Publications

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

Book Chapters:

1) Sawyer, B. J.; Khan, M. I. H.; Le, H. V.* Antimalarial Drugs. In Medicinal Chemistry of Chemotherapeutic Agents; Elsevier/Academic Press: San Diego; 1st Edition; 2022. (the book can be preordered here on the Elsevier website).

Articles:

24) Khan, M. I. H.; Sawyer, B. J.; Akins, N. S.; Le, H. V.* A Systematic Review on the Kappa Opioid Receptor and Its Ligands: New Directions for the Treatment of Pain, Anxiety, Depression, and Drug Abuse. Eur. J. Med. Chem. 2022, under review. Preprint at ChemRxiv 2022, doi: 10.26434/chemrxiv-2022-s3d4b 

23) Khan, M. I. H.; Mahdi, F.; Penfornis, P.; Akins, N. S.; Hossain, M. I.; Kim, S. J.; Sulochana, S. P.; Adam, A. T.; Tran, T. D.; Tan, C.; Claudio, P. P.; Paris, J. J.; Le, H. V.* Synthesis and Biological Evaluation of tert-Butyl Ester and Ethyl Ester Prodrugs of L-γ-Methyleneglutamic Acid Amides for Cancer. Bioorg. Med. Chem. 2022, under review. Preprint at ChemRxiv 2022, doi: 10.26434/chemrxiv-2022-rhjcx. Invited paper in a special issue in honor of Professor Richard B. Silverman on the occasion of his receiving the 2021 Tetrahedron Prize for Creativity in Organic Chemistry.

22) Akins, N. S.; Mohammed, S. F.; Pandey, P.; Kim, S. J.; Mahdi, F.; Khan, M. I. H.; Moss, E.; Worth, C. J.; Keane, M. M.; Chittiboyina, A. G.; Doerksen, R. J.; Paris, J. J.; Le, H. V.* Alleviation of Cocaine Withdrawal and Pertinent Interactions Between Salvinorin-Based Antagonists and Kappa Opioid Receptor. ACS Chem. Neurosci. 2022, under review. Preprint at ChemRxiv 2022, doi: 10.26434/chemrxiv-2022-dpn5j-v2

21)  Kdimy, A.; Yadini, M. E.; Guaâdaoui, A.; Bourais, I.; El Hajjaji, S.*; Le, H. V.* Phytochemistry, Biological Activities, Therapeutic Potential, and Socioeconomic Value of the Caper Bush (Capparis spinosa L.). Chem. Biodiversity 2022, under review. Preprint at ChemRxiv 2022, doi: 10.26434/chemrxiv-2022-ph8qc

20) Cichon, J.; Liu, R.*; Le, H. V.* Therapeutic Potential of Salvinorin A and Its Analogues in Various Neurological Disorders. Transl. Perioper. Pain Med. 2022, 9, 452–457.

19)  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. Beilstein J. Org. Chem. 2022, 18, 446–458.

18)  Akins, N. S.; Mishra, N.; Harris, H. M.; Dudhipala, N.; Kim, S. J.; Keasling, A. W.; Majumdar, S.; Zjawiony, J. K.; Paris, J. J.; 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. ChemMedChem 2022, 17, e202100684.

17)  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. 2022, 34, e13047.

16)  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.

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.