Self-quenching activatable COX-2-specific multi-modal molecular probes for diagnosis of cancers, inflammation, and immune system disorders

摘要

Encompassed are pharmaceutically acceptable compositions formulated for the topical or transdermal delivery of probes specific for cyclooxygenase-2 (COX-2) of human and non-human subjects. In particular, an activatable probe comprises a fluorescent moiety comprising a fluorophore attached to a compound having selective affinity for COX-2, and a removable fluorescence quencher linked to the fluorescent moiety by a cleavable linker. Upon delivery to a recipient subject, the activatable probe is localized and concentrated in tissues and cells with elevated levels of COX-2. The linker is cleaved to release the fluorescence quencher. Irradiation by an activating incident illumination results in a detectable fluorescent emission signal

主权项

1. A composition comprising an activatable probe for the detection of a cell or tissue having cyclooxygenase-2 (COX-2) activity, said activatable probe comprising:
(i) a fluorescent moiety consisting of indomethacin conjugated to 5-Rox-D (Fluorocoxib); and (ii) a fluorescence quencher, wherein the fluorescent quencher is GHK-Cu+, wherein the fluorescent moiety and the fluorescence quencher are connected by a cleavable linker comprising a cleavable peptide bond, wherein the linker is GHK, wherein the activatable probe is encapsulated in a liposome comprising sulfasalazine.