Dr. Bruno Gonçalves was hired to work on the project entitled Multidrug Resistance Reversal in Cancer: Natural Compounds as P-glycoprotein and Breast Cancer Resistance Protein Modulators. This project is financed by the Portuguese Science Foundation (FCT) to discover and develop… Read more ›
Human Pgp homology structure Read more ›
The phytochemical study of Euphorbia pedroi led to the isolation of a new tetracyclic triterpenoid with an unusual spiro scaffold, spiropedroxodiol (1), along with seven known terpenoids (2–8). Aiming at obtaining compounds with improved multidrug-resistance (MDR) reversal activity, compound 8,… Read more ›
Aim: Naringenin (1), isolated in large amount from the aerial parts of Euphorbia pedroi, was chemically derivatized to yield 18 imine derivatives (2–19) and three alkylated derivatives through a Mannich-type reaction (20–22) that were tested as multidrug resistance (MDR) reversers… Read more ›
David Cardoso won a PhD scholarship by the iMed.UL MedChemTrain PhD program to develop his studies named Plant derived compounds for targeting multidrug resistance in cancer with the computational part supervised by Dr. Daniel J.V.A. dos Santos. We welcome him… Read more ›
Cátia Alexandra Marques Bonito Ferreira has won a PhD scholarship by the Portuguese Science Foundation to develop her studies named Overcoming Multidrug Resistance: Search for Human P-glycoprotein Modulators and Insights on Drug Efflux Mechanism. We welcome her at the group… Read more ›
P-glycoprotein (P-gp) has been considered an important molecular target in the reversal of multidrug resistance (MDR). As such, the development of P-gp modulators able to restore drug sensitivity in resistant cells is still considered one of the most promising strategies… Read more ›
The paper titled About P-glycoprotein: a new drugable domain is emerging from structural data, was accepted by WIREs Comput. Mol. Sci.
Murine P-glycoprotein structure Read more ›
Background: From a dataset obtained by chemical derivatization of a macrocyclic diterpenic scaffold, in silico approaches identified which structural features correlate with experimental modulation of P-gp activity. Results/methodology: Ninety-two percent of the strongest MDR modulators were positively identified within the… Read more ›
The P-glycoprotein efflux mechanism is being studied since its identification as a leading protagonist in multidrug resistance. Recently, it was suggested that drugs enter the drug-binding pocket (DBP) through gates located between the transmembrane domains. For both a substrate and… Read more ›
The membrane biophysical aspects by which multidrug resistance (MDR) relate to the ABC transporter function still remain largely unknown. Notwithstanding the central role that efflux pumps like P-glycoprotein have in MDR onset, experimental studies classified additionally the lipid micro-environment where… Read more ›
Multidrug-resistance (MDR) phenomena are a worldwide health concern. ATP-binding cassette efflux pumps as P-glycoprotein have been thoroughly studied in a frantic run to develop new efflux modulators capable to reverse MDR phenotypes. The study of efflux pumps has provided some… Read more ›
One of the greatest threats to cancer treatment is the development, by some tumors, of resistance to the pharmacological action of several structurally unrelated cytotoxic agents—multidrug resistance (MDR). As P-glycoprotein (P-gp) is one of the most studied ATP-dependent efflux pumps… Read more ›
P-Glycoprotein (Pgp) is one of the best characterized ABC transporters, often involved in the multidrug-resistance phenotype overexpressed by several cancer cell lines. Experimental studies contributed to important knowledge concerning substrate polyspecificity, efflux mechanism, and drug-binding sites. This information is, however,… Read more ›