C07K1/1077

Multicyclic peptides and methods for their preparation

The invention relates to methods for preparing a compound comprising a peptide attached to a molecular scaffold whereby multiple peptide loops are formed, to compounds that can be obtained with such methods and uses thereof.

GLYCOCONJUGATION PROCESS

The present disclosure relates generally to methods of preparing glycoconjugates containing a saccharide conjugated to a carrier protein by use of stable nitroxyl radical related agent/oxidant as an oxidizing agent, to immunogenic compositions comprising such glycoconjugates, and to methods for the use of such glycoconjugates and immunogenic compositions.

PROTEIN AND/OR PEPTIDE MODIFICATION MOLECULE
20220204481 · 2022-06-30 ·

An object of the present invention is to provide a technique that allows other molecules/substances to be more selectively linked to the N-terminus in a simple and efficient manner, even in natural proteins etc. This object is achieved by reacting a compound represented by formula (1) or a salt thereof, or a hydrate or solvate of the compound or a salt thereof with a protein and/or peptide.

Modified relaxin polypeptides comprising a pharmacokinetic enhancer and pharmaceutical compositions thereof

The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

PLATFORM FOR PRODUCING GLYCOPROTEINS, IDENTIFYING GLYCOSYLATION PATHWAYS
20220186276 · 2022-06-16 ·

Disclosed are components, systems, and methods for glycoprotein protein synthesis in vitro and in vivo. In particular, the disclosed components, systems, and methods relate to modular platforms for producing glycoproteins. The components, systems, and methods disclosed herein may be used in synthesizing glycoproteins and recombinant glycoproteins in cell-free protein synthesis (CFPS) and in modified cells.

Compounds and methods for selective c-terminal labeling

The present disclosure relates to compounds and methods for selective C-terminal functionalization of peptides. In certain embodiments, the compounds have improved water-solubility, and are suitable for use in connection with peptide sequencing methodologies.

A METHOD FOR FUNCTIONALIZATION OF AN AROMATIC AMINO ACID OR A NUCLEOBASE

A method for functionalization of an aromatic amino acid or a nucleobase with a fluoroalkyl-containing moiety RF, wherein the aromatic amino acid is reacted in the presence of at least one reductant with at least one hypervalent iodine fluoroalkyl reagent carrying the floroalkyl-containing moiety RF is disclosed. Novel hypervalent iodine fluoroalkyl reagents is also disclosed.

METHOD FOR MODIFYING AMINO GROUP IN MOLECULE WITH THE ZOLINIUM AND USE THEREOF
20220177515 · 2022-06-09 ·

The present disclosure relates to a method for modifying or marking an amino group in a molecule, wherein the amino group in the molecule is modified or marked with zolinium(s) shown in the following formula 1, wherein the molecule comprises amino acid ester, aminoamide, or peptide/protein. The method has advantages of economy and site selectivity, and has huge potential application value in the field such as pharmaceutical molecular synthesis, probe molecule and diagnostic marker reagent development.

ADDITIVE SYSTEMS FOR USE IN PROTEIN PEGYLATION
20220160883 · 2022-05-26 ·

The present disclosure provides an additive system for use in protein PEGylation. The additive system includes p-aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium salts such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25° C. without stirring until completion, typically within 24 hours.

FLUORINATION METHOD

The invention relates to a process for producing a compound comprising the anion [CF.sub.2.sup.18FSO.sub.2]−, which process comprises treating a difluorocarbene source with (i) a source of .sup.18F.sup.− and (ii) a source of SO.sub.2. The invention relates to a compound which comprises that anion. The invention also relates to the use of the compound comprising the anion [CF.sub.2.sup.18FSO.sub.2].sup.− to produce a compound comprising an .sup.18F-trifluormethyl functionalised aromatic group. Compounds comprising an .sup.18F-trifluoromethyl functionalised aromatic group are also the subject of the present invention.