The present invention provides .sup.18F-labeled amino acids or derivatives thereof having formula (I) and methods of making same, which can be suitable for PET imaging:

##STR00001##

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

The present invention discloses an amino mercaptan compound, preparation method thereof and use thereof in radiation protection. The compound has the structure of formula I, wherein A.sub.1 is selected from: C(O)NR.sup.8, S(O).sub.2NR.sup.8, S(O)NR.sup.8, and R.sup.7NR.sup.8; A.sub.2 is selected from: carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted C.sub.1-6 alkyl; R.sup.1, R.sup.2, R.sup.5, and R.sup.6 may be the same or different and are selected from: hydrogen, substituted or unsubstituted C.sub.1-C.sub.5 alkyl or heteroalkyl; n is an integer from 0 to 20,000; R.sup.3 and R.sup.4 are independently selected from: hydrogen, X, substituted or unsubstituted C.sub.1-6 alkyl; X is selected from: F, Cl, Br and I; R.sup.7 is selected from: substituted or unsubstituted C.sub.1-C.sub.6 alkyl; and R.sup.8 is selected from: hydrogen, substituted or unsubstituted C.sub.1-C.sub.6 alkyl. The compound has the effects of reducing the biological damage caused by ionizing radiation, extending the survival period and survival rate of the radiated animals, and significantly alleviating the side effects of radiotherapy, and has a low toxicity. The present invention opens up a new way for protection and treatment of ionizing radiation damage.

##STR00001##

Provided are antifouling particles and uses thereof in methods of anti-biofouling.

Granzyme B inhibitor compounds, compositions that include the compounds, and methods for using the compounds. The compounds of the invention have advantageous water solubility and effectively inhibit Granzyme B.

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

The present invention provides compounds of formula (I) ##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.

Neuropeptide S receptor agonists are provided. The NPS agonists include trimeric, tetrameric, pentameric or hexameric peptidomimetic analogs exhibiting affinity for and activity at the neuropeptide S receptor. The peptidomimetic molecules may be useful in the treatment of disorders, syndromes and conditions mediated by modulation of the neuropeptide S receptor such as substance abuse, narcolepsy, insomnia, obesity, cognitive decline, dementia, Alzheimer's disease, panic disorder, generalized anxiety, PTSD, phobias, schizophrenia and as supportive medication during any kind of cessation program in cognitive behavioral therapy, such as drug addiction, eating disorders and gambling.

Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

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): ##STR00001##
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.