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Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.
Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J. Frankowski KJ, et al. Among authors: bohn lm. ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. doi: 10.1021/cn200128x. Epub 2012 Jan 20. ACS Chem Neurosci. 2012. PMID: 22737280 Free PMC article.
Development of functionally selective, small molecule agonists at kappa opioid receptors.
Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl E, Schmid CL, Hodder P, Madoux F, Cameron MD, Prisinzano TE, Aubé J, Bohn LM. Zhou L, et al. Among authors: bohn lm. J Biol Chem. 2013 Dec 20;288(51):36703-16. doi: 10.1074/jbc.M113.504381. Epub 2013 Nov 1. J Biol Chem. 2013. PMID: 24187130 Free PMC article.
Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.
Frankowski KJ, Slauson SR, Lovell KM, Phillips AM, Streicher JM, Zhou L, Whipple DA, Schoenen FJ, Prisinzano TE, Bohn LM, Aubé J. Frankowski KJ, et al. Among authors: bohn lm. Bioorg Med Chem. 2015 Jul 15;23(14):3948-56. doi: 10.1016/j.bmc.2014.12.033. Epub 2014 Dec 23. Bioorg Med Chem. 2015. PMID: 25593096 Free PMC article.
Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias.
Lovell KM, Frankowski KJ, Stahl EL, Slauson SR, Yoo E, Prisinzano TE, Aubé J, Bohn LM. Lovell KM, et al. Among authors: bohn lm. ACS Chem Neurosci. 2015 Aug 19;6(8):1411-9. doi: 10.1021/acschemneuro.5b00092. Epub 2015 May 1. ACS Chem Neurosci. 2015. PMID: 25891774 Free PMC article.
Molecular-interaction and signaling profiles of AM3677, a novel covalent agonist selective for the cannabinoid 1 receptor.
Janero DR, Yaddanapudi S, Zvonok N, Subramanian KV, Shukla VG, Stahl E, Zhou L, Hurst D, Wager-Miller J, Bohn LM, Reggio PH, Mackie K, Makriyannis A. Janero DR, et al. Among authors: bohn lm. ACS Chem Neurosci. 2015 Aug 19;6(8):1400-10. doi: 10.1021/acschemneuro.5b00090. Epub 2015 May 29. ACS Chem Neurosci. 2015. PMID: 25978068 Free PMC article.
Biased agonism: An emerging paradigm in GPCR drug discovery.
Rankovic Z, Brust TF, Bohn LM. Rankovic Z, et al. Among authors: bohn lm. Bioorg Med Chem Lett. 2016 Jan 15;26(2):241-250. doi: 10.1016/j.bmcl.2015.12.024. Epub 2015 Dec 9. Bioorg Med Chem Lett. 2016. PMID: 26707396 Free PMC article. Review.
113 results