Recent Advances in RNA-Targeted Cancer Therapy.

Ribonucleic acid (RNA) plays a pivotal role in gene regulation and protein biosynthesis. Interfering the physiological function of key RNAs to induce cell apoptosis holds great promise for cancer treatment. Many RNA-targeted anti-cancer strategies have emerged continuously. Among them, RNA interference (RNAi) has been recognized as a promising therapeutic modality for various disease treatments. Nevertheless, the primary obstacle in siRNA delivery-escaping the endosome and crossing the plasma membrane severely impedes its therapeutic potential. Thus far, a variety of nanosystems as well as carrier-free bioconjugation for siRNA delivery have been developed and employed to enhance the drug delivery and anti-tumor efficiency. Besides, the use of small molecules to target specific RNA structures and disrupt their function, along with the covalent modification of RNA, has also drawn tremendous attention recently owing to high therapeutic efficacy. In this review, we will provide an overview of recent progress in RNA-targeted cancer therapy including various siRNA delivery strategies, RNA-targeting small molecules, and newly emerged covalent RNA modification. Finally, challenges and future perspectives faced in this research field will be discussed.

Effect of terminal substituent of iso-indigo-based materials on the intermolecular stacking and memory performance.

Attributed to the characteristics of narrow band gap structural units and full spectral response, iso-indigo is often used as an electron acceptor in organic electronic materials. Organic molecules with large conjugated surfaces and strong intermolecular forces can form ordered stacked structures through self-assembly. In this paper, the self-assembly performances of IDCF3 and IDCN are regulated by changing the end groups. The effects of terminal groups on the resistive memory behaviours and reproducibility are investigated. The properties of IDCF3 and IDCN devices are characterized by UV-VIS spectroscopy, cyclic voltammetry and DSC diffraction. The results show that when the end groups with different steric hindrance are introduced into the ends of the molecules with good backbone plane, the conjugated surfaces of the molecules will bend due to the different steric hindrance of the end groups in the form of cambium and layer-ordered packing, which will affect the threshold voltage and device reproducibility.

Crystal structure and luminescence spectrum of a one-dimensional nickel(II) coordination polymer incorporating 1,4-bis-[(2-methyl-imidazol-1-yl)meth-yl]benzene and adamantane-1,3-di-carboxyl-ate co-ligands.

An NiII coordination polymer, namely, poly[(µ2-adamantane-1,3-di-carboxyl-ato-κ4 O 1,O 1':O 3,O 3')[µ2-1,4-bis-(2-methyl-imidazol-1-ylmeth-yl)benzene-κ2 N 3:N 3']nickel(II)], [Ni(C12H14O4)(C16H18N4)]n or [Ni(adc)(bmib)]n, (I) [adc = adamantane-1,3-di-carboxyl-ate, C12H14O4 2- and bmib = 1,4-bis-(2-methyl-imidazol-1-ylmeth-yl)benzene, C16H18N4] was synthesized and characterized. It exhibits a one-dimensional extended structure built up from alternating [Ni2(bmib)2] 26-membered rings and [Ni2(adc)2] 16-membered rings. The nickel atom lies on a crystallographic twofold axis and both ligands are completed by mirror symmetry. The solid-state luminescence spectra of (I) and the bmib ligand show strong emissions at 442 and 410 nm, respectively.

A novel αvß3 integrin-targeted NIR-II nanoprobe for multimodal imaging-guided photothermal therapy of tumors in vivo.

Developing novel small-molecule-based probes with both deep tissue imaging and therapeutic functions is highly significant in cancer diagnosis and treatment. Herein, we report a novel second near-infrared (NIR-II) fluorescent probe QT-RGD constructed with a NIR-II emissive organic fluorophore and two cyclic-(arginine-glycine-aspartic acid) (cRGD) peptides that can specifically bind to the tumor-associated αvß3 integrin for accurate tumor diagnosis and targeting therapy. The isotopic 125I-labeled probe exhibited great tumor targeting ability and emitted intensive NIR-II/photoacoustic (PA)/single-photon emission computed tomography (SPECT) signals, which allows specific and sensitive multimodal visualization of tumors in vivo. More notably, this probe could also be applied for effective imaging-guided photothermal therapy (PTT) of tumors in mouse models owing to its prominent photothermal conversion efficiency and excellent photothermal stability. We thus envision that our work which unveils a combination of NIR-II/PA/SPECT imaging and PTT would offer a valuable means of improving tumor diagnostic accuracy as well as therapeutic efficacy.