University of Michigan

Michigan State University

The University of New Mexico

The University of Bath

Richard Neubig

Scott D Larsen

Kim Hutchings

Erika Mathes Lisabeth

Larry A Sklar

Raymond E Counsell

Eric R Prossnitz

Roger K Sunahara

Yafei Jin

Peter C Simons

Henry Mosberg

Stephen Husbands

Tione Buranda

Marcian E Van Dort

Daniel F Cimino

Levi Lynn Blazer

John Traynor

Andrew Haak

Hauiling Zhong

Walajapet Rajeswaran

Alex T Key

Dinesh Khanna

Mei Shi

Dylan Kahl

Disclosed herein are inhibitors of Rho/MRTF/SRF-mediated gene transcription, and methods for their use in treating or preventing diseases such as cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

Inhibitors of Rho/MRTF/SRF-mediated gene transcription and methods for use of the same

Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor ('MRTF/SRF'), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: wherein the substituents are as described.

Inhibitors of myocardin-related transcription factor and serum response factor (MRTF/SRF)-mediated gene transcription and methods for use of the same

The invention relates to compositions having RGS (regulator of G-protein Signaling) inhibiting activity, and methods of use thereof. In some embodiments, RGS-inhibiting compositions find use in research on or treatment of disease states (e.g., diabetes, epilepsy, neuropathic pain, depression and other diseases).

Small molecule inhibitors of RGS proteins

The present invention relates to novel inhibitors of G-protein signaling. In particular, the present invention provides peptide inhibitors of G protein signaling proteins and methods of using such inhibitors to modulate physiological effects of G protein signaling. The present invention thus provides novel drug targets for a variety of pathologies mediated by defects in G-protein signaling.

Inhibitors of RGS proteins

The present invention provides a general approach for G protein coupled receptors that may be used to define agonists and antagonists, and the specificity of receptor coupling to G protein subunits. Methods of the present invention use small volumes (microliters) and are compatible with high throughput flow cytometry. When assays of the present invention are multiplexed, the specificity of the interactions of a receptor with many G proteins may be determined simultaneously.

Bead-based detection of ligand-GPCR-G protein complexes

Iodinated clonidine derivatives useful, inter alia, as a probe for identification and characterization of .alpha..sub.2 -adrenergic receptor sites and as tracers for imaging techniques such as positron emission tomography or computer assisted tomography. Binding competition studies have indicated that p-iodoclonidine, for example, is a particularly efficacious binder for .alpha..sub.2 -adrenergic sites.

Iodinated clonidine derivatives as radioactive imaging tracers

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East Lansing, MI, United States of America

Richard Neubig