14 results about "Membrane associated" patented technology

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain biarylamide compounds of formula (I) (also referred to herein as "BAA compounds") which inhibit Protein Kinase, Membrane Associated Tyrosine / Threonine 1 (PKMYT1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKMYT1 kinase; to treat disorders (e.g., diseases) that are ameliorated by the inhibition of PKMYT1 kinase; to treat a proliferative disorder, cancer, etc.

The invention provides a compound capable of being used as a membrane-related tyrosine and threonine specific cdc2 inhibitory kinase PKMYT1 inhibitor, and a pharmaceutical salt and application thereof. The structure of the compound is shown as a formula (I).

The present application discloses PLPC-DB, an ultrapurified phospholipoproteomic composition derived from the supernatant of peripheral blood mononuclear cells (PBMCs). It comprises essential phospholipids, bioactive proteins, regulatory peptides, and intercellular signaling factors. The composition exceeds 99% purity through a multi-stage purification process combining high-speed centrifugation and selective ultrafiltration (1-50 kDa), followed by lyophilization. This process ensures structural stability for ≥24 months and inter-batch variability <2%. PLPC-DB supports reproducibility and molecular integrity in research and diagnostic settings. Key components include phosphatidylcholine and phosphatidylserine for membrane stabilization and intracellular signaling; structural and regulatory lipids for membrane biogenesis and immune-relevant components involved in antigen presentation, cytokine modulation, and membrane-associated signaling. These may include structurally defined molecules compatible with immunological evaluation in experimental and non-therapeutic settings. The composition is formulated for bioaccessible delivery via sublingual, endonasal, transdermal, and injectable routes, and is intended exclusively for non-therapeutic use in experimental and translational models.

This invention discloses lysosome-targeting chimeras based on different ratios and molecular weights, their preparation methods, and applications, belonging to the field of biomedical technology. Lysosome-targeting chimera (LYTAC) molecules contain target protein ligands, linkers, and lysosome-targeting receptor ligands. The core of this invention lies in systematically regulating the molecular weight ratio (range 1:1 to 1:10) between the target protein ligand and the lysosome-targeting receptor ligand, as well as the total molecular weight of LYTAC (range 1000 Da to 5000 Da), to obtain a series of LYTAC molecules with different properties. This invention provides a method for preparing the LYTAC molecules via chemical coupling. Experiments show that by optimizing the above parameters, the LYTAC molecules prepared by this invention can significantly improve the degradation efficiency and specificity of extracellular and membrane-associated target proteins (such as PD-L1, EGFR, etc.), while optimizing their pharmacokinetic properties, showing broad application prospects in the treatment of cancer, neurodegenerative diseases, and other fields.

The present disclosure relates to a PKMYT1 inhibitor compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, and use thereof in preventing or treating a PKMYT1-related disease. X1 to X5, R1 to R4, R7, and R8 in formula (I) are as defined in the specification.

A protein-based probe for detecting the presence of one of two distinct states of a target membrane-associated molecule by means of polarization microscopy is disclosed. The probe contains an anchoring moiety consisting of at least one lipidated peptide and / or at least one transmembrane α-helical peptide, a peptide linker moiety having the length of at least 5 amino acids, wherein at least 50% of the amino acids forming the linker are selected from glycine, serine, and threonine, a fluorescent moiety, and an affinity binding moiety capable of binding the target membrane-associated molecule. The moieties are arranged in the order a-b-c-d or d-c-b-a in the direction from the N-terminus to the C-terminus. Methods of detecting presence or absence of the target molecule, detecting activated or inactive forms of the target molecule, and detecting the activation of the target molecule are also described.

Disclosed herein are bifunctional compounds comprising targeting moieties for binding protein kinases, membrane associated tyrosine / threonine 1 (PKMYT1), pharmaceutical compositions thereof, and methods of treating disorders or diseases associated with PKMYT1, such as cancer.

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain biarylamide compounds of formula (I) (also referred to herein as "BAA compounds") which inhibit Protein Kinase, Membrane Associated Tyrosine / Threonine 1 (PKMYT1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKMYT1 kinase; to treat disorders (e.g., diseases) that are ameliorated by the inhibition of PKMYT 1 kinase; to treat a proliferative disorder, cancer, etc.

A method for treating a cancer in a subject, the method comprising administering a therapeutically effective amount of a membrane- associated tyrosine and threonine-specific cdc2-inhibatory kinase (Myt1) inhibitor, wherein the cancer comprises a truncating biallelic loss- of-function mutation in FBXW7 is disclosed. In a preferred embodiment, the Myt1 inhibitor is a compound of Formula (I). TheMyt1 inhibitors may bee used in combination with other therapeutic agents. Such agents include Wee 1l inhibitor, Fen 1 inhibitor, Top 1 inhibitor, Rrm1 inhibitor, Rrm2 inhibitor, Aurkb inhibitor, Top2A inhibitor, ATR inhibitor, Ttk inhibitor, Sod 1 inhibitor, Sod2 inhibitor, Bub 1 inhibitor, Cdc7 inhibitor, Sae 1 inhibitor, Plk1 inhibitor, Uba2 inhibitor, Out inhibitor, Hdac3 inhibitor, Chek1 inhibitor, Aurka inhibitor, Men 1 inhibitor, Dot 1 I inhibitor, Crebbp inhibitor, Ezh2 inhibitor, Plk4 inhibitor, Haspin inhibitor, Mettl3 inhibitor, nucleoside analog, platinum-based DNA damaging agent, or a combination thereof.

The invention provides a multi-drug-resistant acinetobacter baumannii recombinant vesicular subunit vaccine and application thereof. The subunit vaccine takes an acinetobacter baumannii bilayer membrane vesicle (BBV) as a delivery carrier and a self-adjuvant; the surface of the double-layer membrane vesicle of the acinetobacter baumannii is loaded with three antigen components: an outer membrane protein A (OmpA) of the acinetobacter baumannii, an outer membrane protein W (OmpW) of the acinetobacter baumannii and an outer membrane protein 22 (Omp22) of the acinetobacter baumannii. According to the invention, the limitation of the traditional single target vaccine is broken through, the BBV is used for providing a membrane-related antigen, three core outer membrane proteins of OmpA, Omp22 and OmpW are combined, and pathogenic key links such as multi-dimensional targeting bacterial adhesion, biomembrane formation, drug resistance and the like are realized. On the basis of the natural strain adaptability of the BBV and the high conservative property of the three proteins, the antibody generated through induction after vaccine immunization can be subjected to cross recognition with at least 10 different serotype multi-drug-resistant strains, the protection range is greatly widened, and the problem that an existing vaccine is prone to failure due to antigen variation is solved.

The invention provides methods for treating and selecting cancer patients for therapy using a compound that modulates mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) activity, such as inhibiting MALT1 scaffolding activity.