University of Southern California

Biovinc LLC

University of California

Eric T Richard

Charles E McKenna

Frank Hallock Ebetino

Shuting Sun

Mark Walden Lundy

Keivan Sadrerafi

Parish Sedghizadeh

Philip T Cherian

Boris A Kashemirov

Ichiro Nishimura

Akishige Hokugo

Kenzo Morinaga

Described herein are bisphosphonate quinolone compounds, conjugates and pharmaceutical formulations thereof that can include a bisphosphonate and a quinolone, where the quinolone can be releasably coupled to the bisphosphonate. Also provided herein are methods of making and methods of using the bisphosphonate quinolone compounds, conjugates and pharmaceutical formulations thereof.

Bisphosphonate quinolone conjugates and uses thereof

In certain embodiments osteoadsorptive fluorogenic substrates of cathepsin K (or other proteases) are provided. Utilizing a bisphosphonate targeting moiety, the fluorogenic substrates provide effective bone-targeted protease sensor(s). In certain embodiments the 'probes' comprise cleavable fluorophore-quencher pair linked by a cathepsin K (or other protease) peptide substrate and tethered to a bisphosphonate. Unlike existing probes that are cleared within a few days in vivo, the probes described herein (e.g., OFS-1) allow for monitoring resorption over the course of longer time periods with a single dose.

Osteoadsorptive fluorogenic substrate of cathepsin k for imaging osteoclast activity and migration

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Los Angeles, CA, United States of America

Eric T Richard