| Full text | |
| 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 - Sintese,estudo cinetico e aplicacoes de substratos e inibidores de enzimas proteoliticas. |
| Grantee: | Maria Aparecida Juliano |
| Support Opportunities: | Research Projects - Thematic Grants |