The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula 1 in the synthesis of peptide derivatives. ##STR00001##

The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula 1 in the synthesis of peptide derivatives. ##STR00001##

Provided are a TEV protease variant, a fusion protein thereof, a preparation method therefor and the use thereof. Provided are a TEV protease variant with unique properties obtained by screening and a fusion protein thereof. The TEV protease variant has a low enzyme cleavage activity during expression in hosts, and preferably has a lower enzyme cleavage activity compared to an S219V variant having an amino acid sequence as shown in SEQ ID NO: 10. The enzyme cleavage site of the TEV protease variant is selected from EXXYXQG/S/H, wherein X is any amino acid residue, and the enzyme cleavage site is preferably selected from SEQ ID NO: 7 and 8. Fusion expression using the TEV protease variant of the present invention and a polypeptide can be used for preparing a polypeptide quickly and efficiently, thereby solving the problems currently present in the process of the recombinant production of a polypeptide.

Provided are a TEV protease variant, a fusion protein thereof, a preparation method therefor and the use thereof. Provided are a TEV protease variant with unique properties obtained by screening and a fusion protein thereof. The TEV protease variant has a low enzyme cleavage activity during expression in hosts, and preferably has a lower enzyme cleavage activity compared to an S219V variant having an amino acid sequence as shown in SEQ ID NO: 10. The enzyme cleavage site of the TEV protease variant is selected from EXXYXQG/S/H, wherein X is any amino acid residue, and the enzyme cleavage site is preferably selected from SEQ ID NO: 7 and 8. Fusion expression using the TEV protease variant of the present invention and a polypeptide can be used for preparing a polypeptide quickly and efficiently, thereby solving the problems currently present in the process of the recombinant production of a polypeptide.

The present specification provides compositions of β-endorphin and adrenocorticotropic hormone (ACTH). These compositions are useful in methods of treating disease.

The present invention relates to protein nanocages comprising a melanocyte-targeting moiety and pharmaceutical compositions comprising the protein cages as well as methods for treating or diagnosing hyperpigmentation disorders or other melanocyte-related disorders using the protein nanocages or pharmaceutical compositions. In the preferred embodiment, the protein nanocage is composed of Bacillus stearothermophilus E2 protein of pyruvate dehydrogenase multi-enzyme complex (E2), with a skin penetrating and cell permeating SPACE moiety, and a melanocyte-targeting moiety of alpha melanocyte stimulating hormone.

The present invention relates to protein nanocages comprising a melanocyte-targeting moiety and pharmaceutical compositions comprising the protein cages as well as methods for treating or diagnosing hyperpigmentation disorders or other melanocyte-related disorders using the protein nanocages or pharmaceutical compositions. In the preferred embodiment, the protein nanocage is composed of Bacillus stearothermophilus E2 protein of pyruvate dehydrogenase multi-enzyme complex (E2), with a skin penetrating and cell permeating SPACE moiety, and a melanocyte-targeting moiety of alpha melanocyte stimulating hormone.

The present invention relates to a method for screening a protease variant and the obtained protease variant, and the protease variant has a special performance. The method for screening the protease variant comprises the following steps: (1) constructing a protease random mutation library, optimizing a protease random mutation virus library, and optimizing a protease random mutation phage library; (2) for the protease random mutation library, optimizing the protease random mutation virus library, and optimizing the protease random mutation phage library and screening a protease variant having weak protease enzyme-cutting activity in a host or a similar condition and having protease enzyme-cutting activity in an in vitro denaturation condition; and (3) the step of optionally characterizing the protease variant, wherein the protease optimizes TEV protease or enterokinase. The protease variant in the present invention facilitates industrial production of protein.

The invention belongs to the technical field of polypeptide preparation methods, and in particular relates to a high-purity ACTH (human sequence) or analogue and large-scale preparation method thereof. The main steps include: amino acids are coupled from the C-terminal to the N-terminal by Fmoc solid-phase synthesis method to obtain the crude ACTH (human sequence) or analogue peptidyl-resin with protective groups, wherein the reaction temperature of C-15 peptide synthesis is 40-60° C. After cleavge and precipitation, the crude product of ACTH (human sequence) or analogue is obtained, and then the high-purity product is obtained by liquid chromatography. The chromatographic purity of ACTH (human sequence) or analogue prepared by the invention is more than 99%, the stability is good, and the yield of the target peptide is ≥63%.

The present invention relates to protein nanocages comprising a melanocyte-targeting moiety and pharmaceutical compositions comprising the protein cages as well as methods for treating or diagnosing hyperpigmentation disorders or other melanocyte-related disorders using the protein nanocages or pharmaceutical compositions.