A conjugated cationic dendrimer comprising end groups conjugated to charge-shielding groups, wherein some charge-shielding groups are chemically linked to active pharmaceutical ingredients.

Disclosed herein is are conjugates that comprise a ubiquitin dimer or multimer, comprising a distal moiety conjugated to a proximal moiety. The distal moiety comprises a polypeptide comprising a distal ubiquitin at its C-terminus, said ubiquitin comprising at least one of the following mutations: K6X, K11X, K27X, K29X, K33X, K48X, K48X, K63X, or K63X, where X is selected from R, A or C. The proximal moiety comprises a polypeptide comprising either a proximal ubiquitin at its C-terminus or a proximal ubiquitin at its N-terminus; said ubiquitin comprising a blocked C-terminus. The distal moiety is conjugated to the proximal moiety via an amide bond from G76 of the distal ubiquitin to one of M1, K6, K11, K27, K29, K33, K48, or K63 of the proximal ubiquitin. Also provided are methods for the production of said conjugates, formulations comprising said conjugates and methods of using said conjugates.

An antiviral agent is provided, having a phosphorodiamidate morpholino oligomer with an antisense sequence to a portion of a genome of a strain of a coronavirus. The coronavirus may be SARS-CoV-2 or another βCoV. The antiviral agent finds many uses, such as in a pharmaceutical composition, a method of treating coronavirus-mediated disease, a method of preventing coronavirus-mediated disease, a method of reducing or preventing the replication of coronavirus in a host cell, a method of controlling the spread of coronavirus in donated tissue, a treated tissue sample, and in the manufacture of a medicament for the treatment or prevention or coronavirus-mediated disease.

Provided herein is a dendrimer comprising: i) a core unit (C); and ii) building units (BU), wherein the core unit is covalently attached to at least two building units; the dendrimer having from two to six generations of building units; wherein building units of different generations are covalently attached to one another; and the dendrimer further comprising: iii) one or more first terminal groups attached to an outermost building unit, wherein each first terminal group comprises a radionuclide-containing moiety; and iv) one or more second terminal groups attached to an outermost building unit, wherein each second terminal group comprises a pharmacokinetic-modifying moiety; or a salt thereof. Also provided are compositions comprising the dendrimers, and methods of using the dendrimers and compositions in diagnostic and therapeutic applications.

Disclosed herein are compositions and methods for reducing the antigenicity of molecules. The antigenicity of a molecule may be reduced or eliminated by conjugating at least one branched polymer to the molecule to form a molecule-polymer conjugate. The branched polymer may include a backbone and a plurality of side chains, each side chain covalently attached to the backbone.

The present invention relates to the technical field of medicines, and relates to a polyethylene glycol conjugated drug, a preparation method therefor and the use thereof. In particular, the present invention relates to a polyethylene glycol conjugated drug as shown in formula I or a pharmaceutically acceptable salt thereof. The present invention also relates to a method for preparing the polyethylene glycol conjugated drug or the pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the polyethylene glycol conjugated drug or the pharmaceutically acceptable salt thereof, and the use thereof in the preparation of a drug. ##STR00001##

An object of the present invention is to increase an amount of oligonucleotide transported into cytoplasm by allowing a cellular internalization enhancer to efficiently interact with target cells. An oligonucleotide conjugate according to the present invention contains a dendritic polymer, a plurality of oligonucleotides, one or a plurality of cellular internalization enhancers, and one or a plurality of hydrophilic linkers, wherein each oligonucleotide is bonded to the dendritic polymer directly or through a linker, and each cellular internalization enhancer is bonded to the dendritic polymer through the hydrophilic linker.

The present disclosure relates to pharmaceutical compositions comprising a peptide or multivalent polypeptide, and an anti-cancer agent. In some embodiments, the anti-cancer agent is conjugated to the peptide or multivalent polypeptide. The present disclosure also relates to a method of treating cancer or reducing cancer cell proliferation using the peptide or multivalent polypeptide. In some aspects, the peptide or multivalent polypeptide enhances the efficacy of the anti-cancer agent, the targeting of the anti-cancer agent to the cancer cells, or both.

Disclosed are methods of treating cancer in a subject, comprising subcutaneously administering to the subject an effective amount of a dendrimer of formula (I):

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and pharmaceutically acceptable salts thereof.

The present invention relates to polypeptides which are covalently bound to non-aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of the Eph receptor tyrosine kinase A2 (EphA2). The invention also relates to pharmaceutical compositions comprising said peptide ligands and to the use of said peptide ligands in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).