METHODS AND COMPOSITIONS FOR INHIBITING RHO/MRTF-MEDIATED DISEASES AND CONDITIONS

摘要

The present disclosure relates to methods, compositions, and kits for the inhibition of signaling by members of the Rho GTPase family. Specifically, the disclosure relates to methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signaling and action of the transcription co-factors MRTF-A and/or MRTF-B. The disclosure finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis and fibrosis), Rho-mediated biological conditions, and in cell signaling research.

主权项

1. A method of treating or preventing a rho-mediated disease in a subject comprising administering a compound of structure I,wherein Y is C—R3 or N, R2 is (CH2)nCOOR1, wherein each CH2 group may be optionally substituted, R1 is H or C1-C6 alkyl, n is an integer from 1 to 10, and R3 is the same or different and is H, a halide, an ether, or a straight or branched alkyl.