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New secondary metabolites of endophytic and marine organisms as proteasome inhibitors: a validated target against cancer

Grant number: 17/06014-4
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): June 01, 2017
Effective date (End): May 31, 2020
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Cooperation agreement: Coordination of Improvement of Higher Education Personnel (CAPES)
Principal Investigator:Roberto Gomes de Souza Berlinck
Grantee:Juliana Regina Gubiani
Home Institution: Instituto de Química de São Carlos (IQSC). Universidade de São Paulo (USP). São Carlos , SP, Brazil

Abstract

The present project aims at the discovery of proteasome inhibitors. The proteasome is the main non-lysosomal proteolytic complex, and is already a validated target for the treatment of multiple myeloma, with potential validation for other human diseases, such as in the treatment of Chagas disease, leishmaniasis and inflammatory diseases. Thus, finding substances capable of inhibiting the proteasome is a validated strategy for multiple myeloma and other neoplasms. In this context, seventeen extracts of fungal and marine origin, among hundreds of extracts tested, presented proteasome inhibitory activity. These extracts will be prioritized for HPLC-UV-MS and UPLC-QTOF analyzes and for bioguided isolation of new proteasome inhibitors. In this way, the objective is to isolate and identify proteasome inhibitors from these extracts from invertebrates and marine and endophytic microorganisms, with unprecedented structural characteristics. (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)
BERLINCK, ROBERTO G. S.; MONTEIRO, AFIF F.; BERTONHA, ARIANE F.; BERNARDI, DARLON I.; GUBIANI, JULIANA R.; SLIVINSKI, JULIANO; MICHALISKI, LAMONIELLI F.; TONON, LUCIANE A. C.; VENANCIO, VICTOR A.; FREIRE, VITOR F. Approaches for the isolation and identification of hydrophilic, light-sensitive, volatile and minor natural products. NATURAL PRODUCT REPORTS, v. 36, n. 7, p. 981-1004, JUL 1 2019. Web of Science Citations: 0.
KURODA, YUSUKE; NICACIO, KAREN J.; DA SILVA-, JR., ILDEFONSO ALVES; LEGER, PAUL R.; CHANG, STANLEY; GUBIANI, JULIANA R.; DEFLON, VICTOR M.; NAGASHIMA, NOZOMU; RODE, ALEXANDER; BLACKFORD, KATHERINE; FERREIRA, ANTONIO G.; SETTE, LARA D.; WILLIAMS, DAVID E.; ANDERSEN, RAYMOND J.; JANCAR, SONIA; BERLINCK, ROBERTO G. S.; SARPONG, RICHMOND. Isolation, synthesis and bioactivity studies of phomactin terpenoids. NATURE CHEMISTRY, v. 10, n. 9, p. 938-945, SEP 2018. Web of Science Citations: 6.

Please report errors in scientific publications list by writing to: cdi@fapesp.br.