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1983 1
1985 1
1989 1
1992 1
1993 1
1996 1
1999 1
2000 1
2002 1
2004 2
2010 1
2011 5
2012 2
2013 3
2014 5
2015 6
2016 4
2017 1
2018 1
2019 5
2020 6
2021 2
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49 results
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Page 1
Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer.
Mirza MR, Monk BJ, Herrstedt J, Oza AM, Mahner S, Redondo A, Fabbro M, Ledermann JA, Lorusso D, Vergote I, Ben-Baruch NE, Marth C, Mądry R, Christensen RD, Berek JS, Dørum A, Tinker AV, du Bois A, González-Martín A, Follana P, Benigno B, Rosenberg P, Gilbert L, Rimel BJ, Buscema J, Balser JP, Agarwal S, Matulonis UA; ENGOT-OV16/NOVA Investigators. Mirza MR, et al. N Engl J Med. 2016 Dec 1;375(22):2154-2164. doi: 10.1056/NEJMoa1611310. Epub 2016 Oct 7. N Engl J Med. 2016. PMID: 27717299 Free article. Clinical Trial.
Ligand-Specific Allosteric Coupling Controls G-Protein-Coupled Receptor Signaling.
Holze J, Bermudez M, Pfeil EM, Kauk M, Bödefeld T, Irmen M, Matera C, Dallanoce C, De Amici M, Holzgrabe U, König GM, Tränkle C, Wolber G, Schrage R, Mohr K, Hoffmann C, Kostenis E, Bock A. Holze J, et al. ACS Pharmacol Transl Sci. 2020 Sep 2;3(5):859-867. doi: 10.1021/acsptsci.0c00069. eCollection 2020 Oct 9. ACS Pharmacol Transl Sci. 2020. PMID: 33073186 Free PMC article.
Allosteric coupling describes a reciprocal process whereby G-protein-coupled receptors (GPCRs) relay ligand-induced conformational changes from the extracellular binding pocket to the intracellular signaling surface. ...We demonstrate that stepwise shortening of their chem …
Allosteric coupling describes a reciprocal process whereby G-protein-coupled receptors (GPCRs) relay ligand-induced conformational ch …
Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay.
Zierau O, Kolodziejczyk A, Vollmer G, Machalz D, Wolber G, Thieme D, Keiler AM. Zierau O, et al. J Steroid Biochem Mol Biol. 2019 May;189:81-86. doi: 10.1016/j.jsbmb.2019.02.014. Epub 2019 Feb 27. J Steroid Biochem Mol Biol. 2019. PMID: 30825507
In the yeast androgen screen, the androgenic effects were lower than in the reporter gene assay in prostate carcinoma cells (e.g. for GSK-2881078, the EC(50) values were 4.44 10(-6)M in the yeast screen and 3.99 10(-9)M in the prostate cells respectively). ...
In the yeast androgen screen, the androgenic effects were lower than in the reporter gene assay in prostate carcinoma cells (e.g. for …
Strategies for the discovery of biased GPCR ligands.
Bermudez M, Nguyen TN, Omieczynski C, Wolber G. Bermudez M, et al. Drug Discov Today. 2019 Apr;24(4):1031-1037. doi: 10.1016/j.drudis.2019.02.010. Epub 2019 Mar 1. Drug Discov Today. 2019. PMID: 30831262 Review.
G-protein-coupled receptors (GPCRs) represent important drug targets with complex pharmacological characteristics. ...We show different approaches for biased ligand discovery in the example of G-protein-biased opioid analgesics and discuss possibilities to design bi
G-protein-coupled receptors (GPCRs) represent important drug targets with complex pharmacological characteristics. ...We show differe
High homogeneity of MMR deficiency in ovarian cancer.
Fraune C, Rosebrock J, Simon R, Hube-Magg C, Makrypidi-Fraune G, Kluth M, Büscheck F, Höflmayer D, Schmalfeldt B, Müller V, Wölber L, Witzel I, Paluchowski P, Wilke C, Heilenkötter U, von Leffern I, Clauditz TS, Wilczak W, Sauter G, Steurer S, Burandt E. Fraune C, et al. Gynecol Oncol. 2020 Mar;156(3):669-675. doi: 10.1016/j.ygyno.2019.12.031. Epub 2020 Jan 8. Gynecol Oncol. 2020. PMID: 31924330
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. Bock A, et al. J Biol Chem. 2016 Jul 29;291(31):16375-89. doi: 10.1074/jbc.M116.735431. Epub 2016 Jun 13. J Biol Chem. 2016. PMID: 27298318 Free PMC article.
G protein-coupled receptors constitute the largest family of membrane receptors and modulate almost every physiological process in humans. Binding of agonists to G protein-coupled receptors induces a shift from inactive to active receptor conformations. ...
G protein-coupled receptors constitute the largest family of membrane receptors and modulate almost every physiological process in hu
Structure versus function-The impact of computational methods on the discovery of specific GPCR-ligands.
Bermudez M, Wolber G. Bermudez M, et al. Bioorg Med Chem. 2015 Jul 15;23(14):3907-12. doi: 10.1016/j.bmc.2015.03.026. Epub 2015 Mar 14. Bioorg Med Chem. 2015. PMID: 25828056 Review.
The combination of experimental and in silico methods in the field of G protein coupled receptors (GPCRs) is indispensable. Despite recent groundbreaking achievements in GPCR crystallography, structural information for the vast majority of this physiologically important pr …
The combination of experimental and in silico methods in the field of G protein coupled receptors (GPCRs) is indispensable. Despite r …
Biased Ligands Differentially Shape the Conformation of the Extracellular Loop Region in 5-HT2B Receptors.
Denzinger K, Nguyen TN, Noonan T, Wolber G, Bermudez M. Denzinger K, et al. Int J Mol Sci. 2020 Dec 20;21(24):9728. doi: 10.3390/ijms21249728. Int J Mol Sci. 2020. PMID: 33419260 Free PMC article.
G protein-coupled receptors are linked to various intracellular transducers, each pathway associated with different physiological effects. ...
G protein-coupled receptors are linked to various intracellular transducers, each pathway associated with different physiological eff
Treatment response lowers tumor symptom burden in recurrent and/or metastatic head and neck cancer.
Hecht M, Hahn D, Wolber P, Hautmann MG, Reichert D, Weniger S, Belka C, Bergmann T, Göhler T, Welslau M, Große-Thie C, Guntinas-Lichius O, von der Grün J, Balermpas P, Orlowski K, Messinger D, Stenzel KG, Fietkau R. Hecht M, et al. BMC Cancer. 2020 Sep 29;20(1):933. doi: 10.1186/s12885-020-07440-w. BMC Cancer. 2020. PMID: 32993574 Free PMC article. Clinical Trial.
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