C07K5/1019

CYCLIN BASED INHIBITORS OF CDK2 AND CDK4

Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

GLYCOPEPTIDE FOR CONTRAST AGENT TARGETING CANCER CELLS AND CONTRAST AGENT KIT CONTAINING THE SAME

The present disclosure relates to a glycopeptide targeting cancer cells and a contrast agent kit containing the same. The glycopeptide is one wherein an azide reporting monosaccharide is bound to a substrate peptide. As the substrate peptide is specifically cleaved by cathepsin B in cancer cells, an azide reporting monosaccharide is expressed onto the cell surface via metabolic glycoengineering, thereby providing a target for action as a contrast agent. Accordingly, because the azide is exposed to the cell surface only by cathepsin B, as it is specifically expressed in cancer cells, in particular in metastatic cancer cells, while it is limitedly expressed in normal cells and is hardly excreted out the cells, the cancer cells can be selectively imaged by an azide-specific contrast agent.

Tunable control of protein degradation in synthetic and endogenous bacterial systems

The methods and compositions described herein relate, in part, to the generation of a synthetic degradation system in E. coli that provides tunable control of the protein level of targeted genes by using components of the Mesoplasma florum tmRNA system. Provided herein are degradation tag variants that permit independent control of both the initial level and inducible degradation rate of attached proteins.

ANALOGS THAT TARGET MITOCHONDRIAL DISEASES
20220041654 · 2022-02-10 ·

Disclosed are analogs of elamipretide (MTP-131). The compounds are useful for the treatment and prevention of ischemia-reperfusion injury (e.g., cardiac ischemia-reperfusion injury) or myocardial infarction.

SERINE DERIVATIVE COMPOUND FOR THE PREVENTION OR TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES

The present invention relates to a serine derivative compound having improved blood-brain barrier (BBB) permeability and the use thereof, and more particularly, to a novel serine derivative compound having improved blood-brain barrier permeability compared to L-serine, and a pharmaceutical composition for preventing, treating or alleviating nervous system diseases such as cognitive disorder, intellectual disability, microcephaly, epilepsy, neurodevelopmental disorder, dementia, autism spectrum disorder, Down's syndrome, Rett's syndrome, fragile X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis, the pharmaceutical composition containing the compound as an active ingredient. The compound of Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient for the pharmaceutical composition for preventing or treating central nervous system diseases according to the present invention exhibits significantly improved blood-brain barrier permeability, activates neuronal cell proliferation, and exhibits a neuronal protective effect of inhibiting neuronal cell death resulting from mitochondrial membrane potential damage and/or endoplasmic reticulum stress caused by oxidative stress, and exhibits improved blood-brain barrier permeability. Therefore, the compound has an excellent effect on the prevention, treatment and alleviation of central nervous system diseases such as cognitive disorder, intellectual disability, microcephaly, epilepsy, neurodevelopmental disorder, dementia, autism spectrum disorder, Down's syndrome, Rett's syndrome, fragile X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis, and thus is a highly useful invention in the pharmaceutical industry, the food industry and the livestock industry.

Metal compound having phase transformation and method of preparing the same
11396453 · 2022-07-26 · ·

The present invention relates to a metal phase transformation compound and a method for preparing the same.

RESIN FILM FORMED OF SCAFFOLD MATERIAL FOR CELL CULTURE, CARRIER FOR CELL CULTURE AND CONTAINER FOR CELL CULTURE

Provided is a resin film formed of a cell culture scaffold material, which has excellent fixation of cells after seeding and is capable of enhancing proliferation rate of cells. A resin film formed of a cell culture scaffold material, in which the cell culture scaffold material contains a synthetic resin, and the resin film has phase-separated structure including least a first phase and a second phase, and a ratio of the surface area of one of the first phase and the second phase to the entire surface is 0.01 or more and 0.95 or less.

Peptide for inhibiting skin inflammation and composition for preventing or treating skin inflammation containing the same
11208433 · 2021-12-28 · ·

The present invention relates to a peptide for inhibiting skin inflammation and a pharmaceutical composition and a cosmetic composition for preventing or treating skin inflammation including the same. Since the peptide, pharmaceutical composition and cosmetic composition are effective for improving symptoms of skin inflammation caused by atopic dermatitis and the like, they are useful for preventing, improving or treating skin inflammation.

PEPTIDES FOR ACTIVATION OF CELL SIGNALING IN OSTEOPROGENITOR CELLS

The present invention provides compounds and pharmaceutical compositions of peptidomimetic ligands. The peptidomimetic ligands can be conjugated with phosphonate drugs. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of osteoporosis and for the promotion of bone growth due to their specificity for the α.sub.4β.sub.1 integrin on mesenchymal stem cells and for the surface of bone.

Prodrug and profluorescent compounds for selective mitochondrial imaging and therapeutic targeting

The present invention relates to the use of prodrugs susceptible to nitroreductase (NTR) activation. In particular, provided herein are mitochondria-targeting prodrug compounds and probes, including profluorescent near-infrared (NIR) probes and non-fluorescent prodrugs, as well as to methods of using said prodrug compounds and probes for imaging mitochondria and for mitochondria-specific delivery of therapeutic agents.