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Agonists and Antagonists of Protease-Activated Receptor 2 Discovered within a DNA-Encoded Chemical Library Using Mutational Stabilization of the Target.
Brown DG, Brown GA, Centrella P, Certel K, Cooke RM, Cuozzo JW, Dekker N, Dumelin CE, Ferguson A, Fiez-Vandal C, Geschwindner S, Guié MA, Habeshian S, Keefe AD, Schlenker O, Sigel EA, Snijder A, Soutter HT, Sundström L, Troast DM, Wiggin G, Zhang J, Zhang Y, Clark MA. Brown DG, et al. SLAS Discov. 2018 Jun;23(5):429-436. doi: 10.1177/2472555217749847. Epub 2018 Jan 9. SLAS Discov. 2018. PMID: 29316408 Free article.
Functional impact of intramolecular cleavage and dissociation of adhesion G protein-coupled receptor GPR133 (ADGRD1) on canonical signaling.
Frenster JD, Stephan G, Ravn-Boess N, Bready D, Wilcox J, Kieslich B, Wilde C, Sträter N, Wiggin GR, Liebscher I, Schöneberg T, Placantonakis DG. Frenster JD, et al. Among authors: wiggin gr. J Biol Chem. 2021 Jan-Jun;296:100798. doi: 10.1016/j.jbc.2021.100798. Epub 2021 May 20. J Biol Chem. 2021. PMID: 34022221 Free PMC article.
Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.
Doré AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH. Doré AS, et al. Among authors: wiggin gr. Nature. 2014 Jul 31;511(7511):557-62. doi: 10.1038/nature13396. Epub 2014 Jul 6. Nature. 2014. PMID: 25042998
Structural insight into allosteric modulation of protease-activated receptor 2.
Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N. Cheng RKY, et al. Nature. 2017 May 4;545(7652):112-115. doi: 10.1038/nature22309. Epub 2017 Apr 26. Nature. 2017. PMID: 28445455
Expression profiling of the adhesion G protein-coupled receptor GPR133 (ADGRD1) in glioma subtypes.
Frenster JD, Kader M, Kamen S, Sun J, Chiriboga L, Serrano J, Bready D, Golub D, Ravn-Boess N, Stephan G, Chi AS, Kurz SC, Jain R, Park CY, Fenyo D, Liebscher I, Schöneberg T, Wiggin G, Newman R, Barnes M, Dickson JK, MacNeil DJ, Huang X, Shohdy N, Snuderl M, Zagzag D, Placantonakis DG. Frenster JD, et al. Neurooncol Adv. 2020 Apr 28;2(1):vdaa053. doi: 10.1093/noajnl/vdaa053. eCollection 2020 Jan-Dec. Neurooncol Adv. 2020. PMID: 32642706 Free PMC article.
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. Christopher JA, et al. Among authors: wiggin gr. J Med Chem. 2015 Aug 27;58(16):6653-64. doi: 10.1021/acs.jmedchem.5b00892. Epub 2015 Aug 12. J Med Chem. 2015. PMID: 26225459
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