Burnham Institute for Medical Research

Sanford-burnham Medical Research Institute

The Burnham Institute

University of California

Triad Therapeutics, Inc.

Virginia Commonwealth University

Sanford Burnham Prebys Medical Discovery Institute

Triad Liquidating Company, LLC

Traid Therapeutics, Inc.

Maurizio Pellecchia

Daniel S Sem

John C Reed

Anna Maria Tempczyk-Russell

Jun Wei

Paul B Fisher

Swadesh K Das

Mitchell E Menezes

Luni Emdad

Timothy P Kegelman

Carlo Baggio

Luca Gambini

Bainan Wu

Surya K De

Elisa Barile

Qing Dong

Surya Kanta De

Min Sang Lee

Mark Kelly

Alex Strongin

Alex Y Strongin

Parima Udompholkul

Alexander Aronson

Lutz Tautz

Tomas Michael Mustelin

Provided herein are, inter alia, compositions that bind to a PDZ1 domain of MDA-9/Syntenin (syndecan binding protein: SDCBP), thereby inhibiting MDA-9/Syntenin activity, and methods of use of same. The compositions and methods provided herein are useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.

Inhibitors of cancer invasion, attachment, and/or metastasis

The methods and compositions of the disclosure provide for novel therapeutic compounds to treat obesity and aspects related thereto. Embodiments of the disclosure relate to oligonucleotide therapeutic (ONT) agents targeting miR-22 miRNA for the treatment of human obesity and related cardiometabolic disorders. Accordingly, aspects of the disclosure relate to modified nucleic acids, including locked nucleic acids, ethylene-bridged nucleotides, peptide nucleic acids, phosphorodiamidate morpholino oligonucleotides, and or a 5'(E)-vinyl-phosphonate modification.

EPHA2 agonists and uses thereof

Provided is a compound of formula (I): or a salt thereof, wherein R-Rhave any of the values described in the specification, as well as compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof and therapeutic methods comprising the administration of a compound of formula (I) or a pharmaceutically acceptable salt thereof. The compounds are useful as matrix metalloprotease MMP-12 inhibitors.

Therapeutic compounds and methods

Disclosed herein, inter alia, are methods of use and composition of novel inhibitors that target the Smac binding site of a variety of inhibitor of apoptosis proteins that contain a Bir domain, including XIAP, cIAP1, cIAP2, or other IAP proteins.

Agents targeting inhibitor of apoptosis proteins

Disclosed herein are Furin/PC inhibitors for inhibiting Furin and other Propprotein Convertases. Method of making the Furin/PC inhibitors, chemical and biological characterization of the Furin/PC inhibitors, and the use of the Furin/PC inhibitors to treat infectious diseases, cancers, and inflammatory/autoimmune disorders, are also disclosed.

Inhibitors of Furin and other pro-protein convertases

Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently selected from the group consisting of H, C(O)X, C(O)NHX, NH(CO)X, SONHX, and NHSOX, wherein X is selected from the group consisting of an alkyl, a substituted alkyl, an aryl, a substituted aryl, an alkylaryl, and a heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Naphthalene-based inhibitors of anti-apoptotic proteins

The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.

Apogossypolone derivatives as anticancer agents

A compound of Formula I: or a pharmaceutically acceptable salt thereof is disclosed. In addition, pharmaceutical compositions thereof, methods for preparing and methods for using this compound or composition for treating a variety of diseases, including cancer and inflammation are also provided.

Optically pure apogossypol derivative as pan-active inhibitor of anti-apoptotic B-cell lymphoma/leukemia-2 (BCL-2)

Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SONHX, or NHSOX, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

The present disclosure provides compound having the general structure A or pharmaceutically acceptable salts thereof:Het-L-P&#x2003;&#x2003;(A)wherein Het is an aromatic moiety comprising a heterocyclic structure mimicking ATP, P is a docking site derived peptide or a docking site peptide mimetic, and L is a linking moiety, wherein L links the ATP mimetic to the docking site peptide moiety. The compounds having the general structure A can serve as inhibitors of kinases, such as the kinases JNK, Erk and p38.

Bi-dentate compounds as kinase inhibitors

The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.

Methods and compounds useful to induce apoptosis in cancer cells

The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein X is a six-member ring selected from phenyl, pyridine, or pyrimidine; Y is H, an alkenyl, a substituted alkenyl, or alkynyl, and R is H or alkyl. Pharmaceutical compositions for treating various disorders such as cancers, the compositions including compound I are also provided.

Pyrazole derivatives as kinase inhibitors

The invention provides compounds that can efficiently and specifically inhibit bacterial toxins, such as inhibit the lethal factor (LF) protease activity of anthrax toxin and/or botulinum neurotoxin type A. The invention also provides methods for inhibiting proteases, such as lethal factor protease, as well as methods for treating bacterial infections, such as anthrax and botulinum.

Growing community of inventors

San Diego, CA, United States of America

Maurizio Pellecchia