Short tri- and tetrapeptides according to the following Formula I Ar(CH2).sub.mX.sup.1X.sup.2COX.sup.3X.sup.4X.sup.5-(Trp).sub.n-NX.sup.6R are potent, selective agonists of melanocortin 1 receptor (MC1R). Provided herein are pharmaceutical compositions including Formula I peptide agonists of MC1R and methods of treating skin diseases and disorders that include administering to an individual in need thereof a therapeutic amount of a Formula I peptide. The peptides, pharmaceutical compositions, and methods described herein are useful in the treatment of diseases and disorders that benefit from agonism of MC1R, including melanoma, basal cell carcinoma, squamous cell carcinoma, porphyria, polymorphous light eruption, vitiligo, and solar urticaria.

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.

A water-soluble peptide fluorescence material having a structure of formula (I):

##STR00001##

In formula (I), n is an integer greater than or equal to 1, R.sub.1 is independently selected from hydrogen or a nitrogen-containing functional group, R.sub.2 is independently selected from hydrogen or alkyl, and A.sub.1 is polymerized by at least one amino acid monomer and having a structure of formula (II):

##STR00002##

In formula (II), m is an integer greater than or equal to 1, and R.sub.3 in each, of the amino acid monomers of A.sub.1 is independently selected from hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, or guanidinylalkyl, A.sub.2 is OR.sub.5 or N(R.sub.4).sub.2, and R.sub.4 is independently selected from hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, guanidinylalkyl, monoglycosyl, biglycosyl, or oligosaccharyl, and R.sub.5 is hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, or guanidinylalkyl.

The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below: ##STR00001##
wherein the definitions of T, Q, R.sub.1 and R.sub.2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.

The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (, -) dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.

Novel collagen mimics are disclosed with a tripeptide unit having the formula (Xaa-Yaa-Gly).sub.n, where one of the positions Xaa or Yaa is a bulky, non-electron withdrawing proline derivative. By substituting a proline derivative at either the Xaa or Yaa position in the native collagen helix, the stability of the helix is increased due solely to steric effects relative to prior known collagen-related triple helices. Methods are also disclosed for making the novel collagen mimics.

This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.

A piezoelectric transducer is provided herein, comprising a three-dimensional structure made of a plurality of peptides, the peptides being self-assembling and the structure being piezoelectric, wherein at least a portion, or each, of said plurality of peptides comprises peptides of 2 to 10 amino acid residues, provided that the plurality of peptides is not consisted of a plurality of Phe-Phe dipeptides. Further described herein are peptides having an amino acid sequence Hyp-Phe-Phe, Boc-Dip-Dip, (L)Trp-(D)Trp or (D)Trp-(L)Trp, as well as three-dimensional structures comprising such peptides.

Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.