The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.

Compositions and methods for treating a depressive disorder or an anxiety disorder in a subject in need of such treatment are described herein. A therapeutically effective amount of a composition comprising a melanocortin 5 receptor (MC5R) peptide ligand according to the following:

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in a pharmaceutically acceptable carrier is administered to the subject. Xaa can be Cha or Pro. The MC5R peptide is a selective MC5R antagonist, and administration thereof to the subject can treat the depressive or anxiety disorder with clinical improvement observed in a relatively short time.

Disclosed are an intermediate drug having synergistic anticancer activity and a polyethylene glycol-coupled synergistic anticancer drug, and a method preparing therefor and use thereof. The intermediate drug has the general structural formula of (I), and the polyethylene glycol-coupled synergistic anticancer drug has the general structural formula of (II). The drugs achieve the combined medication of various anticancer drugs and avoid the toxic reaction caused by the interaction among the drugs or by the pharmacokinetics of the drugs when taking various anticancer drugs, facilitate overcoming the multidrug resistance of cancers, have a synergistic effect, and can be used for preparing anticancer medicaments and for treating cancers.

A method for producing imidazole dipeptide using a microorganism having imidazole dipeptide synthesis activity, the production method not including adding ATP, or including adding an amount of ATP that is less than the amount of imidazole dipeptide that is produced in terms of the number of moles, by utilizing an ATP supply system of the microorganism.

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.

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X):

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and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [.sup.68Ga]GaCl.sub.3 with high yields and excellent radiochemical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.

Provided are a novel peptide compound, a method of producing the same, and use of the peptide compound. Since the peptide compound has anticancer activity, the peptide compound may be used for the prevention or treatment of cancer.

In some embodiments, a mass spectrometry tag may comprise a linker region, a mass balance region, and a reporter region. The mass spectrometry tag may be configured to fragment in a mass spectrometer via an energy dependent process to produce multiple reporter molecules. For example, the reporter region of the tag may be configured to produce at least two reporter molecules via fragmentation. In some embodiments, one or more regions of the tag may comprise at least one heavy isotope. In some such embodiments, the ability to fragment into multiple reporter molecules as well as the placement and/or number of heavy isotope(s) allows the mass spectrometry tag to be distinguished from other similar mass spectrometry tags. In some such embodiments, the ability to distinguish between tags having the same or substantially similar total mass to charge ratio and reporter region mass may allow the system to have a greater multiplexing capacity than conventional systems.