41 results about "Cleavable linker" patented technology

The efficacy and indication of donanemab do not depend on the Fc region and are subject to transit across cell walls. They can be expanded by using their scFvs conjugated with N-methyl lobe of transferrin protein connected with an environment-sensitive cleavable linker to prevent exocytosis of the scFv yielding high exposure inside body cells such as in the brain, eye, and cancer cells that overexpress transferrin receptors.

The present disclosure provides methods of polynucleotide synthesis and compounds, compositions useful for synthesis of polynucleotides. The chemical compounds include nucleotides and their analogs that are attached to polymerase though a cleavable linker comprising an enzymatically cleavable amino acid ester.

A method for DNA synthesis using protected nucleosides is disclosed. The nucleosides may be nucleoside triphosphates or nucleoside phosphoramidites with nucleobases attached to electrochemically-cleavable linkers. Removal of a protecting group by application of a voltage in solution triggers a cyclization reaction that cleaves the electrochemically-cleavable linkers. The electrochemically-cleavable linkers may include an amide linkage and an amide that forms a lactam or an ester linkage and a protected alcohol that forms a lactone when the protecting group is removed. The voltage used to cleave the electrochemically-cleavable linkers may be generated by activation of individual electrodes on a microelectrode array. The microelectrode array can be a substrate for solid-phase synthesis of oligonucleotides. Activation of specific electrodes removes the protecting groups at those electrodes and thus enables spatially-controlled extension of the oligonucleotides. Protected nucleosides linked to protecting groups by electrochemically-cleavable linkers are also disclosed.

Compositions and methods are provided of a therapeutic nanoparticle composed of collagenase IV linked via a linker (e.g. cathepsin B cleavable linker) to ferumoxytol (iron oxide). The collagenase IV is key in the composition intended for the breakdown of the tumor wall as the collagenase. Such compositions and methods are aimed at solving at the same time two of the main challenges of current approaches in the treatment of glioblastoma multiforme (GBM) which are low specificity and poor uptake.

The application discloses a fast and efficient chemical proteomics sample preparation method, relates to the field of proteomics, and designs and synthesizes agarose microspheres coated with a cleavable linker compound. The free end of the cleavable linker compound contains an azido group, which has good compatibility with existing alkyne probes. Through one-step efficient click chemistry reaction, the probe-labeled peptide segment can be specifically captured on the surface of the agarose microspheres. Since the agarose microspheres and the peptide segment are covalently connected, very strong denaturants or surfactants can be used to wash the medium to remove non-specific adsorption as much as possible. Finally, the probe-labeled peptide segment can be efficiently dissociated from the agarose microspheres through cleavage treatment. The sample preparation method in the application simplifies the cumbersome "click chemistry and streptavidin enrichment" into one-step fast "click chemistry" reaction, and greatly simplifies the operation process.

The invention is directed to self-eliminating cleavable conjugates according to general formula (I) or (II) wherein AR is capable of an elimination reaction upon cleavage of CL.

Provided herein are cleavable linkers, pharmaceutical compositions thereof, as well as nucleic acids, and methods for making and discovering the same. The cleavable linkers described herein have improved efficacy and safety.

The present disclosure relates to multifunctional molecules comprising masked interleukin 12 and methods of making and using the same. In certain embodiments, the multifunctional molecules disclosed herein comprise a cleavable linker.

To provide a method for purifying peptides or peptide nucleic acids produced by solid-phase peptide synthesis in a way that is inexpensive and is less prone to faults, and linker molecules for use in the purification.SOLUTION: The present invention relates to linker molecules of formula (1), X-Tb-Va-U-Y-Z (1) and a method for purifying peptides using the linker molecules. The linker molecule can be coupled to a purification resin via the moiety X and to a peptide via the moiety Y under the release of the leaving group Z. T is an optional spacer moiety and V is an optional electron withdrawing moiety. U is an aryl or 5- or 6-membered heteroaryl moiety bound to at least one electron withdrawing moiety V, W, or E. The linker is stable under acidic conditions and releases the peptide upon addition of a reducing agent.SELECTED DRAWING: None

The present specification relates to conjugates comprising a linker of formula (ICA): (ICA) and their pharmaceutically acceptable salts. The specification also relates to the use of these conjugates for the treatment of diseases such as cancer, as well as intermediates useful in the synthesis of these conjugates.

