Missing Avatar

Michael Saporito

Vice President of Research - Melior Discovery Inc.
Exton Pennsylvania, US

Position - Company  
Vice President of Research - Melior Discovery Inc. 2012 - Present
Degree - University  
Ph.D., Pharmacology - University of the Sciences in Philadelphia 1985 - 1989
Publication Info
MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo. Saporito MS, Ochman AR, Lipinski CA, Handler JA, Reaume AG J Pharmacol Exp Ther. 342(1):15-22. doi: 10.1124/jpet.112.192096. July 2012. View on PubMed.
The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes. Ochman AR, Lipinski CA, Handler JA, Reaume AG, Saporito MS J Pharmacol Exp Ther. 342(1):23-32. doi: 10.1124/jpet.112.192187. July 2012. View on PubMed.
Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. Shetty RS, Lee Y, Liu B, Husain A, Joseph RW, Lu Y, Nelson D and 17 others J Med Chem. 54(1):179-200. doi: 10.1021/jm100659v. January 13, 2011. View on PubMed.
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. Hudkins RL, Diebold JL, Tao M, Josef KA, Park CH, Angeles TS, Aimone LD and 13 others J Med Chem. 51(18):5680-9. doi: 10.1021/jm8005838. September 25, 2008. View on PubMed.
Inhibition of mixed lineage kinase 3 attenuates MPP+-induced neurotoxicity in SH-SY5Y cells. Mathiasen JR, McKenna BA, Saporito MS, Ghadge GD, Roos RP, Holskin BP, Wu ZL and 6 others Brain Res. 1003(1-2):86-97. doi: 10.1016/j.brainres.2003.11.073. April 2, 2004. View on PubMed.
Targeting the JNK pathway for therapeutic benefit in CNS disease. Bozyczko-Coyne D, Saporito MS, Hudkins RL Curr Drug Targets CNS Neurol Disord. 1(1):31-49. February 2002. View on PubMed.
Mixed lineage kinase activity of indolocarbazole analogues. Murakata C, Kaneko M, Gessner G, Angeles TS, Ator MA, O'Kane TM, McKenna BA and 5 others Bioorg Med Chem Lett. 12(2):147-50. January 21, 2002. View on PubMed.
Discovery of CEP-1347/KT-7515, an inhibitor of the JNK/SAPK pathway for the treatment of neurodegenerative diseases. Saporito MS, Hudkins RL, Maroney AC Prog Med Chem. 40:23-62. 2002. View on PubMed.
MPTP activates c-Jun NH(2)-terminal kinase (JNK) and its upstream regulatory kinase MKK4 in nigrostriatal neurons in vivo. Saporito MS, Thomas BA, Scott RW J Neurochem. 75(3):1200-8. September 2000. View on PubMed.
CEP-1347 increases ChAT activity in culture and promotes cholinergic neurone survival following fimbria-fornix lesion. Harper SJ, Saporito MS, Hewson L, Young L, Smith D, Rigby M, Jackson P and 5 others Neuroreport. 11(10):2271-6. July 14, 2000. View on PubMed.
CEP-1347/KT-7515, an inhibitor of c-jun N-terminal kinase activation, attenuates the 1-methyl-4-phenyl tetrahydropyridine-mediated loss of nigrostriatal dopaminergic neurons In vivo. Saporito MS, Brown EM, Miller MS, Carswell S J Pharmacol Exp Ther. 288(2):421-7. February 1999. View on PubMed.
Preservation of cholinergic activity and prevention of neuron death by CEP-1347/KT-7515 following excitotoxic injury of the nucleus basalis magnocellularis. Saporito MS, Brown ER, Carswell S, DiCamillo AM, Miller MS, Murakata C, Neff NT, Vaught JL, Haun FA Neuroscience. 86(2):461-72. September 1998. View on PubMed.
High levels of synthesis and local effects of nerve growth factor in the septal region of the adult rat brain. Saporito MS, Carswell S J Neurosci. 15(3 Pt 2):2280-6. March 1995. View on PubMed.
Systemic dexamethasone administration increases septal Trk autophosphorylation in adult rats via an induction of nerve growth factor. Saporito MS, Brown ER, Hartpence KC, Wilcox HM, Robbins E, Vaught JL, Carswell S Mol Pharmacol. 45(3):395-401. March 1994. View on PubMed.
Chronic 1,25-dihydroxyvitamin D3-mediated induction of nerve growth factor mRNA and protein in L929 fibroblasts and in adult rat brain. Saporito MS, Brown ER, Hartpence KC, Wilcox HM, Vaught JL, Carswell S Brain Res. 633(1-2):189-96. January 7, 1994. View on PubMed.
Pharmacological induction of nerve growth factor mRNA in adult rat brain. Saporito MS, Wilcox HM, Hartpence KC, Lewis ME, Vaught JL, Carswell S Exp Neurol. 123(2):295-302. doi: 10.1006/exnr.1993.1162. October 1993. View on PubMed.
1-Methyl-4-(2'-ethylphenyl)-1,2,3,6-tetrahydropyridine-induced toxicity in PC12 cells is enhanced by preventing glycolysis. Basma AN, Heikkila RE, Saporito MS, Philbert M, Geller HM, Nicklas WJ J Neurochem. 58(3):1052-9. March 1992. View on PubMed.
Dopaminergic neurotoxicity of 1-methyl-4-phenylpyridinium analogs in cultured neurons: relationship to the dopamine uptake system and inhibition of mitochondrial respiration. Saporito MS, Heikkila RE, Youngster SK, Nicklas WJ, Geller HM J Pharmacol Exp Ther. 260(3):1400-9. March 1992. View on PubMed.
Inhibition of serotonin release by bombesin-like peptides in rat hypothalamus in vitro. Saporito MS, Warwick RO Jr Life Sci. 45(1):15-23. 1989. View on PubMed.
  • Michael Saporito hasn't received any ratings yet...