Biomarkers in retinoblastoma.

Retinoblastoma (RB) is the most common intraocular malignancy of childhood caused by inactivation of the genes. The prognosis of RB is better with an earlier diagnosis. Many diagnostic approaches and appropriate clinical treatments have been developed to improve clinical outcomes.

Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters.

The balance of normal anion concentrations in cells provides basis for maintaining cellular morphology and function. Disrupting the homeostasis of cellular anions and lysosomal pH, in particular with high selectivity for cancer cells over normal cells may serve as a promising approach for the treatment of cancers. Small-molecule organic compounds with transmembrane anion transport activity, namely synthetic anion transporters are able to destroy the homeostasis of cellular anions, in particular chloride anions to trigger cell death and thus may be developed as a new class of anti-tumor drugs.

Synthesis and biological evaluation of aza-crown ether-squaramide conjugates as anion/cation symporters.

Anion/cation symport across cellular membranes may lead to cell apoptosis and be developed as a strategy for new anticancer drug discovery. Four aza-crown ether-squaramide conjugates were synthesized and characterized. Their anion recognition, anion/cation symport, cytotoxicity and probable mechanism of action were investigated in details.

Fluorinated bisbenzimidazoles: a new class of drug-like anion transporters with chloride-mediated, cell apoptosis-inducing activity.

Anion transporters have attracted substantial interest due to their ability to induce cell apoptosis by disrupting cellular anion homeostasis. In this paper we describe the synthesis, anion recognition, transmembrane anion transport and cell apoptosis-inducing activity of a series of fluorinated 1,3-bis(benzimidazol-2-yl)benzene derivatives. These compounds were synthesized from the condensation of 1,3-benzenedialdehyde or 5-fluoro-1,3-benzenedialdehyde with the corresponding 1,2-benzenediamines and fully characterized.

Synthesis and properties of a lysosome-targeting fluorescent ionophore based on coumarins and squaramides.

In this paper we present the first example of a lysosome-targeting fluorescent ionophore. Specifically, we synthesized a squaramide derivative bearing a coumarin fluorophore and a morpholinyl group, and found that it was able to target and efficiently deacidify lysosomes. In contrast, an analogue without a morpholinyl group exhibits much lower ability to localize in lysosomes and is much less active in regulating the lysosomal pH.

Synthesis, anionophoric activity and apoptosis-inducing bioactivity of benzimidazolyl-based transmembrane anion transporters.

In this paper we show that a series of 1,3-bis(benzimidazol-2-yl)benzene (m-Bimbe) derivatives exhibit excellent performance as transmembrane anion transporters with anticancer activity. The transport efficiency of m-Bimbe and its derivatives has been firstly optimized by adding a strong electron-withdrawing nitro group at the 5-position of the central phenyl subunits to enhance the CH···anion interactions. Evidences for the interactions were obtained from ESI MS, spectrophotometric and H NMR titrations.

Synthesis, Anion Recognition, and Transmembrane Anionophoric Activity of Tripodal Diaminocholoyl Conjugates.

In this paper, we present the synthesis, anion recognition, and anionophoric activity of 1,3,5-tris(aminomethyl)-2,4,6-triethylbenzene-based tripodal 3α-hydroxy-7α,12α-diamino-5β-cholan-24-oate conjugate 1 and the corresponding tris(2-aminoethyl)amine-based analogue 2 and choloyl analogue 3. Their affinity toward anions was evaluated by means of competitive displacement assay using 5-carboxyfluorescein (5-FAM) as a fluorescent indicator. The results indicate compounds 1 and 2 exhibit strong recognition toward a wide range of biologically important anions, in particular, toward sulfate and phosphate anions.