Kirk R. Gustafson, Ph.D.

Kirk R. Gustafson, Ph.D.
Senior Scientist
Head, Natural Products Chemistry Group

Dr, Gustafson studies the structural chemistry and biological properties of naturally occurring compounds from terrestrial plants, marine organisms, and microbial isolates. His discovery of biologically active natural products has provided novel structural classes of complex secondary metabolites with unusual molecular scaffolds and functional group arrays.

Dr. Gustafson directs the laboratory’s Natural Products Chemistry Section, which engages in the isolation and structural characterization of bioactive compounds from natural product extracts that demonstrated activity in anticancer or anti-HIV screens. These compounds can serve as chemical probes for molecular target and mechanism of action studies or as preclinical development candidates.

Areas of Expertise

1) natural products chemistry, 2) NMR spectroscopy, 3) molecular targets,
4) high throughput screens, 5) structural elucidation

Contact Info

Kirk R. Gustafson, Ph.D.
Center for Cancer Research
National Cancer Institute
Building 562, Room 201
Frederick, MD 21702-1201
Ph: 301-846-5197

The NCI maintains a repository of natural product extracts that is the largest and most diverse in the world. These extracts, derived from terrestrial, marine and microbial organisms, constitute a unique source of chemical diversity for the discovery of compounds that can interact with specific molecular targets associated with human cancer. We are utilizing high throughput screening technologies to help identify compounds and extracts that can specifically interact with or modulate the function of selected biochemical targets or processes. Bioassay-guided chemical fractionation of natural products extracts is employed to isolate and purify the individual bioactive compounds. Identification and structural characterization of these compounds provides new structural classes or molecular scaffolds for the development of potential drug leads or biological probes which can interact with the desired molecular target. In addition to extensive spectroscopic analyses, our efforts include rigorous evaluation of a new compound's potency, molecular target specificity, and mode of action.

NIH Scientific Focus Areas:
Chemical Biology, Molecular Biology and Biochemistry
View Dr. Gustafson's PubMed Summary.

Selected Key Publications

  1. Yan P, Li G, Wang C, Wu J, Sun Z, Martin GE, Wang X, Reibarkh M, Saurí J, Gustafson KR.
    Org Lett. 21(18): 7577-81, 2019. [ Journal Article ]
  2. Kang U, Caldwell DR, Cartner LK, Wang D, Kim CK, Tian X, Bokesch HR, Henrich CJ, Woldemichael GM, Schnermann MJ, Gustafson KR.
    Org Lett. 21(12): 4750-53, 2019. [ Journal Article ]
  3. Singh AJ, Gorka AP, Bokesch HR, Wamiru A, O'Keefe BR, Schnermann MJ, Gustafson KR.
    J Nat Prod. 81(12): 2750-55, 2018. [ Journal Article ]
  4. Zlotkowski K, Hewitt WM, Yan P, Bokesch HR, Peach ML, Nicklaus MC, O'Keefe BR, McMahon JB, Gustafson KR, Schneekloth JS Jr.
    Org Lett. 19(7): 1726-29, 2017. [ Journal Article ]
  5. Goey AK, Chau CH, Sissung TM, Cook KM, Venzon DJ, Castro A, Ransom TR, Henrich CJ, McKee TC, McMahon JB, Grkovic T, Cadelis MM, Copp BR, Gustafson KR, Figg WD.
    J Nat Prod. 79(5): 1267-75, 2016. [ Journal Article ]

Dr. Gustafson earned his Ph.D. in organic chemistry from the University of British Columbia in 1984 under the direction of Professor Raymond J. Andersen. From 1984 to 1987 he worked as a postdoctoral fellow with Professor William Fenical at the Scripps Institution of Oceanography. He has a longstanding interest in the isolation, structural determination, and biological characterization of new secondary metabolites produced by terrestrial plants, marine organisms, and microbial isolates. Dr. Gustafson joined the NCI in 1987 and his studies have focused on utilizing the inherent chemical diversity found in natural product sources to help discover new compounds which can serve as biochemical probes or drug leads relevant to cancer and other human diseases.

Name Position
Heidi R. Bokesch, M.S. Scientist II (Leidos)
Richard W. Fuller M.S. Chemist
Unwoo Kang Ph.D. Postdoctoral Fellow (Visiting)
Chang-Kwon Kim Ph.D. Postdoctoral Fellow (Visiting)
Xiangrong Tian Ph.D. Special Volunteer
Laura Cartner
Laura Cartner 1998-2018