School of Pharmacy

The University of Mississippi

Dr. Hoang V. Le

Posted on: August 29th, 2016 by sydney
Assistant Professor of Medicinal Chemistry
Faser Hall 419
662-915-2555
 

Education:

  • Ph.D. Cornell University
  • B.S. University of California, Berkeley

Appointment(s):

  • Assistant Professor of Medicinal Chemistry
  • Research Assistant Professor in the Research Institute of Pharmaceutical Sciences

Career Highlights:

Hoang V. Le graduated from the University of California, Berkeley with a B.S. degree in chemistry in 2008. While at Berkeley, Hoang worked in the laboratory of Professor Kenneth Raymond, studying supramolecular chemistry, synthesizing dicationic linkers, and investigating their stability in supramolecular systems. In 2013, he graduated from Cornell University with a Ph.D. degree in organic chemistry under the guidance of Professor Bruce Ganem. His graduate work expanded the scope of multicomponent reaction (MCR) chemistry by improving known synthetically useful MCRs and developing new MCRs. Hoang then held a postdoctoral position in the laboratory of Professor Richard Silverman at Northwestern University. His postdoctoral research contributed to the development of two patented potential drug candidates for the treatment of epilepsy and drug addiction. His postdoctoral research also contributed to the discovery of many inactivators of Toxoplasma gondii ornithine aminotransferase for the treatment of toxoplasmosis. In July 2016, he started his independent research career as an Assistant Professor of Medicinal Chemistry in the Department of BioMolecular Sciences at the University of Mississippi School of Pharmacy.

Research:

Our research goal is to develop new drugs for the treatment of cancer, including both common types of cancer such as lung, liver, stomach, breast, and prostate cancer and rare types of cancer such as leukemia and gliomas. According to the World Cancer Report 2014, cancer accounted for 14.6% of all human deaths, equaling to 8.2 million lives in 2012. If considered as a single entity, cancer has become the biggest cause of mortality worldwide. Metabolic enzymes have recently become the focus of intensive efforts in the discovery of new therapeutic targets and new cancer drugs, particularly kidney-type glutaminase (GLS1), mutant isocitrate dehydrogenases (IDH1 and IDH2), succinate dehydrogenase, and fumarate hydratase. Currently, we are focusing on the development of inhibitors and inactivators of several metabolic enzymes for the treatment of cancer and for the discovery of new antibiotic agents. Our strategies for the development of effective and selective inhibitors of these enzymes utilize a wide range of modern drug development tools and methods to guide the drug design process. The research in our group covers the full range of in vitro drug development, including computational design, synthesis, and biological evaluation of potential medicinal agents and investigation of their molecular mechanisms of action.

Publications:

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.Tetrahedron2011, 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. Provisional Patent Application No. 62/406,104, filed October 10, 2016.

2) Silverman, R. B.; Juncosa, J. I.; Le, H. V.; Takaya, K. “(S)-3-Amino-4-(difluoromethylenyl)-cyclopent-1-ene-1-carboxylic acid, a Highly Potent GABA Aminotransferase Inactivator for the Treatment of Epilepsy, Addiction and Hepatocellular Carcinoma.” U.S. Formal/Utility Application, Serial No. 15/289,480, filed October 10, 2016. PCT International Patent Application, Serial No. PCT/US2016/056245, filed October 10, 2016.

1) Silverman, R. B.; Hawker, D. D.; Le, H. V.“Tetrahydrothiophene-based GABA Aminotransferase Inactivators.” U.S. Formal/Utility Application, Serial No. 15/065,487, filed March 9, 2016. PCT International Patent Application, Serial No. PCT/US2016/021565, filed March 9, 2016.

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