Rigel Pharmaceuticals, Incorporated

Jianing Huang

Sarkiz D Issakani

Julie Sheung

Todd R Pray

Donald G Payan

Rajinder Paul Singh

David Carroll

Simon Shaw

Arvinder Sran

Henry Lu

Lyuben Tsvetkov

Sarkiz Issakani

Disclosed are sulfonamidoquinoline compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R, R, Rand Rare as described herein. In certain embodiments, a compound disclosed herein inhibits ubiquitination, and can be used to treat disease by blocking the degradation of tumor suppressors.

Ubiquitination inhibitors

The invention relates to assays for measuring ubiquitin ligase activity and for identifying modulators of ubiquitin ligase enzymes.

Ubiquitin ligase assay

Provided are methods and compositions for assaying for ubiquitin agents that are enzymatic components of ubiquitin-mediated proteolysis and, more particularly, methods and compositions for assaying for agents that modulate the activity of such ubiquitin agents.

Assays for identifying ubiquitin agents and for identifying agents that modify the activity of ubiquitin agents

The invention provides methods for identifying an anti-poxviral agents. In many embodiments, the methods involve contacting a poxviral p28 polypeptide with a candidate agent, and determining an effect of the agent on a ubiquitin ligase activity of the p28 polypeptide. The effect of the agent may be determined using a variety of different cell based or biochemical assays, such as polyubiquitylation assays and cell viability assays. The invention also provides methods for modulating poxvirus pathogenicity in a cell, and methods of treating an individual infected with a poxvirus. The subject methods find use in a variety of drug discovery, research and military applications.

Methods and compositions for the identification of anti-poxvirus agents

Ubiquitin conjugation assays

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Foster City, CA, United States of America

Jianing Huang