Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.6.3.44 (
P-glycoprotein
)
13,344
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Multidrug resistance is a major cause of failure in the clinical cancer therapy, in which the overexpression of
P-glycoprotein
(
P-gp
) plays a crucial role. Herein, we fabricate a theranostic nanoprobe with the function of simultaneous detection and inhibition of
P-gp
to diagnose and combat multidrug-resistant cancer in vitro and in vivo. For constructing the nanoprobe, elacridar modified quantum dots (QDs-
Ela
), acting as a gatekeeper, are grafted onto the doxorubicin (DOX) loaded, folic acid (FA) decorated mesoporous silica nanoparticles (MSNs). Upon targeted uptake by multidrug-resistant cancer cells, Bel-7402/ADR are used as a model, the acidic environment results in QDs-
Ela
removal from the nanoprobe, and subsequent DOX release. The removed QDs-
Ela
could specifically combine with
P-gp
in the cancer cell membrane and inhibit their active sites, which prevents the efflux of intracellular DOX and increases the retention of DOX. Another way, the fluorescence intensity of the binding QDs-
Ela
quantifies the
P-gp
expression level. Subsequently, in vitro and in vivo experiments both demonstrate the enhanced multidrug-resistant cancer therapy efficacy, i.e., nanoprobe has 10 times better curative effect than free DOX. In addition, due to the conjugation of FA, the nanoprobe exhibits a selective cell targeting ability to Bel-7402/ADR cells. This nanoplatform paves a new avenue for the accurate treatment of multidrug-resistant cancers.
...
PMID:Theranostic Nanoprobe Mediated Simultaneous Monitoring and Inhibition of P-Glycoprotein Potentiating Multidrug-Resistant Cancer Therapy. 3140 76
