119643-69-5Relevant academic research and scientific papers
IMPROVED CONJUGATION LINKERS
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Paragraph 0100; 0101; 0105; 106, (2020/10/19)
Provided are β-eliminative linkers suitable for the conjugation of small molecule, peptide, and protein and compounds comprising the linkers.
TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
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Paragraph 00360, (2016/01/25)
Nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker have been designed. Such nanoparticles and microparticles can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
A method for preparing covalent lipid-spacer-peptide conjugates
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Page/Page column 5, (2008/12/06)
The present invention discloses a method for preparing lipid-spacer-reactive functional group-peptide, wherein the peptide consists of 3 to 16 amino acid residues in which at least one amino acid residue is lysine (Lys), the reactive functional group is a formula of -X-CO-Y-CO-, wherein X represents an oxygen atom or a nitrogen atom, and Y represents C1-6 alkylene which may be interrupted by one or two oxygen or nitrogen atom(s), the spacer is a hydrophilic polymer, and the lipid is phosphatidylethanoaminecarbonyl represented by the formula (I): R1 and R2 are the same or different and individually represent linear or branch C7-30 alkyl or linear or branch C7-30 alkenyl; which is characterized in that the reaction is carried out in a liquid phase and comprises the following steps of (a) firstly protecting Lys amino acid residue in the peptide through a protection group; (b) subsequently reacting the peptide with the lipid-spacer-reactive functional group; and (c) finally removing the protection group from Lys amino acid residue in the peptide.
