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Items: 1 to 20 of 42

1.

Novel BQCA- and TBPB-Derived M1 Receptor Hybrid Ligands: Orthosteric Carbachol Differentially Regulates Partial Agonism.

Schramm S, Agnetta L, Bermudez M, Gerwe H, Irmen M, Holze J, Littmann T, Wolber G, Tränkle C, Decker M.

ChemMedChem. 2019 Jul 17;14(14):1349-1358. doi: 10.1002/cmdc.201900283. Epub 2019 Jul 3.

PMID:
31166078
2.

The GPRC5A frameshift variant c.183del is not associated with increased breast cancer risk in BRCA1 mutation carriers.

Klaschik K, Hauke J, Neidhardt G, Tränkle C, Surowy HM, Heilmann-Heimbach S, Rappl G, Mangold E, Arnold N, Niederacher D, Sutter C, Burwinkel B, Engel C, Wappenschmidt B, Meindl A, Ernst C, Weber-Lassalle K, Weber-Lassalle N, Schmidt S, Borde J, Schmutzler RK, Hahnen E, Pohl-Rescigno E.

Int J Cancer. 2019 Apr 1;144(7):1761-1763. doi: 10.1002/ijc.32016. Epub 2019 Jan 6. No abstract available.

PMID:
30474284
3.

Characterization of methanthelinium binding and function at human M1-M5 muscarinic acetylcholine receptors.

Irmen M, Holze J, Bödefeld T, Tränkle C.

Naunyn Schmiedebergs Arch Pharmacol. 2018 Oct;391(10):1037-1052. doi: 10.1007/s00210-018-1525-1. Epub 2018 Jun 24.

PMID:
29938305
4.

Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M1 and M2.

Messerer R, Dallanoce C, Matera C, Wehle S, Flammini L, Chirinda B, Bock A, Irmen M, Tränkle C, Barocelli E, Decker M, Sotriffer C, De Amici M, Holzgrabe U.

Medchemcomm. 2017 Apr 27;8(6):1346-1359. doi: 10.1039/c7md00149e. eCollection 2017 Jun 1.

5.

M2 Subtype preferring dibenzodiazepinone-type muscarinic receptor ligands: Effect of chemical homo-dimerization on orthosteric (and allosteric?) binding.

Keller M, Tränkle C, She X, Pegoli A, Bernhardt G, Buschauer A, Read RW.

Bioorg Med Chem. 2015 Jul 15;23(14):3970-90. doi: 10.1016/j.bmc.2015.01.015. Epub 2015 Jan 14.

PMID:
25650309
6.

Pilot the pulse: controlling the multiplicity of receptor dynamics.

Bock A, Kostenis E, Tränkle C, Lohse MJ, Mohr K.

Trends Pharmacol Sci. 2014 Dec;35(12):630-8. doi: 10.1016/j.tips.2014.10.002. Epub 2014 Oct 31.

PMID:
25455830
7.

Beta and gamma carboline derivatives as potential anti-Alzheimer agents: A comparison.

Otto R, Penzis R, Gaube F, Winckler T, Appenroth D, Fleck C, Tränkle C, Lehmann J, Enzensperger C.

Eur J Med Chem. 2014 Nov 24;87:63-70. doi: 10.1016/j.ejmech.2014.09.048. Epub 2014 Sep 16.

PMID:
25240096
8.

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
9.

Dynamic ligand binding dictates partial agonism at a G protein-coupled receptor.

Bock A, Chirinda B, Krebs F, Messerer R, Bätz J, Muth M, Dallanoce C, Klingenthal D, Tränkle C, Hoffmann C, De Amici M, Holzgrabe U, Kostenis E, Mohr K.

Nat Chem Biol. 2014 Jan;10(1):18-20. doi: 10.1038/nchembio.1384. Epub 2013 Nov 10.

PMID:
24212135
10.

A muscarinic view on Gq.

Mohr K, Tränkle C.

Naunyn Schmiedebergs Arch Pharmacol. 2013 Nov;386(11):935-6. doi: 10.1007/s00210-013-0895-7. No abstract available.

PMID:
23779215
11.

Molecular alliance-from orthosteric and allosteric ligands to dualsteric/bitopic agonists at G protein coupled receptors.

Mohr K, Schmitz J, Schrage R, Tränkle C, Holzgrabe U.

Angew Chem Int Ed Engl. 2013 Jan 7;52(2):508-16. doi: 10.1002/anie.201205315. Epub 2012 Dec 6. Review.

PMID:
23225228
12.

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling.

Bock A, Merten N, Schrage R, Dallanoce C, Bätz J, Klöckner J, Schmitz J, Matera C, Simon K, Kebig A, Peters L, Müller A, Schrobang-Ley J, Tränkle C, Hoffmann C, De Amici M, Holzgrabe U, Kostenis E, Mohr K.

Nat Commun. 2012;3:1044. doi: 10.1038/ncomms2028.

13.

A hydrazide linker strategy for heterobivalent compounds as ortho- and allosteric ligands of acetylcholine-binding proteins.

Elsinghorst PW, Härtig W, Gündisch D, Mohr K, Tränkle C, Gütschow M.

Curr Top Med Chem. 2011 Nov;11(22):2731-48. Review.

PMID:
22039876
14.

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.

15.

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity.

Antony J, Kellershohn K, Mohr-Andrä M, Kebig A, Prilla S, Muth M, Heller E, Disingrini T, Dallanoce C, Bertoni S, Schrobang J, Tränkle C, Kostenis E, Christopoulos A, Höltje HD, Barocelli E, De Amici M, Holzgrabe U, Mohr K.

FASEB J. 2009 Feb;23(2):442-50. doi: 10.1096/fj.08-114751. Epub 2008 Oct 8.

PMID:
18842964
16.

First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.

Elsinghorst PW, Cieslik JS, Mohr K, Tränkle C, Gütschow M.

J Med Chem. 2007 Nov 15;50(23):5685-95. Epub 2007 Oct 18.

PMID:
17944454
17.

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.

18.

Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors.

Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E.

Naunyn Schmiedebergs Arch Pharmacol. 2006 Feb;372(5):354-61. Epub 2006 Feb 18.

PMID:
16489449
19.

Allosteric site in M2 acetylcholine receptors: evidence for a major conformational change upon binding of an orthosteric agonist instead of an antagonist.

Grossmüller M, Antony J, Tränkle C, Holzgrabe U, Mohr K.

Naunyn Schmiedebergs Arch Pharmacol. 2006 Jan;372(4):267-76. Epub 2005 Dec 16.

PMID:
16362429
20.

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

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