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Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands.
Kotsikorou E, Sharir H, Shore DM, Hurst DP, Lynch DL, Madrigal KE, Heynen-Genel S, Milan LB, Chung TD, Seltzman HH, Bai Y, Caron MG, Barak LS, Croatt MP, Abood ME, Reggio PH. Kotsikorou E, et al. Among authors: seltzman hh. Biochemistry. 2013 Dec 31;52(52):9456-69. doi: 10.1021/bi4008885. Epub 2013 Dec 17. Biochemistry. 2013. PMID: 24274581 Free PMC article.
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide (SR144528).
Kotsikorou E, Navas F 3rd, Roche MJ, Gilliam AF, Thomas BF, Seltzman HH, Kumar P, Song ZH, Hurst DP, Lynch DL, Reggio PH. Kotsikorou E, et al. Among authors: seltzman hh. J Med Chem. 2013 Sep 12;56(17):6593-612. doi: 10.1021/jm400070u. Epub 2013 Aug 14. J Med Chem. 2013. PMID: 23855811 Free PMC article.
N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A) interaction with LYS 3.28(192) is crucial for its inverse agonism at the cannabinoid CB1 receptor.
Hurst DP, Lynch DL, Barnett-Norris J, Hyatt SM, Seltzman HH, Zhong M, Song ZH, Nie J, Lewis D, Reggio PH. Hurst DP, et al. Among authors: seltzman hh. Mol Pharmacol. 2002 Dec;62(6):1274-87. doi: 10.1124/mol.62.6.1274. Mol Pharmacol. 2002. PMID: 12435794
Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity.
Zhao P, Sharir H, Kapur A, Cowan A, Geller EB, Adler MW, Seltzman HH, Reggio PH, Heynen-Genel S, Sauer M, Chung TD, Bai Y, Chen W, Caron MG, Barak LS, Abood ME. Zhao P, et al. Among authors: seltzman hh. Mol Pharmacol. 2010 Oct;78(4):560-8. doi: 10.1124/mol.110.066746. Epub 2010 Jul 22. Mol Pharmacol. 2010. PMID: 20826425 Free PMC article.
Metabolic Profiling of CB1 Neutral Antagonists.
Seltzman HH, Maitra R, Bortoff K, Henson J, Reggio PH, Wesley D, Tam J. Seltzman HH, et al. Methods Enzymol. 2017;593:199-215. doi: 10.1016/bs.mie.2017.06.025. Epub 2017 Jul 10. Methods Enzymol. 2017. PMID: 28750803 Free PMC article.
51 results