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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Functionalization of new anticancer Pt(II) complex with transferrin receptor binding peptide

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Author(s):
Teles, Catherine M. [1] ; Antunes, Victor U. [1] ; Cardoso, Raquel S. [2] ; Candido, Tuany Z. [3] ; Lima, Carmen S. P. [3] ; Ruiz, Ana Lucia T. G. [2] ; Juliano, Maria A. [4] ; Favaro, Denize C. [1] ; Abbehausen, Camilla [1]
Total Authors: 9
Affiliation:
[1] Univ Estadual Campinas, Inst Chem, UNICAMP, POB 6154, BR-13083970 Campinas, SP - Brazil
[2] Univ Estadual Campinas, Fac Pharmaceut Sci, UNICAMP, BR-13083871 Campinas, SP - Brazil
[3] Univ Estadual Campinas, Fac Med Sci, UNICAMP, BR-13083970 Campinas, SP - Brazil
[4] Univ Fed Sao Paulo, UNIFESP, Escola Paulista Med, BR-04063062 Sao Paulo, SP - Brazil
Total Affiliations: 4
Document type: Journal article
Source: Inorganica Chimica Acta; v. 511, OCT 1 2020.
Web of Science Citations: 0
Abstract

One strategy to improve the selectivity of metallocompounds is to functionalize them by conjugation with biomolecules as folate, hormones, and peptides. In this work, we describe the conjugation of a transferrin re-ceptor binding peptide of sequence HAIYPHRH to a Pt(II) bis(2-pyridylmethyl)glycine complex. The complex was fully characterized by mass spectrometry and 1D and 2D NMR. Among several synthetic strategies, the preparation of bis-(2-pyridylmethyl)glycyl-NH-HAIYPHRH by solid-phase peptide synthesis, its purification by HPLC, followed by the coordination of Pt(II) was the successful method. The metal coordination was studied by H-1 NMR and H-1 -N-15 HSQC. The results show the metal ion interacts by fast exchange reaction with the two terminal histidines and slow exchange with bis(2-pyridylmethyl)glycine moiety. The compounds presented in-hibition of growth for renal cancer cells; therefore, it is not an effect of the peptide as the precursor, {[}PtCl(bis(2-pyridylmethyl)glycine)], presents similar GI(50). The peptide-Pt(II) complex presents a high binding constant with serum albumin and demonstrated to bind covalently to DNA by electrophoretic mobility assays. The work re-presents a complete description of the coordination of platinum in this system and demonstrates the challenges to develop new metallopeptides. (AU)

FAPESP's process: 19/16904-2 - Targeted metallodrug design for antileishmaniasis
Grantee:Camilla Abbehausen
Support Opportunities: Regular Research Grants
FAPESP's process: 16/07729-4 - Metal complex from golden, palladium and silver in the treatment of skin squamous cell carcinoma
Grantee:Tuany Zambroti Cândido
Support Opportunities: Scholarships in Brazil - Doctorate
FAPESP's process: 12/50191-4 - Synthesis, kinetic studies and applications of substrates and inhibitors for proteolytic enzymes
Grantee:Maria Aparecida Juliano
Support Opportunities: Research Projects - Thematic Grants