The present disclosure provides multispecific antigen-binding molecules that bind both a T-cell antigen (e.g., CD3) and a target antigen (e.g., a tumor associated antigen), and which include tandem antigen-binding domains, and uses thereof.

This invention relates to a branched, enzyme-cleavable linker-payload and a method for its efficient production.

The present disclosure provides multispecific antigen-binding molecules that bind both a T-cell antigen (e.g., CD3) and a target antigen (e.g., a tumor associated antigen), and which include tandem antigen-binding domains, and uses thereof.

Disclosed herein, inter alia, are silicon containing cleavable linkers and compounds for use in nucleic acid sequencing.

The present disclosure provides tumor-specific cleavable linkers and their use in drugs and prodrugs for delivering therapeutics to a tumor cell environment. The present disclosure also provides cleavage products of said drugs and prodrugs, and methods related to the use of the same.

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a —S(═O)(═N—)— functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and / or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

Disclosed herein, inter alia, are compounds, compositions, and methods of use thereof for sequencing a nucleic acid.

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and / or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

The present disclosure relates generally to cleavable linkers and uses thereof.SOLUTION: A multi-targeted molecule comprising at least two effector molecules, wherein said effector molecules are linked together via an endosomal cleavable linker or a protease cleavable linker, wherein said linker is a carbohydrate linker, and wherein said linker is cleaved at least 1.25 times faster in cells (or under in vitro conditions selected to mimic intracellular conditions) as compared to blood or serum (or under in vitro conditions selected to mimic extracellular conditions).SELECTED DRAWING: None

The invention relates generally to multispecific polypeptides having constrained CD3 binding. In some embodiments, components of the multispecific polypeptides are connected by a non-cleavable linker. Also provided are methods of making and using these multispecific polypeptides in a variety of therapeutic, diagnostic and prophylactic indications.

The specification relates to conjugates of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates the use of the conjugates for the treatment of diseases such as cancer, and intermediates useful for the synthesis of the conjugates.

The efficacy and indication of belimumab do not depend on the Fc region and are subject to transit across cell walls. They can be expanded by using their scFvs conjugated with N-methyl lobe of transferrin protein connected with an environment-sensitive cleavable linker to prevent exocytosis of the scFv yielding high exposure inside body cells such as in the brain, eye, and cancer cells that overexpress transferrin receptors

The present disclosure provides a particulate delivery system comprising an extracted yeast cell wall comprising beta-glucan and a pro-payload molecule comprising a payload scaffolding molecule operably and reversibly linked to a payload molecule through a cleavable linker. The disclosure further provides methods of making and methods of using the particulate delivery system.

The present disclosure is concerned with chemical release agents containing a release trigger (e.g., a benzisoxazole), a polymeric element, and an active agent such as, for example, a radioligand, a residue of a peptide, a residue of a protein, a residue of an oligonucleotide, or a residue of a small molecule therapeutic agent, containing the compounds, and methods for using the same. Also disclosed are intermediate compounds useful in the preparation of chemical release agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Provided herein are dye-drug conjugate (DDC) compounds comprising: a tumor-targeting near-infrared dye; a chemotherapeutic drug; and a cleavable linker, and methods of use thereof.

The present specification relates to conjugates comprising a linker of formula (IA) and pharmaceutically acceptable salts thereof. The specification also relates to the use of these conjugates for the treatment of diseases, such as cancer, and intermediates useful in the synthesis of these conjugates. IA

This disclosure relates to a multifunctional molecule containing a shielding interleukin 12, and to methods for fabricating and using the same. In certain embodiments, the multifunctional molecule disclosed herein includes a cleavable linker.

The present specification relates to conjugates comprising a linker of formula (IA): and pharmaceutically acceptable salts thereof. The specification also relates to the use of these conjugates for the treatment of diseases such as cancer, as well as intermediates useful in the synthesis of these conjugates.

The efficacy and indication of Aducanumab do not depend on the Fc region and are subject to transit across cell walls. They can be expanded by using their scFvs conjugated with N-methyl lobe of transferrin protein connected with an environment-sensitive cleavable linker to prevent exocytosis of the scFv yielding high exposure inside body cells such as in the brain, eye, and cancer cells that overexpress transferrin receptors