An embodiment relates to a depsipeptide-based building block for inhibiting protein-protein interactions, a nanostructure including the same, and a use thereof, wherein the depsipeptide-based building block may remain in the body and cells for a long time when administered in vivo and be delivered to a target tissue with high efficiency, and a peptide for inhibiting protein-protein interactions may be gradually released over a long time to obtain a high effect.

An embodiment relates to a depsipeptide-based building block for inhibiting protein-protein interactions, a nanostructure including the same, and a use thereof, wherein the depsipeptide-based building block may remain in the body and cells for a long time when administered in vivo and be delivered to a target tissue with high efficiency, and a peptide for inhibiting protein-protein interactions may be gradually released over a long time to obtain a high effect.

The present disclosure relates to compounds of formula (1):

RCG1-L-P(i)

wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.

The present disclosure relates to compounds of formula (1):

RCG1-L-P(i)

wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.

An object of the present invention is to provide methods of discovering drugs effective for tough targets, which have conventionally been discovered only with difficulty. The present invention relates to novel methods for cyclizing peptide compounds, and novel peptide compounds and libraries comprising the same, to achieve the above object.

An object of the present invention is to provide methods of discovering drugs effective for tough targets, which have conventionally been discovered only with difficulty. The present invention relates to novel methods for cyclizing peptide compounds, and novel peptide compounds and libraries comprising the same, to achieve the above object.

The invention provides a peptide having an antimicrobial activity comprising the amino acid sequence as set forth in SPRVCIRVCRNGVCYRRCWG (SEQ ID NO:1), wherein at least one, two, three or all of the cysteine amino acids of the sequence of SEQ ID No. 1, in position No. 5, 9, 14 and/or 18 is substituted by another amino acid. Further provided are methods of using the same for the treatment or prevention of an infectious disease or condition.

The invention provides a peptide having an antimicrobial activity comprising the amino acid sequence as set forth in SPRVCIRVCRNGVCYRRCWG (SEQ ID NO:1), wherein at least one, two, three or all of the cysteine amino acids of the sequence of SEQ ID No. 1, in position No. 5, 9, 14 and/or 18 is substituted by another amino acid. Further provided are methods of using the same for the treatment or prevention of an infectious disease or condition.