Synthesis and characterization of peptide bioconjugates with antitumor activities

• Grant number: 23/03857-1
• Support Opportunities: Regular Research Grants
• Start date: October 01, 2023
• End date: September 30, 2026
• Field of knowledge: Physical Sciences and Mathematics - Chemistry
• Principal Investigator: Norival Alves Santos Filho
• Grantee: Norival Alves Santos Filho
• Host Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
• Associated researchers: Eduardo Maffud Cilli ; Ives Charlie da Silva ; Matheus Carlos Romeiro Miranda ; Tereza da Silva Martins ; Valeria Valente

Abstract

Currently, cancer is becoming increasingly common, being one of the main causes of death, especially in developing countries, representing today a real crisis for health systems worldwide. Conventionally administered treatment against tumor cells is not fully efficient, producing a range of side effects, decreasing the patient's quality of life, in addition to giving rise to multidrug resistance on the part of tumor cells. The associated toxicity and limited success of these traditional anticancer treatments have led to new studies for the development of innovative therapeutic strategies to combat the disease. Small molecules, such as anticancer peptides, which have great tissue penetration, high selectivity for tumor targets and efficient uptake by cancer cells, can be used in cancer therapies. However, their lack of specificity and high toxicity on normal cells lead to the need to work with antitumor peptides bioconjugated with aptamer peptides, which are more selective and lead to greater efficiency in killing tumor cells. In this context, the present work aims to synthesize and evaluate the antitumor potential of peptides and peptide bioconjugates and nanoparticles functionalized with aptamers, to study the structural characteristics of these compounds and their mechanisms of action on the cell membrane and mechanisms involved in cell death and toxicity. Furthermore, the toxicity, effectiveness and greater specificity of the bioconjugates against tumor cells will be analyzed in vivo in zebrafish models. (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)

BICHO, GABRIEL F. H.; NUNES, LETICIA O. C.; FIAMETTI, LOUISE OLIVEIRA; ARGENTIN, MARCELA N.; CANDIDO, VITORIA T.; CAMARGO, ILANA L. B. C.; CILLI, EDUARDO M.; SANTOS-FILHO, NORIVAL A.. Synthesis, Characterization, and Study of the Antimicrobial Potential of Dimeric Peptides Derived from the C-Terminal Region of Lys⁴⁹ Phospholipase A₂ Homologs. TOXINS, v. 16, n. 7, p. 14-pg., 2024-07-01. (23/03857-1, 22/05411-8, 13/07600-3)

FIAMETTI, LOUISE O.; FRANCO, CAMILLA A.; NUNES, LETICIA O. C.; DE CASTRO, LEANDRO M.; SANTOS-FILHO, NORIVAL A.. Study of Intracellular Peptides of the Central Nervous System of Zebrafish (Danio rerio) in a Parkinson's Disease Model. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, v. 26, n. 5, p. 12-pg., 2025-03-01. (23/05219-2, 23/03857-1)

Filed patent(s) as a result of this research project