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A promising chemical series of positive allosteric modulators of the μ-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects.
Pryce KD, Kang HJ, Sakloth F, Liu Y, Khan S, Toth K, Kapoor A, Nicolais A, Che T, Qin L, Bertherat F, Kaniskan HÜ, Jin J, Cameron MD, Roth BL, Zachariou V, Filizola M. Pryce KD, et al. Among authors: roth bl. Neuropharmacology. 2021 Sep 1;195:108673. doi: 10.1016/j.neuropharm.2021.108673. Epub 2021 Jun 18. Neuropharmacology. 2021. PMID: 34153316 Free PMC article.
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. Kaniskan HÜ, et al. Among authors: roth bl. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27. Angew Chem Int Ed Engl. 2015. PMID: 25728001 Free PMC article.
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65.
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. Huang XP, et al. Among authors: roth bl. Nature. 2015 Nov 26;527(7579):477-83. doi: 10.1038/nature15699. Epub 2015 Nov 9. Nature. 2015. PMID: 26550826 Free PMC article.
Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY. Etukala JR, et al. Among authors: roth bl. Bioorg Med Chem. 2016 Aug 15;24(16):3671-9. doi: 10.1016/j.bmc.2016.06.011. Epub 2016 Jun 4. Bioorg Med Chem. 2016. PMID: 27364609 Free PMC article.
Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists.
Chen X, McCorvy JD, Fischer MG, Butler KV, Shen Y, Roth BL, Jin J. Chen X, et al. Among authors: roth bl. J Med Chem. 2016 Dec 8;59(23):10601-10618. doi: 10.1021/acs.jmedchem.6b01208. Epub 2016 Nov 16. J Med Chem. 2016. PMID: 27805392 Free PMC article.
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL. Lansu K, et al. Among authors: roth bl. Nat Chem Biol. 2017 May;13(5):529-536. doi: 10.1038/nchembio.2334. Epub 2017 Mar 13. Nat Chem Biol. 2017. PMID: 28288109 Free PMC article.
546 results