A61K47/6855

OLIGONUCLEOTIDE CONJUGATES AND PREPARATION AND APPLICATIONS THEREOF

The present invention relates to oligonucleotide conjugates and preparation and applications thereof. In particular, the present invention relates to an oligonucleotide conjugated to a biomolecule (e.g. an antibody) and/or an agent of interest (e.g. a drug). In certain embodiments, the oligonucleotide of the present invention is a hybridized complex of a single strand oligonucleotide carrying a biomolecule and a complementary strand oligonucleotide bearing an agent of interest where the hybridized nucleotide segment acts as a linker to link the biomolecule and the agent of interest in one molecule.

Antibody-drug-conjugate and its use for the treatment of cancer

The present invention relates to an antibody-drug-conjugate. From one aspect, the invention relates to an anti-body-drug-conjugate comprising an antibody capable of binding to a Target, said antibody being conjugated to at least one drug selected from derivatives of dolastatin 10 and auristatins. The invention also comprises method of treatment and the use of said anti-body-drug-conjugate for the treatment of cancer.

Monoclonal antibodies against HER2 epitope and methods of use thereof

This invention provides fully human monoclonal antibodies that recognize HER2. The invention further provides methods of using such monoclonal antibodies in a variety of therapeutic, diagnostic, and prophylactic indications.

Pyrrolobenzodiazepine antibody conjugates

A conjugate of formula I:
L-(D.sup.L).sub.P  (1) wherein L is a Ligand unit, D.sup.L is a Drug Linker unit of formula II: ##STR00001## wherein either: (a) R.sup.10 and R.sup.11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (b) R.sup.11 is OH, and R.sup.10 is: ##STR00002## p is an integer of from 1 to 20.

Multi-drug-loading-site, high drug-loading capacity ligand-drug conjugate

The present invention provides a multi-drug-loading site and high drug-loading capacity ligand-drug conjugate. The ligand-drug conjugate has a structure of general formula (I). The ligand-drug conjugate has the characteristics of high loading capacity, high drug efficacy, low toxicity, and low risks. The ligand-drug conjugate can be used particularly to connect to a low toxicity chemical molecule, thereby extending a therapeutic window. Furthermore, the present invention provides an antibody-drug conjugate molecule. The antibody-drug conjugate molecule has the characteristics of multiple drug-loading ability and high drug-loading capacity, such that the antibody-drug conjugate can carry a large amount of a low toxicity chemical molecule and achieve a therapeutic effect without depending on antibody targeting or high toxicity chemicals.
TM-{R.sup.2-PEG1-[R.sup.1-PEG2-(R.sup.3-A′-D).sub.n].sub.m}.sub.l  (I

CYSTEINE ENGINEERED ANTIBODY-DRUG CONJUGATES WITH PEPTIDE-CONTAINING LINKERS
20230021500 · 2023-01-26 ·

The present disclosure relates generally to cysteine engineered antibody-drug conjugates comprising peptide-containing linkers and to methods of using these conjugates as therapeutics and/or diagnostics.

ENZYME-MEDIATED DEPLETION OF ADENOSINE AND/OR METHYLTHIOADENOSINE

Methods and compositions related to the engineering of a protein with MTA/ADO-degrading enzyme activity are described. For example, in certain aspects there may be disclosed an MTase capable of degrading MTA/ADO. Furthermore, certain aspects of the invention provide compositions and methods for the treatment of cancer or SCID with an MTase using the disclosed proteins or nucleic acids.

METHODS FOR THE PREPARATION OF BIOCONJUGATES

A surfactant for a bioconjugation reaction is disclosed, wherein a biomolecule comprising one or more azide moieties is connected to an cyclic alkyne comprising payload. More specifically, the invention concerns a method for the preparation of a bioconjugate of structure B—(Z—L—D).sub.x (1), comprising reacting (i) an alkyne or alkene compound of structure Q—L—D (2), wherein Q is a click probe comprising a cyclic alkyne moiety or a cyclic alkene moiety, L is a linker, and D is a payload; with (ii) a molecule of structure B—(F).sub.x (3), wherein B is a biomolecule that is functionalized with x click probes F; F is a click probe capable of reacting with Q, and x is an integer in the range of 1-10, in presence of a surfactant.

Antibody drug conjugates (ADC) that bind to 191P4D12 proteins

Antibody drug conjugates (ADC's) that bind to 191P4D12 protein and variants thereof are described herein. 191P4D12 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, the ADC's of the invention provide a therapeutic composition for the treatment of cancer.

Antibody conjugates and methods of making the antibody conjugates

Described herein are antibody conjugates and methods of making antibody conjugates.