A61K49/0021

Mitochondria-Targeted Polypeptide, Preparation Method thereof, and Use thereof
20230041271 · 2023-02-09 ·

Disclosed are a type of mitochondria-targeted polypeptides, the preparation method and the uses thereof. The polypeptide is abbreviated as MTP. The synthesis method of the present disclosure is simple, and the mitochondria-targeted polypeptide prepared by the method can specifically target the mitochondria of cells and are basically non-toxic to cells. In addition, these synthesized polypeptides demonstrate good cell-membrane-penetrating properties, and can conveniently undergo further multi-functional derivation and modification, thereby providing a potential delivery tool for the preparation of a mitochondria-targeted medicament.

RNA interference agents for GST-PI gene modulation

This invention provides compounds, compositions and methods for modulating the expression of human GST-π using RNA interference. The RNA interference molecules can be used in methods for preventing or treating diseases such as malignant tumor. Provided are a range of siRNA structures, having one or more of nucleotides being modified or chemically-modified. Advantageous structures include siRNAs with 2′-deoxy nucleotides located in the seed region, as well as other nucleotide modifications.

BENZOPYRYLIUM COMPOUNDS

Compounds used as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.

Thrombus imaging aptamers and methods of using same

Provided herein are imaging agents, antidotes to the imaging agents and methods of using the same to image a thrombus or blood clot or thrombin including sites of thrombin accumulation and to diagnose and treat thrombosis. The imaging agents include an aptamer capable of binding the thrombus or thrombin in particular linked to a reporter moiety. The imaging agents may be used to label the thrombus or sites of thrombin accumulation. Antidotes capable of binding to the aptamer in the imaging agent are also provided. The antidotes may further be linked to a quencher capable of quenching the reporter moiety.

Mechanical opening of lipid bilayers by molecular nanomachines

Embodiments of the present disclosure pertain to methods of opening a lipid bilayer by associating the lipid bilayer with a molecule that includes a moving component capable of moving (e.g., rotating) in response to an external stimulus; and exposing the molecule to an external stimulus before, during or after associating the molecule with the lipid bilayer. The exposing causes the moving component of the molecule to move and thereby open the lipid bilayer (e.g., by pore formation). The external stimuli may include an energy source, such as ultraviolet light. The opened lipid bilayer may be a component of cell membranes in vitro or in vivo. The opening of the lipid bilayer may allow for the passage of various materials (e.g., active agents, such as peptide-based drugs) through the lipid bilayer and into cells. Additional embodiments of the present disclosure pertain to the aforementioned molecules for opening lipid bilayers.

NEW COMPOUND FOR PHOTODYNAMIC THERAPY OF CANCER, COMPOSITION INCLUDING SAME, AND METHOD FOR PHOTODYNAMIC THERAPY OF CANCER
20230015033 · 2023-01-19 ·

The present disclosure relates to a novel compound for photodynamic therapy of cancer, a composition including the same, and a method for photodynamic therapy of cancer, and more specifically, a novel photosensitizer compound based on Nplmidazole having a C═S functional group introduced, a composition and sensor including the same and a method for photodynamic therapy using the same.

Coelenterazine analogues

Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.

Cryptate compounds

Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds. ##STR00001##

Compositions and methods for stabilizing coelenterazine and analogs and derivatives thereof

Provided herein are compositions and methods for stabilizing coelenterazine and analogs or derivatives thereof, and for improving the solubility and reconstitution efficiency of coelenterazine and analogs and derivatives thereof.

COMPOUND OR SALT THEREOF

The present invention relates to a compound represented by the following General Formula (1) or a salt thereof.

##STR00001##

In General Formula (1), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R.sup.1 and R.sup.2 may be bonded to each other to form a ring. R.sup.3 and R.sup.4 may be bonded to each other to form a ring. R.sup.1 and/or R.sup.2 may be bonded to a 6-membered ring to which —NR.sup.1R.sup.2 is bonded to form a ring. R.sup.3 and/or R.sup.4 may be bonded to a 6-membered ring to which —NR.sup.3R.sup.4 is bonded to form a ring. R.sup.5 represents —.sup.11CH.sub.3, a linear or branched alkyl group which may have a substituent or the like. R.sup.6 represents —F, —.sup.18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.