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Optimization of P-glycoprotein modulators and insights into the efflux mechanism

iMed.ULisboa/ FFULisboa Research Institute for Medicines/ Faculdade de Farmácia, Universidade de Lisboa
Project classification

Scientific area

3.1 Basic medicine

Discipline(s)

Medicinal chemistry

Project description

Project title

Optimization of P-glycoprotein modulators and insights into the efflux mechanism

Scientific Coordinator's name:

Maria José Umbelino Ferreira

Scientific Coordinator's e-mail:

mjuferreira@ff.ul.pt

Principal R&D Unit:

iMed.UL/FFUL

Other R&D Units involved in the project:

Madeira University; Institute of Medical Microbiology, Szeged University; Institute of Pathology Charité Campus Mitte, Humbolt University; First Department of Pathology and Experimental Cancer Research, Faculty of Medicine, Semmelweis University

Project keyword(s)

Multidrug resistance; P-glycoprotein modulators

Short abstract and comments

Multidrug resistance (MDR) is considered the major obstacle for successful cancer chemotherapy. MDR is associated to the overexpression of ABC-transporter proteins, such as P-glycoprotein (Pgp), which acts as an efflux pump for structurally and functionally unrelated chemotherapeutic agents. The broad goals of this project are: i) optimize macrocyclic diterpenes and cucurbitane-type triterpenes as leads for overcoming Pgp-mediated MDR, using QSAR, docking and molecular dynamics simulations along with in vitro and in vivo experiments; ii) unveil their binding modes with Pgp, using in silico and in vitro models and iii) get insight into the efflux mechanism from MD P-glycoprotein modeling.

Potential uses/indications

The project will contribute for overcoming MDR and for better understanding the efflux mechanism of ABC-transporters.

Status

Ongoing

Partner Status: Seeking Partners?

Yes

Grant number (QREN, FP7, Eureka, etc)

Grant number (QREN, FP7, Eureka, etc)

Last edited on

2013-11-04 16:34:30

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