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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:

Latest Publications

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, June 17, 2021.

Full Text

Zhao, Yu, Chin-Ho Chen, Susan L. Morris-Natschke, and Kuo-Hsiung Lee. “Design, synthesis, and structure activity relationship analysis of new betulinic acid derivatives as potent HIV inhibitors.” Eur J Med Chem 215 (April 5, 2021): 113287.

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Feng, Da, Xiaofang Zuo, Lanlan Jing, Chin-Ho Chen, Fisayo A. Olotu, Hao Lin, Mahmoud Soliman, et al. “Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.” Eur J Med Chem 211 (February 5, 2021): 113063.

Full Text

Dang, Zhao, Lei Zhu, Lan Xie, Kuo-Hsiung Lee, Faisal Malik, Zhijun Li, Li Huang, and Chin-Ho Chen. “Design and Synthesis of Quinolizidine Derivatives as Influenza Virus and HIV-1 Inhibitors.” Curr Med Chem, December 29, 2020.

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