Molecular Probes, Inc.

Other

Steven L Young

Hee Chol Kang

Michael H Melner

Richard P Haugland

Richard P Haughland

John Alton Copland

The proliferation of uterine fibroid leiomyoma cells is inhibited by certain Fibroid Cell Growth Inhibitor (FGI) agents. The pharmacological doses of these FGI agents in the milieu of uterine fibroid cells can be made high enough to not only inhibit proliferation, but to also causes cell death. Non-invasive or minimally invasive, non-systemic delivery methods are used to deliver the FGI agent to the milieu of the target fibroid leiomyoma cell population, thereby avoiding the disadvantages and side effects of surgical and systemic hormonal therapy interventions in the treatment of uterine fibroids. The FGI agents are substrates that are normally present or are well tolerated in the human body. The efficacy of the FGI agents appears to be related to their ability to moderate the Protein Kinase C and Mitogen Activated Protein Kinase pathways. Specific FGI agents shown to be useful to inhibit growth or proliferation of uterine fibroid cells include: &agr;-tocopherol, &agr;-tocopherol succinate, and troglitazone. Delivery of the FGI agents to the milieu of the target uterine fibroid cells may be accomplished by intra-vaginal and in situ injection techniques already known in the art.

Compositions and methods for the non-invasive treatment of uterine fibroid cells

Fluorescent compounds useful in the determination of chloramphenicol acetyltransferase (CAT) enzyme activity are described. The compounds are 'fluorescent derivatives related in structure to chloramphenicol and are acylated in the presence of CAT to produce fluorescent mono- and diacylated products, which are then physically separated from the reaction mixture and quantitated by means of their fluorescence and/or absorbance. Fluorescent molecules conjugated to chloramphenicol include derivatives of fluorescein, rhodamine, coumarin, dimethylaminonaph-thalene sulfonic acid (dansyl), pyrene, anthracene, nitrobenz-oxadiazole (NBD), acridine and dipyrrometheneboron difluoride.

Fluorescent chloramphenicol derivatives for determination of

Fluorescent compounds useful in the determination of chloramphenicol acetyltransferase (CAT) enzyme activity are described. The compounds are fluorescent derivatives related in structure to chloramphenicol comprising a base, ##STR1## substituted at one to five aromatic ring positions by substituents, which may be the same or different, that are alkyl-, hydroxy-, alkoxy-, aryl-, halo-, nitro-, amino-, alkylamido-, or arylamido-; and a fluorescent moiety linked to the base at --NH-- by an aliphatic chain of 1-12 atoms other than hydrogen, where such atoms are carbon, nitrogen, oxygen, or sulfur, or combinations thereof. The substrate compounds are acylated in the presence of CAT to produce fluorescent mono- and diacylated products, which are then physically separated from the reaction mixture and quantitated by means of their fluorescence and/or absorbance. Fluorescent molecules conjugated to chloramphenicol include derivatives of fluorescein, rhodamine, coumarin, dimethylaminonaphthalene sulfonic acid (dansyl), pyrene, anthracene, nitrobenzoxadiazole (NBD), acridine and dipyrrometheneboron difluoride.

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Menlo Park, CA, United States of America

Steven L Young