At the interface of medicinal chemistry and enzymology

 Hoang Le Research Group  


​​​​​12) Juncosa, J. I.; Takaya, K.; Le, H. V.; Moschitto, M. J.; Weerawarna, P. M.; Mascarenhas, R.; Liu, D.; Dewey, S. L.; Silverman, R. B. "Design and Mechanism of (S)-3-Amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic Acid, a Highly Potent γ-Aminobutyric Acid Aminotransferase Inactivator for the Treatment of Addiction." J. Am. Chem. Soc. 2018, 140, 2151–2164.

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.; Widom, J.; Sanishvili, R.; Liu, D.; Kelleher, N. L.; 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. 


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 9,670,141, published on June 6, 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 9,856,231, published on January 2, 2018. WIPO Patent WO 2016/145082 A1, published on September 15, 2016. ​​