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Items: 25

1.

Identifying Functional Hotspot Residues for Biased Ligand Design in G-protein-coupled Receptors.

Nivedha A, Tautermann C, Bhattacharya S, Lee S, Casarosa P, Kollak I, Kiechle T, Vaidehi N.

Mol Pharmacol. 2018 Jan 24. pii: mol.117.110395. doi: 10.1124/mol.117.110395. [Epub ahead of print]

2.

Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.

Tautermann CS, Kiechle T, Seeliger D, Diehl S, Wex E, Banholzer R, Gantner F, Pieper MP, Casarosa P.

J Med Chem. 2013 Nov 14;56(21):8746-56. doi: 10.1021/jm401219y. Epub 2013 Oct 25.

PMID:
24088171
3.

β₂ long-acting and anticholinergic drugs control TGF-β1-mediated neutrophilic inflammation in COPD.

Profita M, Bonanno A, Montalbano AM, Albano GD, Riccobono L, Siena L, Ferraro M, Casarosa P, Pieper MP, Gjomarkaj M.

Biochim Biophys Acta. 2012 Jul;1822(7):1079-89. doi: 10.1016/j.bbadis.2012.03.002. Epub 2012 Mar 13.

4.

In vitro anticholinergic drugs affect CD8+ peripheral blood T-cells apoptosis in COPD.

Profita M, Riccobono L, Montalbano AM, Bonanno A, Ferraro M, Albano GD, Gerbino S, Casarosa P, Pieper MP, Gjomarkaj M.

Immunobiology. 2012 Mar;217(3):345-53. doi: 10.1016/j.imbio.2011.07.013. Epub 2011 Aug 3.

PMID:
21855166
5.

Cigarette smoke extract activates human bronchial epithelial cells affecting non-neuronal cholinergic system signalling in vitro.

Profita M, Bonanno A, Montalbano AM, Ferraro M, Siena L, Bruno A, Girbino S, Albano GD, Casarosa P, Pieper MP, Gjomarkaj M.

Life Sci. 2011 Jul 4;89(1-2):36-43. doi: 10.1016/j.lfs.2011.04.025. Epub 2011 May 18.

PMID:
21620875
6.

Functional and biochemical rationales for the 24-hour-long duration of action of olodaterol.

Casarosa P, Kollak I, Kiechle T, Ostermann A, Schnapp A, Kiesling R, Pieper M, Sieger P, Gantner F.

J Pharmacol Exp Ther. 2011 Jun;337(3):600-9. doi: 10.1124/jpet.111.179259. Epub 2011 Feb 28.

7.

Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.

Rasmussen SG, Choi HJ, Fung JJ, Pardon E, Casarosa P, Chae PS, Devree BT, Rosenbaum DM, Thian FS, Kobilka TS, Schnapp A, Konetzki I, Sunahara RK, Gellman SH, Pautsch A, Steyaert J, Weis WI, Kobilka BK.

Nature. 2011 Jan 13;469(7329):175-80. doi: 10.1038/nature09648.

8.

Differential inverse agonism at the human muscarinic M₃ receptor.

Casarosa P, Kiechle T, Bakker RA.

Methods Enzymol. 2010;485:81-101. doi: 10.1016/B978-0-12-381296-4.00005-1.

PMID:
21050912
9.

Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models.

Bouyssou T, Casarosa P, Naline E, Pestel S, Konetzki I, Devillier P, Schnapp A.

J Pharmacol Exp Ther. 2010 Jul;334(1):53-62. doi: 10.1124/jpet.110.167007. Epub 2010 Apr 6. Erratum in: J Pharmacol Exp Ther. 2013 Jul;346(1):161.

10.

The constitutive activity of the human muscarinic M3 receptor unmasks differences in the pharmacology of anticholinergics.

Casarosa P, Kiechle T, Sieger P, Pieper M, Gantner F.

J Pharmacol Exp Ther. 2010 Apr;333(1):201-9. doi: 10.1124/jpet.109.163188. Epub 2009 Dec 24.

11.

Significance of N-terminal proteolysis of CCL14a to activity on the chemokine receptors CCR1 and CCR5 and the human cytomegalovirus-encoded chemokine receptor US28.

Richter R, Casarosa P, Ständker L, Münch J, Springael JY, Nijmeijer S, Forssmann WG, Vischer HF, Vakili J, Detheux M, Parmentier M, Leurs R, Smit MJ.

J Immunol. 2009 Jul 15;183(2):1229-37. doi: 10.4049/jimmunol.0802145. Epub 2009 Jun 24.

