Patent classifications
C07K9/006
Glycopeptide constructs and uses thereof
Glycopeptide conjugates, and methods of making and using such conjugates are disclosed. Certain glycopeptide conjugates comprise tumor associated carbohydrate antigens and peptide epitopes. Certain glycopeptide conjugates comprise cyclic peptide scaffolds that display carbohydrate antigens in a clustered fashion. The immunogenicity of select glycopeptide conjugates is demonstrated.
Cyclic compound having selective KRAS inhibitory effect on HRAS and NRAS
Cyclic compounds that selectively inhibit KRAS were found. Moreover, cyclic compounds were found to interact with an amino acid residue specific to KRAS.
GLYCOSYLATED CYCLIC ENDOMORPHIN ANALOGS
Glycosylated, cyclic peptides of Formula (I): A.sup.1-cyclo[A.sup.2-A.sup.3-A.sup.4-A.sup.5]-A.sup.6-O-Carb, Formula (II): A.sup.1-cyclo[A.sup.5-A.sup.3-A.sup.4-A.sup.2]-A.sup.6-O-Carb, and pharmaceutically acceptable salts thereof, are described herein, which are useful, e.g., in treating pain. In some embodiments A.sup.1 is L-Tyr; A.sup.2 is a D-Lys, D-Orn, D-Dab, or D-Dpr; A.sup.3 is L-Trp; A.sup.4 is L-Phe, A.sup.5 is an amino acid residue selected from the group consisting of Asp, Glu, iso-Asp, and iso-Glu; A.sup.6 is (a) a hydroxy-substituted amino acid residue (HO-AA), or (b) an oligopeptide comprising 2 to 5 amino acid residues comprising the HO-AA; Carb is a carbohydrate group bonded to the sidechain oxygen of the HO-AA by a 3-D-glycosidic bond, and the C-terminus of A.sup.6 optionally is amidated, e.g., as a primary amide.