Publications

Underscored names are members of my lab. * Corresponding author.

19) Salahuddin, M. F.; Qrareya, A. N.; Mahdi, F.; Moss, E.; Akins, N. S.; Li, J.; Le, H. V.; Paris, J. J.* "Allopregnanolone and NeuroHIV: Potential Benefits of Neuroendocrine Modulation in the Era of Antiretroviral Therapy" J. Neuroendocrinol. 2021, under peer review.

18) Madkhali, H.; Tarawneh, A.; Ali, Z.; Le, H. V.; Cutler, S. J.; Khan, I. A.; Shariat-Madar, Z.* "Identification of Human Kinin-forming Enzyme Inhibitors from Medicinal Herbs" Molecules 2021, 26, 4126.

17) Hossain, M. I.; Khan, M. I. H.; Kim, S. J.; Le, H. V.* “Synthesis of 3,4,5-Trisubstituted Isoxazoles in Water via a [3+2]-Cycloaddition of Nitrile Oxides and 1,3-Diketones, β-Ketoesters, or β-Ketoamides: Base-mediated and Keto-enol-controlled Mechanism” J. Org. Chem. 2021, under peer review. ChemRxiv. Preprint. DOI: 10.26434/chemrxiv.14269472

16) Akins, N. S.; Mishra, N.; Harris, H. M.; Dudhipala, N.; Kim, S. J.; Keasling, A. W.; Majumdar, S.; Zjawiony, J. K.; Ashpole, N. M.; Le, H. V.* “6,5-Fused Ring, C2-Salvinorin Ester, Dual Kappa and Mu Opioid Receptor Agonists as Analgesics Devoid of Anxiogenic Effects” ACS Med. Chem. Lett. 2021, in revision. ChemRxiv. Preprint. DOI: 10.26434/chemrxiv.14204834.v1

15) Hossain, M. I.; Thomas, A. G.; Mahdi, F.; Adam, A. T.; Akins, N. S.; Woodard, M. M.; Paris, J. J.; Slusher, B. S.; Le, H. V.* “An Efficient Synthetic Route to L-γ-Methyleneglutamine and Its Amide Derivatives, and Their Selective Anticancer Activity” RSC Adv. 2021, 11, 7115–7128.

14) Xu, J.; Chen, F.; Wang, S.; Akins, N. S.; Hossain, M. I.; Zhou, Y.; Huang, J.; Ji, J.; Xi, J.; Lin, W.; Grothusen, J.; Le, H. V.; Liu, R.* “Kappa Opioid Receptors Internalization Is Protective Against Oxygen-glucose Deprivation Through β-Arrestin Activation and Akt-mediated Signaling Pathway.” Neurochem. Int.  2020, 137, 104748.

13) Akins, N. S.; Nielson, T. C.; Le, H. V.* “Inhibition of Glycolysis and Glutaminolysis: An Emerging Drug Discovery Approach to Combat Cancer.” Curr. Top. Med. Chem.  2018, 18, 494–504.​​​​​​​​​​​​​​​​​​​

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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.

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.

5) Le, H. V.*; Hossain, M. I. “L-γ-Methyleneglutamine Compounds, Methods of Forming the Same, and Methods of Use Thereof” Worldwide Patent PCT/US20/41839, filed on July 13, 2020.

4) Le, H. V.*; Kim, S-J. “Cytochrome bc1 Complex Inhibitors and Methods of Use Thereof.” U.S. Provisional Patent Application No. 62/689,598, filed on June 25, 2018, refiled on June 25, 2019, refiled on June 25, 2020.

3) Silverman, R. B.*; Le, H. V.; Hawker, D. D.; McLeod, R. L. "Inactivators of Toxoplasma Gondii Ornithine Aminotransferase for Treating Toxoplasmosis and Malaria." United States Patent US 2018/0098952, published on December 4, 2018.

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. ​​