UNIVERSITY OF SOUTHERN CALIFORNIA;The Regents of the University of California
发明人:
Ichiro Nishimura,Akishige Hokugo,Kenzo Morinaga,Charles E. McKenna,Boris A Kashemirov,Eric T. Richard
申请号：
US16623740
公开号：
US20200215205A1
申请日:
2018.07.13
申请国别(地区):
US
年份:
2020
代理人:
摘要：
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.
