Hoang Le Research Group  


At the interface of medicinal chemistry and enzymology

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​​​​​11) Mascarenhas, R.; Le, H. V.; Clevenger, K. D.; Lehrer, H. J.; Ringe, D.; Kelleher, N. L.; Silverman, R. B.; Liu, D. "Selective Targeting by a Mechanism-Based Inactivator against PLP-Dependent Enzymes: Mechanisms of Inactivation and Alternative Turnover." Biochemistry 2017, 56, 4951-4961.


10) Wu, R.; Sanishvili, R.; Belitsky, B. R.; Juncosa, J. I.; Le, H. V; Lehrer, H. J. S.; Farley, M.; Silverman, R. B.; Petsko, G. A.; Ringe, D.; Liu, D. "PLP and GABA Trigger GabR-Mediated Transcription Regulation in Bacillus Subtilis via External Aldimine Formation." Proc. Natl. Acad. Sci. U. S. A. 2017, 114, 3891-3896.


Prior to Arrival at Ole Miss:


9) Lee, H.;# Le, H. V.;# Wu, R.; Doud, E.; Sanishvili, R.; Kellie, J. F., Compton, P. D.; Pachaiyappan, B., Liu, D.; Kelleher, N.; Silverman, R. B. “Mechanism of Inactivation of GABA Aminotransferase by (E)- and (Z)-(1S,3S)-3-Amino-4-fluoromethylenyl-1-cyclopentanoic Acid.ACS Chem. Biol. 2015, 10, 2087–2098. #Co-first authors, featured in “Introducing Our Authors” in the same issue.

8) Le, H. V.; Hawker, D. D.; Wu, R.; Doud, E.; Sanishvili, R.; Liu, D.; M.; Kelleher, N.; Silverman, R. B. “Design and Mechanism of Tetrahydrothiophene-based GABA-Aminotransferase Inactivators.J. Am. Chem. Soc. 2015, 137, 4525−4533.

7) Zigmond, E; Ya'acov, A. B.; Lee, H.; Lichtenstein, Y.; Shalev, Z.; Smith, Y.; Zolotarov, L.; Ziv, E.; Kalman, R.; Le, H. V.; Lu, H.; Silverman, R. B.; Ilan, Y. “Suppression of Hepatocellular Carcinoma by Inhibition of Overexpressed Ornithine Aminotransferase.ACS Med. Chem. Lett. 2015, 6, 840–844.

6) Le, H. V.; Ganem, B. “Mild Oxidation of Tosylmethylisocyanide to Tosylmethylisocyanate: Utility in Synthetic and Medicinal Chemistry.Tetrahedron Lett. 2014, 55, 2003-2005.

5) Le, H. V.; Ganem, B. “A Practical Synthesis of Isocyanates from Isonitriles: Ethyl 2-Isocyanatoacetate.Org. Synth. 2012, 89, 404-408.

4) Gober, C. M.; Le, H. V.; Ganem, B. “A Simple, General Synthesis of Carbonimidic Dichlorides.Tetrahedron Lett. 2012, 53, 4536-4537.

3) Le, H. V.; Ganem, B. “Trifluoroacetic Anhydride-Catalyzed Oxidation of Isonitriles by DMSO: A Rapid, Convenient Synthesis of Isocyanates.Org. Lett. 2011, 13, 2584-2585.

2) Sanguineti, G.; Le, H. V.; Ganem, B. “Studies on the Synthesis of Amidoximes from Nitroalkanes.Tetrahedron 2011, 67, 10208-10211. Invited paper in a special issue in honor of Professor Gilbert Stork on the occasion of his 90th birthday.


1) ­Le, H. V.; Fan, L.; Ganem, B. “A Practical and Inexpensive ‘Convertible’ Isonitrile for Use in Multicomponent Reactions.Tetrahedron Lett. 2011, 52, 2209-2211. Invited paper in a special issue in honor of Professor Harry Wasserman on the occasion of his 90th birthday. 


Patents:


3) Silverman, R. B.; Le, H. V.; Hawker, D. D.; McLeod, R. L. "Inactivators of Toxoplasma Gondii Ornithine Aminotransferase for Treating Toxoplasmosis and Malaria." U.S. Utility/Formal Patent Application No. 15/728,714, filed on October 10, 2017.


2) Silverman, R. B.; Takaya, K.; Le, H. V.; Juncosa, J. I. "(S)-3-Amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid, and Related Compounds as GABA Aminotransferase Inactivators for the Treatment of Epilepsy, Addiction and Hepatocellular Carcinoma.” United States Patent US 2017/0101364 A1, published on April 13, 2017. WIPO Patent WO 2017/062942 A2, published on April 13, 2017.  


1) Silverman, R. B.; Le, H. V.; Hawker, D. D. “Tetrahydrothiophene-based GABA Aminotransferase Inactivators.” United States Patent US 2016/0264544 A1, published on September 15, 2016. WIPO Patent WO 2016/145082 A1, published on September 15, 2016. ​