A method of macrocyclization of peptidomimetics is described which comprises substitution of one or more of the backbone amide C═O bonds with a turn-inducing motif. The method is general with enhancements seen across a range of ring sizes (e.g. tri-, tetra-, penta- and hexapeptides). Specifically, a peptidomimetic macrocycle is described comprising a carbonyl bioisosteric turn-inducing element having the structure: ##STR00001## wherein X is a heteroatom; and wherein R.sub.1 to R.sub.6 are each independently selected from alkyl, aryl, heteroaryl and H.

A method of macrocyclization of peptidomimetics is described which comprises substitution of one or more of the backbone amide C═O bonds with a turn-inducing motif. The method is general with enhancements seen across a range of ring sizes (e.g. tri-, tetra-, penta- and hexapeptides). Specifically, a peptidomimetic macrocycle is described comprising a carbonyl bioisosteric turn-inducing element having the structure: ##STR00001## wherein X is a heteroatom; and wherein R.sub.1 to R.sub.6 are each independently selected from alkyl, aryl, heteroaryl and H.

Provided are novel piperazic acid containing peptide compound stereoisomer, solvate, or pharmaceutically acceptable salt thereof, method of preparing the same, and use thereof. The peptide compound, stereoisomer, solvate, or pharmaceutically acceptable salt thereof has activities of anticancer, anti-metastasis, and growth inhibition of resistant tumors, and thus may be used to prevent or treat various cancers or metastases of cancer.

Provided are novel piperazic acid containing peptide compound stereoisomer, solvate, or pharmaceutically acceptable salt thereof, method of preparing the same, and use thereof. The peptide compound, stereoisomer, solvate, or pharmaceutically acceptable salt thereof has activities of anticancer, anti-metastasis, and growth inhibition of resistant tumors, and thus may be used to prevent or treat various cancers or metastases of cancer.

Disclosed herein are macrocyclic polypeptides having no more than 3 ammo acid substitutions compared to the amino acid sequence of any one of SEQ ID NO: 1-2.37 or a mirror image thereof, wherein the polypeptide includes both L and D amino acids, libraries of such polypeptides, and uses thereof.

In accordance with the present disclosure, macrocyclic compounds have been discovered that bind to PD-L1 and are capable of inhibiting the interaction of PD-L1 with PD-1 and CD80. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.

In accordance with the present disclosure, macrocyclic compounds have been discovered that bind to PD-L1 and are capable of inhibiting the interaction of PD-L1 with PD-1 and CD80. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.

The objective of the present invention is to provide a thickener that can increase the viscosity of a composition with suppressing stickiness and maintaining use feeling in the case of applying the composition on the skin or the like, since the thickener does not contain a polymer thickener or the content amount of a polymer thickener is small. The thickener according to the present invention is characterized in comprising a phospholipid, a biosurfactant, and a 1,2-diol compound represented by the following formula (I):

HO—CH.sub.2—CH(OH)—R.sup.1   (I)

wherein R.sup.1 is a hydrocarbon group having a carbon number of 5 or more and 12 or less.

Melanocortin receptor-specific cyclic peptides of the formula

##STR00001##

where Xaa.sup.1, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.7, R.sub.8, R.sub.9, R.sub.10, t, x and y are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes utilizing melanocortin receptor-specific cyclic peptides of formula I.

Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.