Synthesis, molecular structure, and validation of metalloprobes for assessment of MDR1 P-glycoprotein-mediated functional transport

Abstract

molecular imaging of the functional transport activity of MDR1 Pgp (ABCB1) with (67/68)Ga-metalloprobes could enable non-invasive monitoring of the blood-brain barrier, tumors, and tissues in vivo.

A Folate Receptor-Targeting Nanoparticle Minimizes Drug Resistance in a Human Cancer Model

“…22, 23 As shown in Fig. 1a, both KB-3-1 and KB-8-5 cell lines express membrane-bound folic acid receptor (FR), the potential target of HFT-T nanoparticle.…”

“…32, 33 On the contrary, FR has been found to be highly expressed in a wide range of solid tumors, including ovarian, uterine, lung, breast, and head and neck cancers. 23, 28 These properties make folate an excellent tumor-targeting moiety in the design of multi-functional nanoparticles. 34 It worth noting that although the accumulation of HFT-T in the liver and kidney were relatively high, no obvious tissue damage was observed in any of the organ samples collected from any treatment group, including HFT-T and HT-T. Several facts may be account for the low acute in vivo toxicity of HFT-T under the tested conditions: 1) low FR expression in normal tissues when compared with that in tumors.…”

Drug Efflux Transporters and Multidrug Resistance in Acute Leukemia: Therapeutic Impact and Novel Approaches to Mediation

“…A novel technique, i.e., reverse-phase protein microarray assays, for identification of MDR leukemia cells on the basis of Akt1 activity or phosphorylation was reported, with higher Akt1 activity being demonstrated in MDR cells (Maraldi et al, 2011). Other novel techniques studied for assessment of P-gp-mediated transport activity include the use of gallium-labeled metalloprobes (Sivapackiam et al, 2010) and single-photon emission computed tomography with other radiolabeled metal complexes (Piwnica-Worms and Sharma, 2010).…”

Radiosynthesis and Biological Evaluation of 68Ga-Labeled Colchicine Conjugates

“…These cells are reported not to express any detectable levels of Pgp. 25,26 Cells were cultured in DMEM containing 10% fetal calf serum, 100 U/mL penicillin, 50 lg/mL streptomycin in humidified atmosphere under 5% CO 2 at 37°C. The harvested cells from confluent flasks were washed and a cell suspension of 1 · 10 6 cells/mL was prepared in plain DMEM.…”