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Items: 1 to 20 of 110

1.

Identification of overlapping but differential binding sites for the high-affinity CXCR3 antagonists NBI-74330 and VUF11211.

Scholten DJ, Roumen L, Wijtmans M, Verkade-Vreeker MC, Custers H, Lai M, de Hooge D, Canals M, de Esch IJ, Smit MJ, de Graaf C, Leurs R.

Mol Pharmacol. 2014 Jan;85(1):116-26. doi: 10.1124/mol.113.088633. Epub 2013 Oct 30.

2.

Pharmacological characterization of [3H]VUF11211, a novel radiolabeled small-molecule inverse agonist for the chemokine receptor CXCR3.

Scholten DJ, Wijtmans M, van Senten JR, Custers H, Stunnenberg A, de Esch IJ, Smit MJ, Leurs R.

Mol Pharmacol. 2015 Apr;87(4):639-48. doi: 10.1124/mol.114.095265. Epub 2015 Jan 9.

3.

Synthesis and application of the first radioligand targeting the allosteric binding pocket of chemokine receptor CXCR3.

Bernat V, Heinrich MR, Baumeister P, Buschauer A, Tschammer N.

ChemMedChem. 2012 Aug;7(8):1481-9. doi: 10.1002/cmdc.201200184. Epub 2012 Jun 11.

PMID:
22689503
4.

Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist.

Heise CE, Pahuja A, Hudson SC, Mistry MS, Putnam AL, Gross MM, Gottlieb PA, Wade WS, Kiankarimi M, Schwarz D, Crowe P, Zlotnik A, Alleva DG.

J Pharmacol Exp Ther. 2005 Jun;313(3):1263-71. Epub 2005 Mar 10.

5.

Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors.

Verzijl D, Storelli S, Scholten DJ, Bosch L, Reinhart TA, Streblow DN, Tensen CP, Fitzsimons CP, Zaman GJ, Pease JE, de Esch IJ, Smit MJ, Leurs R.

J Pharmacol Exp Ther. 2008 May;325(2):544-55. doi: 10.1124/jpet.107.134783. Epub 2008 Feb 12.

6.

Development of Photoactivatable Allosteric Modulators for the Chemokine Receptor CXCR3.

Admas TH, Bernat V, Heinrich MR, Tschammer N.

ChemMedChem. 2016 Mar 17;11(6):575-84. doi: 10.1002/cmdc.201500573. Epub 2016 Feb 16.

PMID:
26880380
7.

Analysis of the pharmacokinetic/pharmacodynamic relationship of a small molecule CXCR3 antagonist, NBI-74330, using a murine CXCR3 internalization assay.

Jopling LA, Watt GF, Fisher S, Birch H, Coggon S, Christie MI.

Br J Pharmacol. 2007 Dec;152(8):1260-71. Epub 2007 Nov 5.

8.

Pharmacological characterization of a small-molecule agonist for the chemokine receptor CXCR3.

Scholten DJ, Canals M, Wijtmans M, de Munnik S, Nguyen P, Verzijl D, de Esch IJ, Vischer HF, Smit MJ, Leurs R.

Br J Pharmacol. 2012 Jun;166(3):898-911. doi: 10.1111/j.1476-5381.2011.01648.x.

9.

Small molecule chemokine mimetics suggest a molecular basis for the observation that CXCL10 and CXCL11 are allosteric ligands of CXCR3.

Nedjai B, Li H, Stroke IL, Wise EL, Webb ML, Merritt JR, Henderson I, Klon AE, Cole AG, Horuk R, Vaidehi N, Pease JE.

Br J Pharmacol. 2012 Jun;166(3):912-23. doi: 10.1111/j.1476-5381.2011.01660.x.

10.

Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists.

Storelli S, Verzijl D, Al-Badie J, Elders N, Bosch L, Timmerman H, Smit MJ, De Esch IJ, Leurs R.

Arch Pharm (Weinheim). 2007 Jun;340(6):281-91.

PMID:
17562560
11.

Modelling of the membrane receptor CXCR3 and its complexes with CXCL9, CXCL10 and CXCL11 chemokines: putative target for new drug design.

Trotta T, Costantini S, Colonna G.

Mol Immunol. 2009 Dec;47(2-3):332-9. doi: 10.1016/j.molimm.2009.09.013. Epub 2009 Oct 1.

PMID:
19800124
14.

Molecular interactions of CCR5 with major classes of small-molecule anti-HIV CCR5 antagonists.

Kondru R, Zhang J, Ji C, Mirzadegan T, Rotstein D, Sankuratri S, Dioszegi M.

Mol Pharmacol. 2008 Mar;73(3):789-800. Epub 2007 Dec 20.

15.

Label-free impedance responses of endogenous and synthetic chemokine receptor CXCR3 agonists correlate with Gi-protein pathway activation.

Watts AO, Scholten DJ, Heitman LH, Vischer HF, Leurs R.

Biochem Biophys Res Commun. 2012 Mar 9;419(2):412-8. doi: 10.1016/j.bbrc.2012.02.036. Epub 2012 Feb 13.

PMID:
22349504
16.

Ligand-biased and probe-dependent modulation of chemokine receptor CXCR3 signaling by negative allosteric modulators.

Bernat V, Brox R, Heinrich MR, Auberson YP, Tschammer N.

ChemMedChem. 2015 Mar;10(3):566-74. doi: 10.1002/cmdc.201402507. Epub 2015 Feb 5.

PMID:
25655398
17.

Molecular mechanisms of biased and probe-dependent signaling at CXCR3 induced by negative allosteric modulators.

Brox R, Milanos L, Saleh N, Baumeister P, Buschauer A, Hofmann D, Heinrich MR, Clark T, Tschammer N.

Mol Pharmacol. 2018 Jan 17. pii: mol.117.110296. doi: 10.1124/mol.117.110296. [Epub ahead of print]

18.

The N-terminal region of CXCL11 as structural template for CXCR3 molecular recognition: synthesis, conformational analysis, and binding studies.

Palladino P, Portella L, Colonna G, Raucci R, Saviano G, Rossi F, Napolitano M, Scala S, Castello G, Costantini S.

Chem Biol Drug Des. 2012 Aug;80(2):254-65. doi: 10.1111/j.1747-0285.2012.01397.x. Epub 2012 May 23.

PMID:
22531000
19.

Structure-function relationship between the human chemokine receptor CXCR3 and its ligands.

Clark-Lewis I, Mattioli I, Gong JH, Loetscher P.

J Biol Chem. 2003 Jan 3;278(1):289-95. Epub 2002 Nov 1.

20.

Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.

Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R.

J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. doi: 10.1124/jpet.111.179531. Epub 2011 Apr 1.

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