University of Florida Research Foundation, Incorporated

University of Minnesota

Other

Oklahoma Medical Research Foundation

Torrey Pines Institute for Molecular Studies

Colorado Seminary

Carrie Haskell-Luevano

Richard Allen Houghten

Clemencia Pinilla

Jerry Ryan Holder

Miles B Brennan

Ute H Hochgeschwender

Radleigh G Santos

Skye Doering

Robert M Dores

Mark Ericson

Jon Richard Appel

Marc A Giulianotti

Jessica L Costa

Jessica Costa

Marcello A Giulianotti

The invention provides compounds having the general formula I: and salts thereof, wherein the variables R, R, Rand Rhave the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Selective small molecule peptidomimetic melanocortin ligands

Certain embodiments of the invention provide a cyclic compound of formula I: wherein: Pro is a residue of L-proline; Xis a residue of Arg or DArg; Xis a residue of Phe or DPhe; Xis a residue of Phe, DPhe or hPhe; Xis a residue of a natural or unnatural amino acid; Xis a residue of Ala, Asp, Glu, Lys, His, Phe, Ser, Leu or Gly; Xis a residue of Phe, Ala, Gly, Ser, Lys, Asp, Leu, Nle, Trp, Tyr, Cha or hPhe; and DPro is a residue of D-proline; or a salt thereof. Certain embodiments also provide compositions comprising such compounds, as well as methods of using such compounds and compositions.

Cyclic peptides and methods of use thereof

The invention provides compounds having the general formula I: and salts thereof, wherein the variables Pro, DPro, DPhe, Arg, Trp, X, X, Xand Xhave the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Chimeric melanocortin ligands and methods of use thereof

Certain embodiments of the invention provide a compound of formula (I):R&#x2014;C(&#x2550;O)&#x2014;W&#x2014;X&#x2014;Y&#x2014;Z&#x2014;N(R)&#x2003;&#x2003;(I)or a salt thereof, wherein R, R, W, X, Y and Z are as defined herein, as well as methods of use thereof.

Melanocortin ligands and methods of use thereof

Disclosed are novel ligands based on an AGRP template that can rescue endogenous melanocortin agonist and/or antagonist dysfunction at MCR polymorphisms. In particular, the present invention provides novel synthetic ligands based on AGRP templates that can rescue endogenous melanocortin agonist dysfunction at MC4R polymorphisms to treat children and adults with these mutations and increase their quality of life.

Biological active ligands of melanocortin receptors

ACTH analog compounds of the present invention include compounds comprising an ACTH peptide sequence with one or more structural modifications that can have one or more of the following preferred ACTH analog biological functions: (1) reduction of corticosteroid secretion by adrenal membrane in the presence of the ACTH analog compared to unmodified ACTH, (2) reduction of corticosteroid secretion by adrenal membrane in the presence of endogenous ACTH and (3) increased MC-2R binding affinity with reduced activation of the MC-2R receptor compared to unmodified ACTH binding to the MC-2R melanocortin. The ACTH analog compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders related to ACTH, ACTH receptors or corticosteroid secretion, such as premature labor and Cushing's Disease.

Adrenocorticotropic hormone analogs and related methods

The present invention relates to novel chimeric peptides and templates containing a combination of antagonist and agonist endogenous ligand residues. In particular, the present invention relates to novel chimeric peptides and templates thereof based upon melanocortin agonist peptides and agouti related protein (AGRP). The present invention provides multifunctional chimeric peptides having specific bioactivity at melanocortin receptors and their use as drugs to treat various diseases and conditions.

Melanocortin receptor templates, peptides and use thereof

The subject invention provides novel peptides for use in treating mammals to control appetite and obesity. Disclosed is a peptide derivative having the formula:X-Z-Q-arg-trp-NHwherein: Xis an acyl group, Z is amino-2-naphthyl-carboxylic acid or histidine, Q is (D)phenylalanine or p-iodo-(D)phenylalanine, or a pharmacologically acceptable salt, complex or derivative thereof, the peptide derivative having melanocortin-4 receptor agonist activity.

Peptides and methods for the control of obesity

Melanocortin receptor templates, peptides, and use thereof

The subject invention provides novel peptides for use in treating mammals to control appetite and obesity. Disclosed is a peptide derivative having the formula:X-Z-Q-arg-trp-NH

Growing community of inventors

Minneapolis, MN, United States of America

Carrie Haskell-Luevano