Screening of (bio)synthetic organic compounds with biological targets against cancer

• Grant number: 11/21358-5
• Support Opportunities: Scholarships abroad - Research Internship - Post-doctor
• Start date: March 01, 2012
• End date: August 31, 2012
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Ronaldo Aloise Pilli
• Grantee: Daniela Barretto Barbosa Trivella
• Supervisor: Bradley S. Moore
• Host Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
• Institution abroad: University of California, San Diego (UC San Diego), United States
• Associated to the scholarship: 10/17544-5 - Structural and molecular bases of inhibitor recognition by the CDC-25 and LMW-PTP human protein phosphatases involved in cancer, BP.PD

Abstract

Two main activities, related to the original aims of the post doctoral research project, were outlined: the search for new classes of phosphatase inhibitors and the search for new biological targets against cancer. It is intended to include the 20S subunit of the proteasome as a new biological target in trials with the organic compounds already synthesized in the context of the Thematic Project "Chemistry Biology: new natural and synthetic molecular targets against cancer. Structural studies, biological evaluation and mechanism of action" (Fapesp 2009/51602-5), associated with this research proposal; as well as to test natural products derived from marine organisms and biosynthetic derivatives, available in the foreign laboratory, against the activity of the protein phosphatases under study by the Pos-Doctoral fellow. In parallel, it is intended to widen her knowledge in the use of biotechnological tools with application on organic (bio)synthesis, aiming at obtaining new compounds with biological activity, research area in which the foreign researcher has been outstanding and is one of the main international references in the field. The pos-doctoral fellow demonstrates large interest in widen her knowledge in this research area, which represents an interface between her background in biochemistry and structural biology and the activities under development by the organic synthesis collaborative groups. It is a research area in constant expansion in the international context, which shows potential for implementation in the State of Sao Paulo and contribution to the national development in science and technology. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

TRIVELLA, DANIELA B. B.; PEREIRA, ALBAN R.; STEIN, MARTIN L.; KASAI, YUSUKE; BYRUM, TARA; VALERIOTE, FREDERICK A.; TANTILLO, DEAN J.; GROLL, MICHAEL; GERWICK, WILLIAM H.; MOORE, BRADLEY S.. Enzyme Inhibition by Hydroamination: Design and Mechanism of a Hybrid Carmaphycin-Syringolin Enone Proteasome Inhibitor. CHEMISTRY & BIOLOGY, v. 21, n. 6, p. 782-791, JUN 19 2014. (11/21358-5)

BAUMAN, KATHERINE D.; SHENDE, VIKRAM V.; CHEN, PERCIVAL YANG-TING; TRIVELLA, DANIELA B. B.; GULDER, TOBIAS A. M.; VELLALATH, SREEKUMAR; ROMO, DANIEL; MOORE, BRADLEY S.. Enzymatic assembly of the salinosporamide gamma-lactam-beta-lactone anticancer warhead. Nature Chemical Biology, v. 18, n. 5, p. 23-pg., 2022-03-21. (11/21358-5)