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Items: 1 to 20 of 104

1.

A New Molecular Mechanism To Engineer Protean Agonism at a G Protein-Coupled Receptor.

De Min A, Matera C, Bock A, Holze J, Kloeckner J, Muth M, Traenkle C, De Amici M, Kenakin T, Holzgrabe U, Dallanoce C, Kostenis E, Mohr K, Schrage R.

Mol Pharmacol. 2017 Apr;91(4):348-356. doi: 10.1124/mol.116.107276. Epub 2017 Feb 6.

PMID:
28167741
2.

Ligand Binding Ensembles Determine Graded Agonist Efficacies at a G Protein-coupled Receptor.

Bock A, Bermudez M, Krebs F, Matera C, Chirinda B, Sydow D, Dallanoce C, Holzgrabe U, De Amici M, Lohse MJ, Wolber G, Mohr K.

J Biol Chem. 2016 Jul 29;291(31):16375-89. doi: 10.1074/jbc.M116.735431. Epub 2016 Jun 13.

3.

Engineered Context-Sensitive Agonism: Tissue-Selective Drug Signaling through a G Protein-Coupled Receptor.

Seemann WK, Wenzel D, Schrage R, Etscheid J, Bödefeld T, Bartol A, Warnken M, Sasse P, Klöckner J, Holzgrabe U, DeAmici M, Schlicker E, Racké K, Kostenis E, Meyer R, Fleischmann BK, Mohr K.

J Pharmacol Exp Ther. 2017 Feb;360(2):289-299. doi: 10.1124/jpet.116.237149. Epub 2016 Nov 15.

PMID:
28082514
4.

Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites.

Schober DA, Croy CH, Xiao H, Christopoulos A, Felder CC.

Mol Pharmacol. 2014 Jul;86(1):116-23. doi: 10.1124/mol.114.091785. Epub 2014 May 7.

PMID:
24807966
5.

Allosteric modulation in monomers and oligomers of a G protein-coupled receptor.

Shivnaraine RV, Kelly B, Sankar KS, Redka DS, Han YR, Huang F, Elmslie G, Pinto D, Li Y, Rocheleau JV, Gradinaru CC, Ellis J, Wells JW.

Elife. 2016 May 6;5. pii: e11685. doi: 10.7554/eLife.11685.

6.

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects.

Valant C, Felder CC, Sexton PM, Christopoulos A.

Mol Pharmacol. 2012 Jan;81(1):41-52. doi: 10.1124/mol.111.074872. Epub 2011 Oct 11.

PMID:
21989256
7.

Rational design of dualsteric GPCR ligands: quests and promise.

Mohr K, Tränkle C, Kostenis E, Barocelli E, De Amici M, Holzgrabe U.

Br J Pharmacol. 2010 Mar;159(5):997-1008. doi: 10.1111/j.1476-5381.2009.00601.x. Epub 2010 Feb 5. Review.

8.

Allosteric small molecules unveil a role of an extracellular E2/transmembrane helix 7 junction for G protein-coupled receptor activation.

Jäger D, Schmalenbach C, Prilla S, Schrobang J, Kebig A, Sennwitz M, Heller E, Tränkle C, Holzgrabe U, Höltje HD, Mohr K.

J Biol Chem. 2007 Nov 30;282(48):34968-76. Epub 2007 Sep 21.

9.

Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.

Schmitz J, van der Mey D, Bermudez M, Klöckner J, Schrage R, Kostenis E, Tränkle C, Wolber G, Mohr K, Holzgrabe U.

J Med Chem. 2014 Aug 14;57(15):6739-50. doi: 10.1021/jm500790x. Epub 2014 Aug 4.

PMID:
25051097
10.

New insight into active muscarinic receptors with the novel radioagonist [³H]iperoxo.

Schrage R, Holze J, Klöckner J, Balkow A, Klause AS, Schmitz AL, De Amici M, Kostenis E, Tränkle C, Holzgrabe U, Mohr K.

Biochem Pharmacol. 2014 Aug 1;90(3):307-19. doi: 10.1016/j.bcp.2014.05.012. Epub 2014 May 23.

PMID:
24863257
11.

Atypical muscarinic allosteric modulation: cooperativity between modulators and their atypical binding topology in muscarinic M2 and M2/M5 chimeric receptors.

Tränkle C, Dittmann A, Schulz U, Weyand O, Buller S, Jöhren K, Heller E, Birdsall NJ, Holzgrabe U, Ellis J, Höltje HD, Mohr K.

Mol Pharmacol. 2005 Dec;68(6):1597-610. Epub 2005 Sep 12.

PMID:
16157694
12.

When simple agonism is not enough: emerging modalities of GPCR ligands.

Smith NJ, Bennett KA, Milligan G.

Mol Cell Endocrinol. 2011 Jan 15;331(2):241-7. doi: 10.1016/j.mce.2010.07.009. Epub 2010 Jul 21. Review.

PMID:
20654693
13.

Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors.

Croy CH, Schober DA, Xiao H, Quets A, Christopoulos A, Felder CC.

Mol Pharmacol. 2014 Jul;86(1):106-15. doi: 10.1124/mol.114.091751. Epub 2014 May 7.

PMID:
24807965
14.

A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor.

Steinfeld T, Mammen M, Smith JA, Wilson RD, Jasper JR.

Mol Pharmacol. 2007 Aug;72(2):291-302. Epub 2007 May 3.

PMID:
17478612
15.

Discovery and characterization of orthosteric and allosteric muscarinic M2 acetylcholine receptor ligands by affinity selection-mass spectrometry.

Whitehurst CE, Nazef N, Annis DA, Hou Y, Murphy DM, Spacciapoli P, Yao Z, Ziebell MR, Cheng CC, Shipps GW Jr, Felsch JS, Lau D, Nash HM.

J Biomol Screen. 2006 Mar;11(2):194-207. Epub 2006 Feb 20.

PMID:
16490772
16.

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor.

Miao Y, Goldfeld DA, Moo EV, Sexton PM, Christopoulos A, McCammon JA, Valant C.

Proc Natl Acad Sci U S A. 2016 Sep 20;113(38):E5675-84. doi: 10.1073/pnas.1612353113. Epub 2016 Sep 6.

17.

Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor.

Nelson CP, Nahorski SR, Challiss RA.

J Pharmacol Exp Ther. 2006 Jan;316(1):279-88. Epub 2005 Sep 27.

PMID:
16188951
18.

Dualsteric GPCR targeting and functional selectivity: the paradigmatic M(2) muscarinic acetylcholine receptor.

Bock A, Mohr K.

Drug Discov Today Technol. 2013 Summer;10(2):e245-52. doi: 10.1016/j.ddtec.2012.12.003. Review.

PMID:
24050275
19.

Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors.

May LT, Avlani VA, Langmead CJ, Herdon HJ, Wood MD, Sexton PM, Christopoulos A.

Mol Pharmacol. 2007 Aug;72(2):463-76. Epub 2007 May 24.

PMID:
17525129
20.

An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators.

Kebig A, Kostenis E, Mohr K, Mohr-Andrä M.

J Recept Signal Transduct Res. 2009;29(3-4):140-5. doi: 10.1080/10799890903047437.

PMID:
19586284

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