12.

Preclinical evaluation of long-acting muscarinic antagonists: comparison of tiotropium and investigational drugs.

Casarosa P, Bouyssou T, Germeyer S, Schnapp A, Gantner F, Pieper M.

J Pharmacol Exp Ther. 2009 Aug;330(2):660-8. doi: 10.1124/jpet.109.152470. Epub 2009 May 28.

13.

Smoke, choline acetyltransferase, muscarinic receptors, and fibroblast proliferation in chronic obstructive pulmonary disease.

Profita M, Bonanno A, Siena L, Bruno A, Ferraro M, Montalbano AM, Albano GD, Riccobono L, Casarosa P, Pieper MP, Gjomarkaj M.

J Pharmacol Exp Ther. 2009 May;329(2):753-63. doi: 10.1124/jpet.108.145888. Epub 2009 Feb 3.

14.

Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.

Hulshof JW, Casarosa P, Menge WM, Kuusisto LM, van der Goot H, Smit MJ, de Esch IJ, Leurs R.

J Med Chem. 2005 Oct 6;48(20):6461-71.

PMID:
16190772
15.

The human cytomegalovirus-encoded chemokine receptor US28 induces caspase-dependent apoptosis.

Pleskoff O, Casarosa P, Verneuil L, Ainoun F, Beisser P, Smit M, Leurs R, Schneider P, Michelson S, Ameisen JC.

FEBS J. 2005 Aug;272(16):4163-77.

16.

CC and CX3C chemokines differentially interact with the N terminus of the human cytomegalovirus-encoded US28 receptor.

Casarosa P, Waldhoer M, LiWang PJ, Vischer HF, Kledal T, Timmerman H, Schwartz TW, Smit MJ, Leurs R.

J Biol Chem. 2005 Feb 4;280(5):3275-85. Epub 2004 Nov 16.

17.

Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors.

Bakker RA, Casarosa P, Timmerman H, Smit MJ, Leurs R.

J Biol Chem. 2004 Feb 13;279(7):5152-61. Epub 2003 Nov 10.

18.

Constitutive signaling of the human cytomegalovirus-encoded receptor UL33 differs from that of its rat cytomegalovirus homolog R33 by promiscuous activation of G proteins of the Gq, Gi, and Gs classes.

Casarosa P, Gruijthuijsen YK, Michel D, Beisser PS, Holl J, Fitzsimons CP, Verzijl D, Bruggeman CA, Mertens T, Leurs R, Vink C, Smit MJ.

J Biol Chem. 2003 Dec 12;278(50):50010-23. Epub 2003 Sep 30.

19.

Human cytomegalovirus chemokine receptor US28-induced smooth muscle cell migration is mediated by focal adhesion kinase and Src.

Streblow DN, Vomaske J, Smith P, Melnychuk R, Hall L, Pancheva D, Smit M, Casarosa P, Schlaepfer DD, Nelson JA.

J Biol Chem. 2003 Dec 12;278(50):50456-65. Epub 2003 Sep 22.

20.

Virally encoded G protein-coupled receptors: targets for potentially innovative anti-viral drug development.

Smit MJ, Vink C, Verzijl D, Casarosa P, Bruggeman CA, Leurs R.

Curr Drug Targets. 2003 Jul;4(5):431-41. Review.

PMID:
12816350
21.

The carboxyl terminus of human cytomegalovirus-encoded 7 transmembrane receptor US28 camouflages agonism by mediating constitutive endocytosis.

Waldhoer M, Casarosa P, Rosenkilde MM, Smit MJ, Leurs R, Whistler JL, Schwartz TW.

J Biol Chem. 2003 May 23;278(21):19473-82. Epub 2003 Mar 18.

22.

Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor.

Casarosa P, Menge WM, Minisini R, Otto C, van Heteren J, Jongejan A, Timmerman H, Moepps B, Kirchhoff F, Mertens T, Smit MJ, Leurs R.

J Biol Chem. 2003 Feb 14;278(7):5172-8. Epub 2002 Nov 26.

24.

The rat cytomegalovirus R33-encoded G protein-coupled receptor signals in a constitutive fashion.

Gruijthuijsen YK, Casarosa P, Kaptein SJ, Broers JL, Leurs R, Bruggeman CA, Smit MJ, Vink C.

J Virol. 2002 Feb;76(3):1328-38.

25.

Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28.

Casarosa P, Bakker RA, Verzijl D, Navis M, Timmerman H, Leurs R, Smit MJ.

J Biol Chem. 2001 Jan 12;276(2):1133-7.

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