This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 2 (PAR2) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR2 activity.

The present invention relates to a compound of formula (I), wherein X is C═O, C═S or B—OH; Y is an electrophile and Z is a leaving group, or Y═Z is an electrophile; R.sup.1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, the first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits β1 and β2 of a proteasome; R.sup.2 and R.sup.3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethynyl and cyano, wherein methyl and ethyl may be substituted with OH or halogen. ##STR00001##

The present application relates to a method of inducing differentiation of stem cells into chondrocytes using an oligopeptide, and a pharmaceutical composition for treating cartilage injury disease containing differentiated chondrocytes obtained by the method.

Provided herein are heterocyclic compounds useful for imaging Granzyme B. Methods of imaging Granzyme B, combination therapies, and kits comprising the Granzyme B imaging agents are also provided.

Provided is at least one peptide of formula (I) and its use, where formula (I) is as follows: X-(Xaa.sub.1).sub.n-Pro*-(Xaa.sub.2).sub.m-Y (I). In formula (I), n=0 and m=1. At the N terminal end of the peptide, X is selected from H, —CO—R.sub.1 and —SO.sub.2—R.sub.1. At the C terminal end of the peptide, Y is selected from OH, OR.sub.1, NH.sub.2, NHR.sub.1 or NR.sub.1R.sub.2, R.sub.1 and R.sub.2 being independently selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulphured, with the possibility to have in said group skeleton a O, S and/or N heteroatom. Pro* corresponds to a Proline, an analogue or derivative thereof.

The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.

There is provided a self-assembly amphiphilic peptide having the formula (I): XYZ (I), wherein X is a polar moiety at the N-terminus; X and Z each independently has between 1 to 4 residues of aliphatic amino acids or analogs or derivatives thereof, and wherein the average degree of hydrophobicity of the residues in block Z is more than the average degree of hydrophobicity of the residues in block Y. Disclosed are compositions and hydrogel comprising the peptide thereof. Also disclosed are methods of treatment for tissue regeneration, wound healing and methods of culture of stem cells, tissues and organoids.

The present invention relates to a linker of the following formula (I) or a salt thereof: (I). The present invention relates to a linker-drug conjugate of the following formula (II) or a salt thereof: (II). The present invention relates also to a binding unit-drug corrugate, such as an antibody-drug conjugate, of the following formula (III) or (IV) or a salt thereof: (III), (IV), as well as a pharmaceutical composition comprising such a binding unit-drug corrugate and its use in the treatment of cancer.

##STR00001##

Described herein is a process for the total synthesis of macrolactones and macrolactams of formula I ##STR00001##
including E- and Z-configuration thereof, in particular, nannocystins.

Disclosed are geminoid peptide-like compound according to Formula I:

R.sup.1—C(═O)—Z.sub.n—NR.sup.3-R.sup.2  (I)

in which R.sup.1 and R.sup.2 are each independently saturated, partly saturated or unsaturated, straight, branched or cyclic alkyl chains, wherein R.sup.1 has a number of C atoms of 11 or more, preferably 11 to 19, and R.sup.2 has a number of C atoms of 12 or more, preferably 12 to 20; R.sup.3 is hydrogen or C.sub.1-C.sub.6 alkyl; n is an integer from 1-15;
each Z independently is an amino acid residue, wherein Z.sub.n comprises an N-terminus attached to C(═O) and a C-terminus that is attached to NR.sup.3, for use as a medicament.