| Full text | |
| Author(s): Show less - |
Ramalho, Suelem D.
[1]
;
De Sousa, Lorena R. F.
[1]
;
Nebo, Liliane
[1]
;
Maganhi, Stella H.
[2]
;
Caracelli, Ignez
[2]
;
Zukerman-Schpector, Julio
[1]
;
Lima, Maria Ines S.
[3]
;
Alves, Marcio F. M.
[4]
;
Da Silva, M. Fatima das G. F.
[1]
;
Fernandes, Joao B.
[1]
;
Vieira, Paulo C.
[1]
Total Authors: 11
|
| Affiliation: | [1] Univ Fed Sao Carlos, Dept Chem, BR-13565905 Sao Carlos, SP - Brazil
[2] Univ Fed Sao Carlos, BioMat Dept Phys, BR-13565905 Sao Carlos, SP - Brazil
[3] Univ Fed Sao Carlos, Dept Bot, BR-13565905 Sao Carlos, SP - Brazil
[4] Univ Fed Sao Paulo, Dept Biophys, BR-04039032 Sao Paulo - Brazil
Total Affiliations: 4
|
| Document type: | Journal article |
| Source: | CHEMISTRY & BIODIVERSITY; v. 11, n. 9, p. 1354-1363, SEP 2014. |
| Web of Science Citations: | 3 |
| Abstract | |
Cathepsins L (catL) and B play an important role in tumor progression and have been considered promising therapeutic targets in the development of novel anticancer agents. Using a bioactivity-guided fractionation, a series of triterpenoids was identified as a new class of competitive inhibitors towards cathepsin L with affinity values in micromolar range. Among the 14 compounds evaluated, the most promising were 3-epiursolic acid (3), 3-(hydroxyimino) oleanolic acid (9), and 3-(hydroxyimino) masticadienoic acid (13) with IC50 values of 6.5, 2.4, and 2.6 mu m on catL, respectively. Most of the evaluated triterpenoids do not inhibit cathepsin B. Thus, the evaluated compounds exhibit a great potential to help in the design of new inhibitors with enhanced potency and affinity towards catL. Docking studies were performed in order to gain insight on the binding mode and SAR of these compounds. (AU) | |
| FAPESP's process: | 12/22524-9 - Synthesis, characterization and docking studies of controlled drug delivery systems for drugs and potential drugs using chitosan as a carrier |
| Grantee: | Stella Hernandez Maganhi |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |