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Antiviral Drug Discovery Laboratory

Photo of Chin-Ho Chen, PhD

Chin-Ho Chen, PhD

Office: SORF Bldg Room 117 Durham, NC 27710
Phone: 919-684-3819

Scientific Focus

The Laboratory of Antiviral Drug Discovery conducts research for the development of novel therapeutics against HIV-1 and influenza viruses.

  • Novel small molecules against HIV-1 and influenza viruses
  • Identification of biological active principles from natural products
  • Lead optimization of antivirals
  • Molecular mechanisms of antiviral actions

Selected Achievements

 

  1. Discovery of HIV-1 entry inhibitors through studying HIV-1 Env-mediated cell-cell fusion. We study the structure and function of HIV-1 envelope glycoproteins with a goal of identifying inhibitors that can block HIV-1 entry. We are among the pioneers in defining the helix-helix interaction in gp41 that is critical for HIV-1 entry. Eventually, this led to the development of the FDA-approved HIV-1 fusion inhibitor, Fuzeon, which inhibits the helix-helix interaction of gp41. The discovery of the helix-helix interaction in gp41 is the theoretical basis for the development of the HIV-1 fusion inhibitor, Fuzeon. We believe small-molecule HIV-1 entry inhibitors also have potential to become useful additions to current antiretroviral therapy.
  2. Development of anti-HIV bi-functional betulinic acid derivatives. We have synthesized a class of betulinic acid derivatives that targets both HIV entry and maturation.
  3. Development of anti-HIV maturation inhibitor that can overcome bevirimat resistance observed in clinical trials.
  4. We have discovered that a daphnane diterpene, gnidimacrin, can inhibit HIV-1 entry at pM concentration. Gnidimacrin also activates HIV from latently infected cells and leads to the elimination of infected cells. Thus, gnidimacrin may also become a useful agent for purging HIV-1 from latent HIV reservoirs.
  5. Discovery of novel influenza virus inhibitors.

Contact Us

Li Huang: lihuang@duke.edu

Latest Publications

Li, Qi-Run, Yung-Yi Cheng, Lei Zhao, Xiao-Lei Huang, Xiao-Gang Jiang, Ya-Dong Cui, Susan L. Morris-Natschke, et al. “New phorbol ester derivatives as potent anti-HIV agents.” Bioorg Med Chem Lett 50 (October 15, 2021): 128319. https://doi.org/10.1016/j.bmcl.2021.128319.

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Li, Jing, Xiangyi Jiang, Alexej Dick, Prem Prakash Sharma, Chin-Ho Chen, Brijesh Rathi, Dongwei Kang, et al. “Design, synthesis, and antiviral activity of phenylalanine derivatives as HIV-1 capsid inhibitors.” Bioorg Med Chem 48 (October 15, 2021): 116414. https://doi.org/10.1016/j.bmc.2021.116414.

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Niwa, Kanji, Naonobu Tanaka, Yusei Shimomoto, Daisuke Tsuji, Sang-Yong Kim, Mareshige Kojoma, Kohji Itoh, Chin-Ho Chen, Kuo-Hsiung Lee, and Yoshiki Kashiwada. “Hyperdioxanes, dibenzo-1,4-dioxane derivatives from the roots of Hypericum ascyron.” J Nat Med 75, no. 4 (September 2021): 907–14. https://doi.org/10.1007/s11418-021-01540-y.

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Otsuki, Kouharu, Mi Zhang, Takashi Kikuchi, Minami Tsuji, Miyuko Tejima, Zi-Song Bai, Di Zhou, et al. “Identification of anti-HIV macrocyclic daphnane orthoesters from Wikstroemia ligustrina by LC-MS analysis and phytochemical investigation.” J Nat Med 75, no. 4 (September 2021): 1058–66. https://doi.org/10.1007/s11418-021-01551-9.

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