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Page 1
Identification of metabolites of the tryptase inhibitor CRA-9249: observation of a metabolite derived from an unexpected hydroxylation pathway.
Yu W, Dener JM, Dickman DA, Grothaus P, Ling Y, Liu L, Havel C, Malesky K, Mahajan T, O'Brian C, Shelton EJ, Sperandio D, Tong Z, Yee R, Mordenti JJ. Yu W, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4053-8. doi: 10.1016/j.bmcl.2006.05.003. Epub 2006 May 18. Bioorg Med Chem Lett. 2006. PMID: 16713261
Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease.
Sperandio D, Gangloff AR, Litvak J, Goldsmith R, Hataye JM, Wang VR, Shelton EJ, Elrod K, Janc JW, Clark JM, Rice K, Weinheimer S, Yeung KS, Meanwell NA, Hernandez D, Staab AJ, Venables BL, Spencer JR. Sperandio D, et al. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3129-33. doi: 10.1016/s0960-894x(02)00680-7. Bioorg Med Chem Lett. 2002. PMID: 12372517
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Palmer JT, Rydzewski RM, Mendonca RV, Sperandio D, Spencer JR, Hirschbein BL, Lohman J, Beltman J, Nguyen M, Liu L. Palmer JT, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3434-9. doi: 10.1016/j.bmcl.2006.04.013. Epub 2006 Apr 27. Bioorg Med Chem Lett. 2006. PMID: 16644215
Structure-guided design of peptide-based tryptase inhibitors.
McGrath ME, Sprengeler PA, Hirschbein B, Somoza JR, Lehoux I, Janc JW, Gjerstad E, Graupe M, Estiarte A, Venkataramani C, Liu Y, Yee R, Ho JD, Green MJ, Lee CS, Liu L, Tai V, Spencer J, Sperandio D, Katz BA. McGrath ME, et al. Among authors: sperandio d. Biochemistry. 2006 May 16;45(19):5964-73. doi: 10.1021/bi060173m. Biochemistry. 2006. PMID: 16681368
Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
Sperandio D, Tai VW, Lohman J, Hirschbein B, Mendonca R, Lee CS, Spencer JR, Janc J, Nguyen M, Beltman J, Sprengeler P, Scheerens H, Lin T, Liu L, Gadre A, Kellogg A, Green MJ, McGrath ME. Sperandio D, et al. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4085-9. doi: 10.1016/j.bmcl.2006.04.088. Epub 2006 May 24. Bioorg Med Chem Lett. 2006. PMID: 16725321
Discovery and structure-activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers.
Tai VW, Sperandio D, Shelton EJ, Litvak J, Pararajasingham K, Cebon B, Lohman J, Eksterowicz J, Kantak S, Sabbatini P, Brown C, Zeitz J, Reed C, Maske B, Graupe D, Estevez A, Oeh J, Wong D, Ni Y, Sprengeler P, Yee R, Magill C, Neri A, Cai SX, Drewe J, Qiu L, Herich J, Tseng B, Kasibhatla S, Spencer JR. Tai VW, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4554-8. doi: 10.1016/j.bmcl.2006.06.018. Epub 2006 Jun 19. Bioorg Med Chem Lett. 2006. PMID: 16784854
Discovery of 5-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-7-phenyl-(E)-2,3,6,7-tetrahydro-1,4-thiazepines as a new series of apoptosis inducers using a cell- and caspase-based HTS assay.
Drewe J, Kasibhatla S, Tseng B, Shelton E, Sperandio D, Yee RM, Litvak J, Sendzik M, Spencer JR, Cai SX. Drewe J, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4987-90. doi: 10.1016/j.bmcl.2007.05.098. Epub 2007 Jun 6. Bioorg Med Chem Lett. 2007. PMID: 17562361
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
Novel series of tunable µOR modulators with enhanced brain penetration for the treatment of opioid use disorder, pain and neuropsychiatric indications.
Nerurkar A, Nguyen T, Wang S, Bhatt U, Li K, Li Y, Ding P, Seidl FJ, Holan M, Lee J, Widjaja T, Wei ZL, Sadlowski C, Sperandio D, McGee LR, Youngblood B, Schwartz N, Gehlert D, Medina JC. Nerurkar A, et al. Among authors: sperandio d. Bioorg Med Chem Lett. 2023 Aug 15;92:129405. doi: 10.1016/j.bmcl.2023.129405. Epub 2023 Jul 5. Bioorg Med Chem Lett. 2023. PMID: 37414346 Free PMC article.
28 results