7 results about "Bioconjugation" patented technology

This invention discloses a selenylamide-based hydrogenation reaction of acetylacetamide compounds and its application in the modification of selenium-containing peptides and proteins, belonging to the fields of organic chemistry and chemical biology. The reaction involves the reaction of a selenium-containing compound with an acetylacetamide compound in a solvent with the addition of an additive. The applications of this reaction include: 1) selective modification and labeling of selenocysteine ​​in peptides and proteins; 2) cyclization reactions of selenium-containing peptides and selenoproteins; and 3) sequential modification of selenium-containing peptides in the presence of cysteine ​​by precise pH control combined with the hydrogen sulfide reaction of acetylacetamide. This reaction has advantages such as mild conditions, simple operation, fast reaction rate, high yield, good stability, and good selectivity. It provides a new and robust approach for the selective modification and labeling of selenium groups in bioconjugations, peptides, and / or proteins, and also provides a new method for the construction of cyclic peptides, offering a powerful tool for the development of selenium-containing peptide drugs.

The invention relates to compounds of general structure (1): Q-(L1)n-(L2)o-(L3)p-(L4)q-D (1), wherein Q is a click probe; D is a cytotoxin containing an enediyne moiety; L1, L2, L3 and L4 are each individually linkers that together link Q to D; n, o, p and q are each individually 0 or 1, provided that n+o+p+q=1, 2, 3 or 4, wherein D comprises a functional moiety (21):wherein R12=C1-3-alkyl, the wavy line indicates the connection to the remainder of the cytotoxin, and wherein D is conjugated to (L4)q by replacing the amine H atom, and to conjugates obtainable by reacting the compound according to the invention with a protein comprising a click probe F capable of reacting with click probe Q in a click reaction. The invention further relates to a bioconjugate according to general structure (2): Pr-[(L6)-Z-(L1)n-(L2)o-(L3)p-(L4)q-D]xx (2), wherein Z is a connecting group that is formed in a click reaction, L6 is a linker that links Z to Pr and Pr is a (glyco)protein.

The present invention relates generally to the field of bioconjugation. More particularly, the present invention relates to trivalent phosphonates and their use as reducing disulfide heavy bridging agents. Accordingly, the present invention relates to compounds selected from the group consisting of compounds of formula (la) and (lb), conjugates obtained by linking these compounds to another moiety, methods of modifying disulfide containing compounds using compounds selected from the group consisting of compounds of formula (la) and (lb), and compounds obtained by such methods.

Anionically functionalized polypeptides, methods of making same, and uses thereof. Anionically functionalized polypeptides comprise one or more anionic group(s), where each anionic group is covalently bound to an anionically functionalized polypeptide sidechain or N-terminus, and one or more cleavable group(s). Anionically functionalized polypeptides can be made by reaction of a bioconjugation reagent comprising one or more anionic group(s) with a polypeptide, which may be a modified polypeptide. Anionically functionalized polypeptides can be used, in various examples, to intracellularly deliver a polypeptide, in cell transfection methods, or in treatment methods.

The present invention involves the conjugation of tubulysin derivatives (analogs) to cell-binding molecules via branched (side chain) linkers, with the resulting conjugates having better pharmacokinetic properties and thus enabling more precise targeting and killing of diseased cells. The present invention also relates to methods for synthesizing the conjugates of tubulysin analogs to cell-binding agents and the molecules involved therein, as well as targeted treatment of cancer, infectious diseases, and autoimmune diseases using the conjugates. Conjugates of tubulysin with long branched linkers extend half-life during targeted delivery and minimize exposure to non-target cells, tissues, or organs in the blood circulation, thereby reducing off-target toxicity.

Provided are component polypeptides for Antibody Cage (AbC) nanostructures. The nanostructures may have 04, D2, T4, T8, or 15 architecture. Further provided are Fc-binding polypeptides that include a Z domain with defined amino acid substitutions relative to a reference Z domain. The amino acid substitution or substitutions may be D6E, S9N, N16H, M17L, N21T, A23E, G27A, T40A, or A50N, or a combination thereof, or other disclosed amino acid substitutions and combinations. The component polypeptides may be modified to enhance Fc affinity, reduce internal disulfide formation, and / or enable bioconjugation of the nanostructure. Further provided are AbC nanostructures, polynucleotides encoding the component polypeptides or nanostructures, delivery vehicles, pharmaceutical compositions, host cells, methods of making, methods of use, and other embodiments.