72 results about "Molecular targeted drug" patented technology

The present disclosure describes how all-retinoic acid (ATRA) binds and inhibits Pin1 activity and induces degradation of the activated Pin1 monomer selectively in cancer cells. Identification of the binding mechanism of ATRA with Pin1 confirm ATRA binding specificity to Pin1 residues in the PPIase active site, thus demonstrating that drug-induced Pin1 ablation has potent anticancer activity, such as in acute promyelocytic leukemia (APL), by inducing PML-RARa degradation, as well as against other types of cancer and diseases that are associated with Pin1 overexpression, such as aggressive triple negative breast cancer, lupus, asthma, cocaine addiction, among others, due to their unique ability to simultaneously block numerous cancer-driving pathways, with relatively lower toxicity. The present disclosure also provides a rationale for developing sustained released ATRA-containing formulations. ATRA-containing formulations may be used in combinations with other existing therapies including chemotherapy or molecularly targeted drugs and other standard of care.

The present invention provides an antitumor agent having high safety, which is a molecular target drug against malignant tumors. An anti-malignant tumor agent characterized by containing, as an active ingredient, a substance targeting ribosomal proteins shows increased expression in malignant tumor cells. The substance of the present inventions targeting the ribosomal protein showing increased expression in the malignant tumor cell may be a substance involved in one of biological defense mechanisms which are considered to be intrinsically provided in a living body and prevent onset of disease even if cancer cells develop. Specifically, the ribosomal protein showing increased expression is RPL29 and / or RPS4X. A substance targeting RPL29 and / or RPS4X is an anti-RPL29 antibody and / or anti-RPS4X antibody, a substance capable of activating or enhancing an endogenous anti-RPL29 antibody and / or anti-RPS4X antibody in a living body, a substance capable of inducing production of the anti-RPL29 antibody and / or anti-RPS4X antibody in a living body, or an antagonist of RPL29 and / or RPS4X. Furthermore, the present invention also extends to an examination method of malignant tumors which uses the anti-RPL29 and / or anti-RPS4X antibody titer as an indicator.

The invention discloses a molecular target anticancer photosensitizer tamoxifen-phthalocyanine conjugate and its preparation method and application. The molecular target drug tamoxifen is introduced around the metal phthalocyanine macrocycle to increase the concentration of phthalocyanine. Targeting of cyanine, and linking the phthalocyanine core and tamoxifen with polyethylene glycol chains to enhance its amphiphilicity and biocompatibility. The compound is expected to improve the targeting of photosensitizers in photodynamic therapy, and at the same time may realize the dual efficacy of photodynamic therapy and molecular target therapy. The conjugate has a single structure and a definite composition. The synthesis method of the invention is simple, the raw materials are easy to obtain, the cost is low, and it is beneficial to industrialized production.