Torrey Pines Institute for Molecular Studies

Zymogenetics, Inc.

University of Minnesota

Stc.unm

The Burnham Institute

Merrion Research Iii Limited

Sarlan, Ltd.

Houghten Pharmaceutical Inc.

Torrey Pines Institute

Clemencia Pinilla

Richard Allen Houghten

John M Ostresh

Charles R Petrie

Patricia A McKernan

Daniel Joseph O'Mahony

Emma E Moore

Imelda Lambkin

Jean-Philippe Meyer

Jon Richard Appel

Marc A Giulianotti

John C Reed

Larry A Sklar

Bruce S Edwards

Carrie Haskell-Luevano

Adel Nefzi

Radleigh G Santos

Skye Doering

Jon R Appel, Jr

Kate Welsh

Jose Medina-Franco

Sylvie E Blondelle

Christa Hamashin

Julio Hernan Cuervo

Lisa Osthues-Spindler

Amy Schink

Silvie Blondelle

Marcello A Giulianotti

Richard Houghten

Daniel O'MAHONY

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 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

The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution. The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.

High-affinity small molecule formylpeptide receptor ligands from screening of combinatorial mixture-based libraries

Membrane translocation peptides, compositions comprising them, chimeric molecules comprising them, and methods of using them to achieve transmembrane transport of various agents.

Conjugates of membrane translocating agents and pharmaceutically active agents

The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds.

Methods and compositions for derepression of IAP-inhibited caspase

UEA-1 Mimetics, pharmaceutical formulations comprising them, and their uses as targeting agents for therapeutic and diagnostic purposes.

Pharmaceutical formulations and ligands for use therein; mimetics for UEA-1

The invention provides isolated agents having a core peptide selected from the group consisting of Core peptides 5 through 39 and 42 through 55, wherein the agent derepresses an IAP-inhibited caspase. Also provided is an isolated agent having a core structure selected from any of the structures shown in FIGS.B, andwherein said agent derepresses an IAP-inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The method consists of contacting an IAP-inhibited caspase with an effective amount of an agent to derepress an IAP-inhibited caspase, the agent having a core motif selected from the group consisting of a core peptide having a sequence set forth in any of Core peptides 4 through 39 and 42 through 55, and a core structure selected from the group consisting of TPI759, TPI882, TPI914 or TPI927. The methods of the invention also can be used for promoting apoptosis in a cell and for reducing the severity of a pathology characterized by reduced levels of apoptosis. Methods for identifying agents that derepress an IAP-inhibited caspase are also provided.

Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.

Dialkyl ureas as calcitonin mimetics

Dimeric oligopeptide mixture sets, their synthesis and use in determining the sequence of an oligopeptide dimer ligand that optimally binds to a receptor are disclosed. A dimeric oligopeptide mixture set has two oligopeptide portions bonded together by a disulfide bond. Each oligopeptide of a first oligopeptide portion has the same number of 3 to about 10 residues including an oxidized mercaptan-containing residue that forms part of the disulfide bond and an amino acid residue sequence that includes at least one of at least six residues in addition to the oxidized mercaptan-containing residue at the same one or more predetermined positions of the oligopeptide chain. The second portion has an oligopeptide chain having a length of 4 to about 10 residues, including an oxidized mercaptan-containing residue that forms part of the disulfide bond. The second portion is a mixture whose chains have equimolar amounts of those at least six amino acid residues at the same one or more other positions of the oligopeptide chain.

Dimeric oligopeptide mixture sets

Disclosed are peptides having anti-mellitin activity and having the formulae AC-IVILZZ-NH.sub.2, wherein Z is an amino acid. Also disclosed are compositions containing these peptides and methods of using them.

Peptides having anti-melittin activity

Synthetic peptide combinatorial libraries (sets) having a single, predetermined amino acid residue at a single, predetermined oligopeptide chain position and mixtures of amino acid residues at the other chain positions are disclosed, as are their processes of synthesis and use in determining the amino acid residue sequence of an oligopeptide ligand that binds to an acceptor molecule.

Scanning synthetic peptide combinatorial libraries: oligopeptide mixture

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Cardiff, CA, United States of America

Clemencia Pinilla