Unique compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.

The present invention relates to a process for the purification of Carfiizomib of Formula I that reduces the level of an acetamide impurity of Formula II preferably below 0.10 wt %. Formula I Formula II.

##STR00001##

Compounds with the following structures ##STR00001##
and their analogs are provided. Compositions that include these structures can be used to inhibit glucose transporters and stop or decrease the proliferation of cancer, treat possible organ rejection and treat autoimmune disease.

The present disclosure relates to tertiary amino lipidated and/or PEGylated cationic peptide compounds and complexes thereof with nucleic acids for endocellular delivery, methods for preparing the compounds and complexes, and methods for delivering polyanionic compounds to cells.

A compound of Formula I, ##STR00001##
and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.

The invention provides a method for treating one or more complications of diabetes in a mammal. The method comprises administering to a mammal in need thereof an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (p.sub.m) and the total number of amino acid residues (r) wherein 3 p.sub.m is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (p.sub.t) wherein 2a is the largest number that is less than or equal to p.sub.t+1, except that when a is 1, p.sub.t may also be 1.

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.

Antigenic compositions comprising one or more labyrinthin-derived peptides are described herein. In some embodiment, each peptide of the antigenic composition comprises a T-cell epitope and/or a B-cell epitope. In other aspects, the present disclosure provides, e.g., vaccine compositions comprising tin antigenic composition disclosed herein, including kits, medicines, and compositions (such as pharmaceutical compositions and unit dosages) thereof. Also provided are methods of using the compositions disclosed herein, such as methods of treatment thereof and methods of producing antibodies, and antibody compositions thereof, against the one or more labyrinthin-derived peptides or a portion thereof.

An antitumor pharmaceutical camptothecin derivative and an antibody-drug conjugate thereof. By means of a series of molecular structure modifications, an optimal camptothecin antitumor drug is obtained, so as to be more suitable as a drug for antibody conjugation.

The present disclosure relates to a linker molecule for targeting molecule-drug conjugate, and the corresponding conjugate, the preparation and use thereof.