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
301-846-5197
gustafki@mail.nih.gov

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.

Scientific Focus Areas:
Chemical Biology

View Dr. Gustafson's PubMed Summary.

Selected Key Publications
  1. Oku N, Takada K, Fuller RW, Wilson JA, Peach ML, Pannell LK, McMahon JB, Gustafson KR.
    J. Am. Chem. Soc. 132: 10278-85, 2010. [ Journal Article ]
  2. Versiani MA, Diyabalanage T, Ratnayake R, Henrich CJ, Bates SE, McMahon JB, Gustafson KR.
    J. Nat. Prod. 74: 262-6, 2011. [ Journal Article ]
  3. Diyabalanage T, Ratnayake R, Wilson JA, Henrich CJ, Beutler JA, Colburn NH, McMahon JB, Gustafson KR.
    Bioorg. Med. Chem. Lett. 21: 4397-9, 2011. [ Journal Article ]
  4. Grkovic T, Blees JS, Colburn NH, Schmid T, Thomas CL, Henrich CJ, McMahon JB, Gustafson KR.
    J. Nat. Prod. 74: 1015-20, 2011. [ Journal Article ]
  5. Blees JS, Bokesch HR, Rübsamen D, Schulz K, Milke L, Bajer MM, Gustafson KR, Henrich CJ, McMahon JB, Colburn NH, Schmid T, Brune B.
    PLoS ONE. 7: e46567, 2012. [ 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 Bokesch M.S. Staff Scientist (Contr)
Laura Cartner B.S. Senior Research Assistant (Contr)
Susanna Chan Ph.D. Postdoctoral Fellow (Visiting)
Ana De Castro Valdeira M.Sc. Special Volunteer
Renata Dusi Special Volunteer
Richard Fuller M.S. Research Chemist
Amanda Waters Ph.D. Postdoctoral Fellow (CRTA)
Pengcheng Yan Special Volunteer (Visiting)

Research

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.

Scientific Focus Areas:
Chemical Biology

Publications

View Dr. Gustafson's PubMed Summary.

Selected Key Publications
  1. Oku N, Takada K, Fuller RW, Wilson JA, Peach ML, Pannell LK, McMahon JB, Gustafson KR.
    J. Am. Chem. Soc. 132: 10278-85, 2010. [ Journal Article ]
  2. Versiani MA, Diyabalanage T, Ratnayake R, Henrich CJ, Bates SE, McMahon JB, Gustafson KR.
    J. Nat. Prod. 74: 262-6, 2011. [ Journal Article ]
  3. Diyabalanage T, Ratnayake R, Wilson JA, Henrich CJ, Beutler JA, Colburn NH, McMahon JB, Gustafson KR.
    Bioorg. Med. Chem. Lett. 21: 4397-9, 2011. [ Journal Article ]
  4. Grkovic T, Blees JS, Colburn NH, Schmid T, Thomas CL, Henrich CJ, McMahon JB, Gustafson KR.
    J. Nat. Prod. 74: 1015-20, 2011. [ Journal Article ]
  5. Blees JS, Bokesch HR, Rübsamen D, Schulz K, Milke L, Bajer MM, Gustafson KR, Henrich CJ, McMahon JB, Colburn NH, Schmid T, Brune B.
    PLoS ONE. 7: e46567, 2012. [ Journal Article ]

Biography

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.

Team

Name Position
Heidi Bokesch M.S. Staff Scientist (Contr)
Laura Cartner B.S. Senior Research Assistant (Contr)
Susanna Chan Ph.D. Postdoctoral Fellow (Visiting)
Ana De Castro Valdeira M.Sc. Special Volunteer
Renata Dusi Special Volunteer
Richard Fuller M.S. Research Chemist
Amanda Waters Ph.D. Postdoctoral Fellow (CRTA)
Pengcheng Yan Special Volunteer (Visiting)