Abstract: The present invention disclosed compositions comprising a stabilized Exendin-4 (1-39) and related compounds. The invention describes stabilized Exendin-4 agonists that include at least one modified amino acid residue particularly at positions Gln 13, Met14, Trp25, or Asn28 of the Exendin-4 (1-39) molecule. Disclosed are preferred modifications of deaminated, hydrolyzed, oxidized, or isomerized reaction products of the specified amino acid residues corresponding to the same positions in the Exendin-4 molecule. The invention also relates to methods of making and using the stabilized Exendin compounds, such as for the treatment of diabetes.

Abstract: The present invention relates to use of GLP-1 or a related molecule having a GLP-effect for the manufacture of a medicament for preventing or treating diabetes in a mammal. The amount and timing of administration of said medicament are subsequently reduced to produce a “drug holiday.” Practice of the invention achieves effective therapy without continuous drug exposure and without continuous presence of therapeutic levels of the drug. The invention also discloses a method of treating diabetes and related disorders in a mammal by administering glucagon like peptide (GLP-1) or a related molecule having GLP-1 like effect and thereby providing a therapeutically effective amount of endogenous insulin.

Abstract: The present invention relates to proteins and polypeptides that (i) have the formula A-[Wm-A]n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; each W is independently a linker; m is 1 or 2; and n is any number from 1 through 5; (ii) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to fifteen, m is any number from zero to fifteen, and the sum of n and m is any number from eight to fifteen; (iii) have the formula A-An where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; and n is any number from 1 through 5; or (iv) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to seven, m is any number from zero to seven, and the sum of n and m is any number

Abstract: The invention is directed to a pharmacologically active peptide conjugate having a reduced tendency towards enzymatic cleavage comprising a pharmacologically active peptide sequence (X) and a stabilizing peptide sequence (Z) of 4-20 amino acid residues covalently bound to X.

Abstract: The present invention relates to an improved process for the production of peptides by solid-phase synthesis. The invention also relates to agents which are useful in solid-phase peptide synthesis.

Abstract: Disclosed are novel peptides including antiarrhythmic peptides that have improved stability. Further disclosed are compositions that include such peptides and methods of using the compositions particularly as medicaments.

Abstract: N- or C-terminally modified small peptides having antiarrhythmic properties are disclosed, and in particular small peptides that possess improved pharmacokinetic properties such as having a reduced tendency to inhibit the activity of isozyme 3A4 of cytochrome P450 oxidase. The invention further relates to uses of said compounds in the preparation of a medicament, and to pharmaceutical compositions comprising said compounds.

Abstract: The present invention relates to an improved process for the production of peptides by solid-phase synthesis. The invention also relates to agents, which are useful in solid-phase peptide synthesis.

Abstract: The present invention relates to an improved process for the production of peptides by solid-phase synthesis. The invention also relates to agents which are useful in solid-phase peptide synthesis.

Abstract: The present invention disclosed compositions comprising a stabilized Exendin-4 (1-39) and related compounds. The invention describes stabilized Exendin-4 agonists that include at least one modified amino acid residue particularly at positions Gln 13, Met14, Trp25, or Asn28 of the Exendin-4 (1-39) molecule. Disclosed are preferred modifications of deaminated, hydrolyzed, oxidized, or isomerized reaction products of the specified amino acid residues corresponding to the same positions in the Exendin-4 molecule. The invention also relates to methods of making and using the stabilized Exendin compounds, such as for the treatment of diabetes.

Abstract: Novel peptide agonists of GLP-1 activity useful for lowering blood glucose levels. The novel peptides comprise variants of the GLP-1 or the exendin-4 polypeptide sequence and are pharmacologically active and stable. These peptides are useful in the treatment of diseases that benefit from regulation of excess levels of blood glucose and/or regulation of gastric emptying, such as diabetes and eating disorders.

Abstract: Disclosed are compositions and methods for modulating hemichannel function in a cell, tissue or organ. The invention also relates to useful screens for detecting such compounds, particularly those capable of modulating connexin phosphorylation. Further provided are therapeutic methods for preventing or treating conditions impacted by undesired hemichannel function in a mammal such as heart arrhythmia.

Abstract: The present invention relates to novel peptide conjugates which have increased stability and are useful in the treatment of excess levels of blood glucose.