The present invention provides novel compounds that induce selective polo-like kinase 1 (PLK1) degradation. Specifically, the present invention provides a bifunctional compound in which a PLK1 binding moiety and an E3 ubiquitin ligase-binding moiety are linked by a chemical linker. The present invention provides the compound, a method for preparing the same, and the use thereof. The compounds may be effectively utilized for preventing or treating PLK1 related diseases.

A compound of the formula (II); a pharmaceutical composition comprising same; and methods for treating a fibrotic disease in a subject.

The present disclosure pertains to the technical field of immunotherapy or disease prevention and treatment with vaccines, in particular to a heterocyclic compound containing two or more sulfur atoms and an application thereof in preparing a nano-vaccine. Provided is the application of the heterocyclic compound containing at least two sulfur atoms and capable of being covalently or non-covalently linked to a polypeptide in preparing the nano-vaccine. A nanoparticle prepared by self-assembly of the compound and an antigen can enter the dendritic cytoplasm in nonendocytic pathway, thereby improving the uptake efficiency of the antigen and an immune adjuvant. In the process of entering a cell, the nano-vaccine can effectively avoid or reduce biodegradation of the antigen or nucleic acid adjuvant caused by enzymes in lysosomes, and therefore the nano-vaccine can efficiently activate the dendritic cells and improve the cross-presentation of the antigen, thereby effectively activating CD8+ T cells and promoting T cell proliferation. Therefore, the nano-vaccine can prevent tumor cell proliferation and virus infection by efficient immune activation and immune regulation.

The present disclosure relates generally to compositions of synthetic bifunctional molecules comprising a first domain that specifically binds to a target ribonucleic acid and a second domain that specifically binds to a target polypeptide, and uses thereof.

Described herein is a composition and method of treating COVID-19 with lipid-peptide fusion antiviral therapy. Also described is a composition and method of treating Ebola with lipid-peptide fusion antiviral therapy.

The present invention relates to a conjugate having the formula (I):

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wherein a receptor binding molecule (RBM) is connected with a camptothecin moiety (C). The present invention also relates to intermediates for producing the same, methods of preparing the same, pharmaceutical compositions comprising the same, as well as uses thereof.

Provided herein are heterobifunctional compounds which find utility as modulators of targeted ubiquitination. Also provided herein are pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds, and compositions in the treatment of various diseases, conditions, or disorders.

Disclosed herein are linker architectures for conjugates that do not rely on the SAR of the cleavable trigger or the large steric bulk of a closely positioned antibody to alter payload release. These linkers are expected to reduce off-target payload release facilitated by extracellular cathepsins, and may also be applicable to conjugates of antibody fragments that lack the steric protection from a full antibody. In addition, the linkers disclosed herein are expected to provide more selective intracellular payload release. Thus, these linkers can function synergistically with the targeting vector to confer differential payload release rates in vivo that improve the selectivity of intracellular payload release and reduce off target toxicity.

The invention discloses use of a conjugate of polyethylene glycol and a local anesthetic in non-anesthetic analgesia. A local anesthetic is prepared into a prodrug or a sustained release preparation, wherein a high molecular polymer such as polyethylene glycol in the prodrug is covalently bonded with a local anesthetic, and auxiliary materials with a sustained release effect in the sustained release preparation are non-covalently bonded to the local anesthetic. After administration, there is no anesthesia and analgesic effect before the release of the free local anesthetic. After the free local anesthetic is released, an analgesic effect is achieved. And the prodrug or the sustained-release preparation of the local anesthetic of the present invention releases the drug slowly, and renders the drug concentration kept stable and long-lasting in the effective concentration range of non-narcotic analgesia, and the long-acting non-anesthetic analgesic effect can be achieved while significantly reducing the clinical adverse reactions of local anesthetics and reducing the number of administrations. The effectiveness of the drug is greatly enhanced and the clinical application range of local anesthetics is expanded.

A method of synthesizing a pharmacological compound substance by attaching a psychoactive base substance to an amino acid and creating a prodrug with modified pharmacological behavior. A prodrug made by the method. A pharmaceutical composition comprising a prodrug of a psychoactive base substance attached to an amino acid and a pharmaceutically acceptable salt.