Torrey Pines Institute for Molecular Studies

Louisiana State University and Agricultural & Mechanical College

Stc.unm

University of Minnesota

Jon Richard Appel

Richard Allen Houghten

Clemencia Pinilla

Marc A Giulianotti

Larry A Sklar

Bruce S Edwards

Iris Lindberg

Jose Medina-Franco

Angus Cameron

Carrie Haskell-Luevano

Radleigh G Santos

Skye Doering

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

Small, polybasic peptides are disclosed that are effective as furin inhibitors, e.g. hexa- to nona-peptides having L-Arg or L-Lys in most positions. Removing the peptide terminating groups can improve inhibition of furin. High inhibition was seen in a series of non-amidated and non-acetylated polyarginines. The most potent inhibitor identified to date, nona-L-arginine, had a Kagainst furin of 40 nM. Non-acetylated, poly-D-arginine-derived molecules are preferred furin inhibitors for therapeutic uses, such as inhibiting certain bacterial infections, viral infections, and cancers. Due to their relatively small size, these peptides should be non-immunogenic. These peptides are efficiently transported across cell membranes.

Inhibiting furin with polybasic peptides

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Cardiff, CA, United States of America

Jon Richard Appel