receptor 1 Antagonists. Bioorg. Med. Chem. Lett., 14, 5075-5080.

Vrecl M, Jorgensen R, Pogacnik A, Heding A (2004). Development of a BRET2 Screening Assay Using Beta-Arrestin 2 Mutants J. Biomol. Screen. 9, 322-33.

Heding A (2004). Use of the BRET 7TM receptor/ß-arrestin assay in drug discovery and screening. Expert Rev. Mol. Diagn. 4, 403-11.

Holst B, Holliday N, Bach A, Elling CE, Cox H and Schwartz TW (2004). Common structural basis for constitutive activity in the ghrelin receptor family. J..Biol..Chem. 279, 53806-53817.

Gerlach LO, Jacobsen JS, Jensen KP, Rosenkilde MM, Skerlj RT, Ryder U, Bridger GJ and Schwartz TW (2003). Metal-ion enhanced binding of AMD3100 to Asp262 in the CXCR4 receptor. Biochemistry 42, 710-17.

Frimurer TM, Peters GH, Iversen LF, Andersen HS, Moller NP, Olsen OH (2003).
Ligand-induced conformational changes: improved predictions of ligand binding conformations and affinities. Biophys. J. 84, 2273-81.

Clavier S, Rist O, Hansen S, Gerlach LO, Högberg T, Bergman J (2003). Preparation and evaluation of sulfur-containing metal chelators. Org. Biomol. Chem. 1, 4248-53.

A. Heding, C.E. Elling and T.W. Schwartz (2002). Novel method for the study of receptor Ca++ signalling exemplified by the

NK1 receptor. J. of Receptor and Signal Transduction Research. 22, 241-252.