Abstract: It is disclosed herein that that certain alkylphosphocholine analogs are preferentially taken up by multiple myeloma tumor cells. The alkylphophocholine analogs are compounds having the formula: or salts thereof, wherein n is an integer from 12 to 24; and R2 is —N+H3, —N+H2X, —N+HX2, or —N+HX3, wherein each X is independently —CH3 or —C2H5. The compounds can be used to treat multiple myeloma or to detect multiple myeloma. In therapeutic treatment, R1 includes a radionuclide that locally delivers therapeutic dosages of radiation to the multiple myeloma tumors cells that preferentially take up the compound. In detection/imaging applications, R1 includes a detection moiety, such as a fluorophore or a radiolabel.

Abstract: It is disclosed herein that that certain alkylphosphocholine analogs are preferentially taken up by multiple myeloma tumor cells. The alkylphophocholine analogs are compounds having the formula: or salts thereof, wherein n is an integer from 12 to 24; and R2 is —N+H3, —N+H2X, —N+HX2, or —N+HX3, wherein each X is independently —CH3 or —C2H5. The compounds can be used to treat multiple myeloma or to detect multiple myeloma. In therapeutic treatment, R1 includes a radionuclide that locally delivers therapeutic dosages of radiation to the multiple myeloma tumors cells that preferentially take up the compound. In detection/imaging applications, R1 includes a detection moiety, such as a fluorophore or a radiolabel.

Abstract: The present invention provides methods, compositions and kits for discriminating between COX-1 and COX-2 activity. In particular, the prevent invention provides for the detection and/or measurement of COX-2 activity in subjects, samples thereof, and in laboratory tests. The present invention discloses that 2-arachidonylglycerol is a COX-2 selective substrate which is metabolized by COX-2 to prostaglandin glycerol esters (PG-Gs) and that the diversity of PG-Gs parallels that of arachidonic acid derived metabolites of COX. The present invention also provides certain novel COX-2 selective metabolites including prostaglandin I2-glycerol ester (PGI2-G) and 6-keto-prostaglandin F1?-glycerol ester. Methods and kits are described for detecting COX-2 activity comprising detecting PG-Gs (including the novel PG-Gs disclosed herein). Uses for these methods and kits include the detection and monitoring of inflammation and tumors or cancer.

Abstract: A method of detecting an activity of a COX-2 enzyme in a subject that includes obtaining a sample of the subject; detecting an amino acid eicosanoid metabolite in the sample, wherein the presence of the amino acid eicosanoid metabolite indicates the activity of the COX-2 enzyme of the subject. Preferably the amino acid eicosanoid metabolite is a PGH2-Gly or HETE-Gly metabolite. The metabolite may be detected based on metabolism of a COX-2-selective substrate. Preferably, the substrate is a lipoamino acid. More preferably, the lipoamino acid is selected from NAGly, N-arachidonyl-alanine, and ?-arachidonyl aminobutuyic acid.

Abstract: The present invention provides methods, compositions and kits for discriminating between COX-1 and COX-2 activity. In particular, the prevent invention provides for the detection and/or measurement of COX-2 activity in subjects, samples thereof, and in laboratory tests. The present invention discloses that 2-arachidonylglycerol is a COX-2 selective substrate which is metabolized by COX-2 to prostaglandin glycerol esters (PG-Gs) and that the diversity of PG-Gs parallels that of arachidonic acid derived metabolites of COX. The present invention also provides certain novel COX-2 selective metabolites including prostaglandin I2-glycerol ester (PGI2-G) and 6-keto-prostaglandin F1a-glycerol ester. Methods and kits are described for detecting COX-2 activity comprising detecting PG-Gs (including the novel PG-Gs disclosed herein). Uses for these methods and kits include the detection and monitoring of inflammation and tumors or cancer.

Abstract: A method of detecting an activity of a COX-2 enzyme in a subject that includes obtaining a sample of the subject; detecting an amino acid eicosanoid metabolite in the sample, wherein the presence of the amino acid eicosanoid metabolite indicates the activity of the COX-2 enzyme of the subject. Preferably the amino acid eicosanoid metabolite is a PGH2-Gly or HETE-Gly metabolite. The metabolite may be detected based on metabolism of a COX-2-selective substrate. Preferably, the substrate is a lipoamino acid. More preferably, the lipoamino acid is selected from NAGly, N-arachidonyl-alanine, and &dgr;-arachidonyl aminobutuyic acid.

Abstract: The present invention relates generally to cyclooxygenase enzymes (COX) and more particularly the COX-2 enzyme. The present invention provides compositions, methods and articles of manufacture (kits) for determining the COX-2 activity in a sample of a subject, such as a patient or a cell culture. The present invention is useful in monitoring inflammation and cancer, or other disease processes, in patients in a clinical setting.

Abstract: The present invention provides methods, compositions and kits for discriminating between COX-1 and COX-2 activity. In particular, the prevent invention provides for the detection and/or measurement of COX-2 activity in subjects, samples thereof, and in laboratory tests. The present invention discloses that 2-arachidonylglycerol is a COX-2 selective substrate which is metabolized by COX-2 to prostaglandin glycerol esters (PG-Gs) and that the diversity of PG-Gs parallels that of arachidonic acid derived metabolites of COX. The present invention also provides certain novel COX-2 selective metabolites including prostaglandin I2-glycerol ester (PGI2-G) and 6-keto-prostaglandin F1&agr;-glycerol ester. Methods and kits are described for detecting COX-2 activity comprising detecting PG-Gs (including the novel PG-Gs disclosed herein). Uses for these methods and kits include the detection and monitoring of inflammation and tumors or cancer.