The disclosure provides proteasome inhibitors that can be used to halt cell division of rapidly dividing cells by preventing the degradation of cell cycle-regulating proteins, such as cyclins, cyclin-dependent kinase inhibitors, and p53. The proteasome inhibitor compounds can be used to inhibit the proliferation of cancer cells.

Integrin ligands having serum stability and affinity for αvβ6 integrins are described. Compositions comprising αvβ6 integrin ligands having serum stability and having affinity for αvβ6 integrins and methods of using them are also described.

Methods of treating aging related skin changes and of increasing skin thickness with topical administration of N-acyldipeptide derivatives are described. Compositions comprising N-acyldipeptide derivatives, are therapeutically effective for increasing skin thickness, and for treating extrinsic and intrinsic aging and aging related skin changes, such as fine lines, wrinkles, photoaging, hyperpigmentation, laxity, age spots, lentigines, mottled skin, and cellulite.

Provided is a method of preparing an N-acetyl dipeptide and an N-acetyl amino acid, the method including producing the N-acetyl dipeptide and the N-acetyl amino acid by reaction of an amino acid with acetic anhydride or acetyl chloride.

The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.

The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders, combinations with at least one other active substance, and a kit comprising the substances or the compositions.

Provided is a pharmaceutical formulation comprising a modified IL-7 protein. More particularly, it comprises (a) a modified IL-7 fusion protein; (b) a basal buffer with a concentration of 10 to 50 mM; (c) a sugar with a concentration of 2.5 to 5 w/v%; and (d) a surfactant with a concentration of 0.05 to 6 w/v%.

Such pharmaceutical formulation of a modified IL-7 fusion protein does not show aggregates formation, but shows protective effects on proteins under stress conditions such as oxidation or agitation, and thus can effectively be used for the treatment of a patient.

The present disclosure provides antibody-drug conjugate (ADC) structures, which include a camptothecine or a camptothecine derivative linked to a polypeptide (e.g., an antibody) through a linker. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.

A SMAC mimetic and pharmaceutical compositions thereof and methods of use.

An isobaric stable isotope-containing phosphorylated protein labeling reagent, and a preparation method and application thereof are provided. The protein labeling reagent is a phosphorylated dipeptide organophosphorus reagent labeled by a stable isotope such as deuterium-2, carbon-13, oxygen-18, or nitrogen-15. The preparation method includes: (1) preparation of an isobaric stable isotope-containing amino acid with N-terminal protection, (2) preparation of an isobaric stable isotope-containing amino acid activated ester Fmoc/Boc-R.sub.1-NHS with N-terminal protection, (3) preparation of an isobaric stable isotope-containing dipeptide, (4) preparation of an isobaric stable isotope-containing phosphite, (5) preparation of an isobaric stable isotope-containing phosphite dipeptide, and (6) preparation of a stable isotope-labeled N-phosphorylated amino acid activated ester. The present protein labeling reagent can realize the quantitative analysis of polypeptides, standard proteins, proteins in cells, and proteins in urine samples and blood samples, and has the advantages of good accuracy, high sensitivity, no interference of isotope effect and wide applicability.