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Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities.
Hu M, Giulianotti MA, McLaughlin JP, Shao J, Debevec G, Maida LE, Geer P, Cazares M, Misler J, Li L, Dooley C, Ganno ML, Eans SO, Mizrachi E, Santos RG, Yongye AB, Houghten RA, Yu Y. Hu M, et al. Among authors: houghten ra. Eur J Med Chem. 2015 Mar 6;92:270-81. doi: 10.1016/j.ejmech.2014.12.049. Epub 2014 Dec 29. Eur J Med Chem. 2015. PMID: 25559207
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.
Doering SR, Freeman KT, Schnell SM, Haslach EM, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Speth RC, Houghten RA, Haskell-Luevano C. Doering SR, et al. Among authors: houghten ra. J Med Chem. 2017 May 25;60(10):4342-4357. doi: 10.1021/acs.jmedchem.7b00301. Epub 2017 May 15. J Med Chem. 2017. PMID: 28453292 Free PMC article.
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.
Fleming KA, Freeman KT, Powers MD, Santos RG, Debevec G, Giulianotti MA, Houghten RA, Doering SR, Pinilla C, Haskell-Luevano C. Fleming KA, et al. Among authors: houghten ra. J Med Chem. 2019 Mar 14;62(5):2738-2749. doi: 10.1021/acs.jmedchem.9b00053. Epub 2019 Feb 28. J Med Chem. 2019. PMID: 30741545 Free PMC article.
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
Doering SR, Freeman K, Debevec G, Geer P, Santos RG, Lavoi TM, Giulianotti MA, Pinilla C, Appel JR, Houghten RA, Ericson MD, Haskell-Luevano C. Doering SR, et al. Among authors: houghten ra. J Med Chem. 2021 May 13;64(9):5577-5592. doi: 10.1021/acs.jmedchem.0c02041. Epub 2021 Apr 22. J Med Chem. 2021. PMID: 33886285 Free PMC article.
407 results