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Scalable Technologies For Illuminating The Druggable Gpcr-ome

  • Bryan Roth, M.D., Ph.D.
    Michael Hooker Distinguished Professor of Protein Therapeutics and Translational Proteomics
    Department of Pharmacology
    School of Medicine
    University of North Carolina, Chapel Hill

  • Brian Shoichet, Ph.D.
    Professor Department of Pharmaceutical Chemistry
    University of California, San Francisco


Collaborative work by Dr. Bryan Roth and Dr. Brian Shoichet focuses on illuminating the druggable GPCR-ome by two-pronged approach of empirical screening of drugs followed by computational screening against modeled structures of the GPCR to produced optimized lead compounds. Their work has led to discovery of molecule “ogerin” binding previously orphaned, GPR68.


Highlighted Recent Publications

  • Kroeze WK, Sassano MF, Huang XP, Lansu K, McCorvy JD, Giguère PM, Sciaky N, Roth BL. PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome. Nat Struct Mol Biol. 2015 Apr 20. doi: 10.1038/nsmb.3014. [Epub ahead of print], PubMed Abstract:

  • Cero C, Vostrikov VV, Verardi R, Severini C, Gopinath T, Braun PD, Sassano MF, Gurney A, Roth BL, Vulchanova L, Possenti R, Veglia G, Bartolomucci A. The TLQP-21 peptide activates the G-protein-coupled receptor C3aR1 via a folding-upon-binding mechanism. Structure. 2014 Dec 2;22(12):1744-53. doi: 10.1016/j.str.2014.10.001. Epub 2014 Nov 13., PubMed Abstract:

  • Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL. Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65. Nature. 2015 Nov 26;527(7579):477-83. doi: 10.1038/nature15699. Epub 2015 Nov 9.PubMed Abstract: http://www.ncbi.nlm.nih .gov

  • Roth BLKroeze WK. Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily.  J Biol Chem. 2015 Aug 7;290(32):19471-7. doi: 10.1074/jbc.R115.654764. Epub 2015 Jun 22. Review. PubMed Abstract: http://www.ncbi.nlm
    /pubmed/ 26100629

Genes Under investigation, Bryan Roth, M.D.,Ph.D.

Submitted 6/20/2016


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